标签归档：fmk

Z-VDVAD-FMK

发表于由

Z-VDVAD-FMK;

Z-VDVAD-FMK 是一种特异性的 caspase-2 抑制剂。Z-VDVAD-FMK 可减少 Lovastatin 诱导的细胞凋亡 (apoptosis)。

Z-VDVAD-FMKamp;;

Z-VDVAD-FMK Chemical Structure

CAS No. : 210344-92-6

规格 是否有货
1 mg 询价
5 mg 询价
10 mg 询价

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生物活性

Z-VDVAD-FMK is a special inhibitor of caspase-2. Z-VDVAD-FMK produces a reduction in Lovastatin-induced apoptosis[1][2][3].

IC50 Target[1]

Caspase-2

;

体外研究
(In Vitro)

Cotreatment of cells with the caspase inhibitors Ac-DEVD-CHO, Z-VDVAD-FMK (100 μM), Z-IETD-fmk, and Z-LEHD-fmk alone or in combination, or overexpression of CrmA, prevents many morphological features of apoptosis but not loss of mitochondrial membrane potential (DCm), phospatidilserine exposure, and cell death[1].
Z-VDVAD-FMK (2 μM) greatly inhibits the Rho-kinase activity in HMEC-1 cells stimulated by Thrombin and displays no effect on control cells[2]. 
Z-VDVAD-FMK (zVDVAD-fmk) produces a reduction in Lovastatin-induced apoptosis. Z-VDVAD-FMK (100 μM) significantly reduces Lovastatin-induced loss of DNA by 19.1±8.3%[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: The human T-cell leukemia Jurkat (Clone E6.1, ATCC TIB-152)
Concentration: 100 μM
Incubation Time: 22 hours
Result: Prevented Doxorubicin (1 μM)-induced nuclear apoptosis, but not cell death.

分子量

695.73

Formula

C32H46FN5O11
CAS 号

210344-92-6
Sequence Shortening

{Cbz}-V{Asp(OMe)}-VA-{Asp(OMe)}-CH2F
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. S Gamen, et al. Doxorubicin treatment activates a Z-VAD-sensitive caspase, which causes deltapsim loss, caspase-9 activity, and apoptosis in Jurkat cells. Exp Cell Res. 2000 Jul 10;258(1):223-35.

    [2]. Cédric Sapet, et al. Thrombin-induced endothelial microparticle generation: identification of a novel pathway involving ROCK-II activation by caspase-2. Blood. 2006 Sep 15;108(6):1868-76.

    [3]. Simon W Rabkin, et al. Lovastatin-induced cardiac toxicity involves both oncotic and apoptotic cell death with the apoptotic component blunted by both caspase-2 and caspase-3 inhibitors. Toxicol Appl Pharmacol. 2003 Dec 15;193(3):346-55.

Z-LEHD-FMK TFA

发表于由

Z-LEHD-FMK TFA;

Z-LEHD-FMK TFA 是一种选择性和不可逆的 caspase-9 抑制剂，可防止致命的再灌注损伤并减弱细胞凋亡。Z-LEHD-FMK TFA 在大鼠脊髓损伤模型中也表现出神经保护作用。

Z-LEHD-FMK TFAamp;;

Z-LEHD-FMK TFA Chemical Structure

CAS No. : 524746-03-0

规格 是否有货
100 mg ; 询价 ;
250 mg ; 询价 ;
500 mg ; 询价 ;

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Z-LEHD-FMK TFA 的其他形式现货产品:

Z-LEHD-FMK

生物活性

Z-LEHD-FMK TFA is a selective and irreversible inhibitor of caspase-9, protects against lethal reperfusion injury and attenuates apoptosis. Z-LEHD-FMK TFA exhibits the neuroprotective effect in a rat model of spinal cord trauma[1][2][3].

IC50 Target

Caspase-9

;

体外研究
(In Vitro)

Z-LEHD-FMK (20 μM; pretreated for 30 min) completely protects HCT116 and 293 cells from TRAIL-induced toxicity[1].
Z-LEHD-FMK (20 μM ; 6 h) protects normal human hepatocytes from TRAIL-induced apoptosis[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis[1]

Cell Line: SW480, H460, HCT116 and 293 cells
Concentration: 20 μM
Incubation Time: Pretreated for 30 min
Result: Protected HCT116 and 293 cells from TRAIL-induced apoptosis.

Western Blot Analysis[1]

Cell Line: HCT116, SW480 cells
Concentration: 20 μM
Incubation Time: 2 h
Result: Protected procaspase 3 from cleavage in HCT116 cells but not in SW480 cells, especially at the 16-h time point.

体内研究
(In Vivo)

Z-LEHD-FMK (0.8 μmol/kg; i.v. for 7 d) protects neurons, glia, myelin, axons, and intracellular organelles in spinal cord injury (SCI) rats[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Wistar albino rats (250-350 g) with SCI[2]
Dosage: 0.8 μmol/kg
Administration: I.v. for 1 or 7 days
Result: Decreased the mean apoptotic cell count at 24 hours and 7 days postinjury.

分子量

804.74

Formula

C34H44F4N6O12
CAS 号

524746-03-0
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
Solvent Solubility
In Vitro:;

H2O

Peptide Solubility and Storage Guidelines:

1.;;Calculate the length of the peptide.

2.;;Calculate the overall charge of the entire peptide according to the following table:

; Contents Assign value
Acidic amino acid Asp (D), Glu (E), and the C-terminal -COOH. -1
Basic amino acid Arg (R), Lys (K), His (H), and the N-terminal -NH2 +1
Neutral amino acid Gly (G), Ala (A), Leu (L), Ile (I), Val (V), Cys (C), Met (M), Thr (T), Ser (S), Phe (F), Tyr (Y), Trp (W), Pro (P), Asn (N), Gln (Q) 0

3.;;Recommended solution:

Overall charge of peptide Details
Negative (lt;0) 1.;;Try to dissolve the peptide in water first.
2.;;If water fails, add NH4OH (lt;50 μL).
3.;;If the peptide still does not dissolve, add DMSO (50-100 μL) to solubilize the peptide.
Positive (gt;0) 1.;;Try to dissolve the peptide in water first.
2.;;If water fails, try dissolving the peptide in a 10%-30% acetic acid solution.
3.;;If the peptide still does not dissolve, try dissolving the peptide in a small amount of DMSO.
Zero (=0) 1.;;Try to dissolve the peptide in organic solvent (acetonitrile, methanol, etc.) first.
2.;;For very hydrophobic peptides, try dissolving the peptide in a small amount of DMSO, and then dilute the solution with water to the desired concentration.
参考文献

  • [1]. Ozoren N, et, al. The caspase 9 inhibitor Z-LEHD-FMK protects human liver cells while permitting death of cancer cells exposed to tumor necrosis factor-related apoptosis-inducing ligand. Cancer Res. 2000 Nov 15; 60(22): 6259-65.

    [2]. Colak A, et, al. Neuroprotection and functional recovery after application of the caspase-9 inhibitor z-LEHD-fmk in a rat model of traumatic spinal cord injury. J Neurosurg Spine. 2005 Mar; 2(3): 327-34.

    [3]. Mocanu MM, et, al. Caspase inhibition and limitation of myocardial infarct size: protection against lethal reperfusion injury. Br J Pharmacol. 2000 May; 130(2): 197-200.

Z-IETD-FMK(Synonyms: Z-IE(OMe)TD(OMe)-FMK)

发表于由

Z-IETD-FMK;(Synonyms: Z-IE(OMe)TD(OMe)-FMK) 纯度: ge;98.0%

Z-IETD-FMK (Z-IE(OMe)TD(OMe)-FMK) 是一种具有细胞渗透作用的选择性 caspase-8 抑制剂。Z-IETD-FMK 也是颗粒酶 B (granzyme B) 抑制剂。

Z-IETD-FMKamp;;(Synonyms: Z-IE(OMe)TD(OMe)-FMK)

Z-IETD-FMK Chemical Structure

CAS No. : 210344-98-2

规格 价格 是否有货 数量
10;mM;*;1 mL in DMSO ￥4321 In-stock
1 mg ￥1400 In-stock
5 mg ￥3000 In-stock
10 mg ; 询价 ;
50 mg ; 询价 ;

* Please select Quantity before adding items.

Z-IETD-FMK 相关产品

bull;相关化合物库:

  • Bioactive Compound Library Plus
  • Peptidomimetic Library
  • Peptide Library

生物活性

Z-IETD-FMK (Z-IE(OMe)TD(OMe)-FMK) is a selective and cell permeable caspase-8 inhibitor[1]. Z-IETD-FMK is also a granzyme B inhibitor[5].

IC50 Target[1]

Caspase-8

;

体外研究
(In Vitro)

Z-IETD-FMK causes full inhibition only of the proapoptotic effect of TNFα with an IC50 of 0.46 μM[1]. Z-IETD-FMK and Z-VAD-FMK at non-toxic doses are found to be immunosuppressive and inhibit human T cell proliferation induced by mitogens and IL-2. They are shown to block NF-κB in activated primary T cells, but have little inhibitory effect on the secretion of IL-2 and IFN-γ during T cell activation[2]. Z-IETD-FMK inhibits the cleavage of caspase-8 and only partially inhibits the cleavage of caspase-3 and PARP. Z-IETD-FMK can prevent the execution of apoptosis in retinal cells exposed to different apoptotic stimuli[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

Pharmacological inhibition of caspase-8 by z-IETD-FMK robustly reduces tumour outgrowth and this is closely associated with a reduction in the release of pro-inflammatory cytokines, IL-6, TNF-α, IL-18, IL-1α, IL-33, but not IL-1β. Furthermore, inhibition of caspase-8 reduces the recruitment of innate suppressive cells, such as myeloid-derived suppressor cells, but not of regulatory T cells to lungs of tumour-bearing mice[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

654.68

Formula

C30H43FN4O11
CAS 号

210344-98-2
Sequence

Z-Ile-Glu-Thr-Asp-FMK
Sequence Shortening

ZIETDFMK
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -80deg;C 2 years
-20deg;C 1 year
In solvent -80deg;C 6 months
-20deg;C 1 month
溶解性数据
In Vitro:;

DMSO : 41.67 mg/mL (63.65 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.5275 mL 7.6373 mL 15.2746 mL
5 mM 0.3055 mL 1.5275 mL 3.0549 mL
10 mM 0.1527 mL 0.7637 mL 1.5275 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂：;10% DMSO ;; 40% PEG300 ;; 5% Tween-80 ;; 45% saline

    Solubility: ≥ 2.08 mg/mL (3.18 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.18 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂：;10% DMSO ;; 90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (3.18 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.18 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 3.

    请依序添加每种溶剂：;10% DMSO ;; 90% corn oil

    Solubility: ≥ 2.08 mg/mL (3.18 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.18 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 MCE 网站选购。
参考文献

  • [1]. Cowburn AS, et al. z-VAD-fmk augmentation of TNF alpha-stimulated neutrophil apoptosis is compound specific and does not involve the generation of reactive oxygen species.

    [2]. Lawrence CP, et al. Suppression of human T cell proliferation by the caspase inhibitors, z-VAD-FMK and z-IETD-FMK is independent of their caspase inhibition properties. Toxicol Appl Pharmacol. 2012 Nov 15;265(1):103-12.

    [3]. Tezel G, et al. Inhibition of caspase activity in retinal cell apoptosis induced by various stimuli in vitro. Invest Ophthalmol Vis Sci. 1999 Oct;40(11):2660-7.

    [4]. Terlizzi M, et al. Pharmacological inhibition of caspase-8 limits lung tumour outgrowth. Br J Pharmacol. 2015 Aug;172(15):3917-28.

    [5]. Yang J, et al. Granzyme B Is an Essential Mediator in CD8+ T Cell Killing of Theileria parva-Infected Cells.Infect Immun. 2018 Dec 19;87(1). pii: e00386-18.
Cell Assay
[2]

T cell proliferation following mitogen stimulation is determined using [3H]-thymidine incorporation. In brief, PBMCs or purified T cells are seeded at 1×106 cells/mL in 96 well plates and stimulated with either PHA (5 μg/mL or co-stimulated with anti-CD3 mAb (5 μg/mL) and anti-CD28 mAb (2.5 μg/mL) in the presence or absence of caspase inhibitor Z-IETD-FMK. The cells are cultured for 72 h with the last 16 h pulsed with [[3H]-labelled methyl-thymidine (0.037 MBq) prior to harvest onto glass fibre filter mats using a Tomtec automated multi-well harvester[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[4]

Mice: Mice are divided into three groups: (1) naive, non-treated, mice; (2) CTR (control), i.t. instilled with NMU; and (3) lung cancer-bearing mice treated with Z-IETD-FMK (0.5 μg per mouse). The involvement of caspase-8 in lung cancer development is the determined at different time points (3, 7 and 28 days)[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

  • [1]. Cowburn AS, et al. z-VAD-fmk augmentation of TNF alpha-stimulated neutrophil apoptosis is compound specific and does not involve the generation of reactive oxygen species.

    [2]. Lawrence CP, et al. Suppression of human T cell proliferation by the caspase inhibitors, z-VAD-FMK and z-IETD-FMK is independent of their caspase inhibition properties. Toxicol Appl Pharmacol. 2012 Nov 15;265(1):103-12.

    [3]. Tezel G, et al. Inhibition of caspase activity in retinal cell apoptosis induced by various stimuli in vitro. Invest Ophthalmol Vis Sci. 1999 Oct;40(11):2660-7.

    [4]. Terlizzi M, et al. Pharmacological inhibition of caspase-8 limits lung tumour outgrowth. Br J Pharmacol. 2015 Aug;172(15):3917-28.

    [5]. Yang J, et al. Granzyme B Is an Essential Mediator in CD8+ T Cell Killing of Theileria parva-Infected Cells.Infect Immun. 2018 Dec 19;87(1). pii: e00386-18.

Z-WEHD-FMK

发表于由

Z-WEHD-FMK; 纯度: 98.64%

Z-WEHD-FMK 是一种强效具有细胞通透性可逆的 caspase-1/5 抑制剂。Z-WEHD-FMK 也抑制 cathepsin B 的活性 (IC50=6 μM)。Z-WEHD-FMK 可用于检测细胞凋亡。

Z-WEHD-FMKamp;;

Z-WEHD-FMK Chemical Structure

CAS No. : 210345-00-9

规格 价格 是否有货 数量
10;mM;*;1 mL in DMSO ￥5460 In-stock
5 mg ￥4500 In-stock
10 mg ￥6500 In-stock
50 mg ￥19500 In-stock
100 mg ; 询价 ;
200 mg ; 询价 ;

* Please select Quantity before adding items.

Z-WEHD-FMK 相关产品

bull;相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Metabolism/Protease Compound Library
  • Anti-Cancer Compound Library
  • Pyroptosis Compound Library
  • Angiogenesis Related Compound Library
  • Peptide Library

生物活性

Z-WEHD-FMK is a potent, cell-permeable and irreversible caspase-1/5 inhibitor. Z-WEHD-FMK also exhibits a robust inhibitory effect on cathepsin B activity (IC50=6 μM). Z-WEHD-FMK can be used to investigate cells for evidence of apoptosis[1][2][4].

IC50 Target[1][2]

Caspase-1

;

体外研究
(In Vitro)

Z-WEHD-FMK (80 μM; 9 hours) elicits a near-complete blockage of C. trachomatis-induced cleavage of golgin-84 and increases GM130 expression in cells[1].
Z-WEHD-FMK (30 min before being exposed to E. piscicida) effectively inhibits 0909I E. piscicida induced ZF4 cells cytotoxicity and pyroptotic morphology. And in addition, it also inhibits the cytotoxicity induced by cytosolic LPS delivery[2].
Z-WEHD-FMK (20 μM;18-24 hours following Cr3+,Ni2+, and Co2+) significantly induces a decrease of 76% to 86% in IL-1β release with 200 to 400 ppm Cr3+, it also induces a decrease of 35% to 45% with 48 ppm Ni2+ or higher, Finally, this caspase-1 inhibitor induced a decrease with 6 ppm Co2+, down to a level below the detection threshold, and a decrease of 40% to 48% with 12 to 24 ppm Co2+ in bone marrow-derived macrophages (BMDM)[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: C. trachomatis– or mock-infected HeLa cells
Concentration: 80 μM
Incubation Time: 9 hours
Result: Increased golgin-84 and GM130 expression.

Cell Viability Assay[2]

Cell Line: Mycoplasma free-ZF4 cells
Concentration:
Incubation Time: 30 min before being exposed to E. piscicida
Result: Inhibited ZF4 cells cytotoxicity and pyroptotic morphology.

分子量

763.77

Formula

C37H42FN7O10
CAS 号

210345-00-9
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -80deg;C 2 years
-20deg;C 1 year
In solvent -80deg;C 6 months
-20deg;C 1 month
溶解性数据
In Vitro:;

DMSO : 100 mg/mL (130.93 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.3093 mL 6.5465 mL 13.0929 mL
5 mM 0.2619 mL 1.3093 mL 2.6186 mL
10 mM 0.1309 mL 0.6546 mL 1.3093 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂：;10% DMSO ;; 40% PEG300 ;; 5% Tween-80 ;; 45% saline

    Solubility: ≥ 2.5 mg/mL (3.27 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (3.27 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂：;10% DMSO ;; 90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (3.27 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (3.27 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 3.

    请依序添加每种溶剂：;10% DMSO ;; 90% corn oil

    Solubility: ≥ 2.5 mg/mL (3.27 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (3.27 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 MCE 网站选购。
参考文献

  • [1]. Kamada S, et al. Caspase-4 and caspase-5, members of the ICE/CED-3 family of cysteine proteases, are CrmA-inhibitable proteases.Cell Death Differ. 1997 Aug;4(6):473-8.

    [2]. Yang D, et al. Sensing of cytosolic LPS through caspy2 pyrin domain mediates noncanonical inflammasome activation in zebrafish.Nat Commun. 2018 Aug 3;9(1):3052.

    [3]. Ferko MA, et al. Effects of metal ions on caspase-1 activation and interleukin-1β release in murine bone marrow-derived macrophages.PLoS One. 2018 Aug 23;13(8):e0199936.

    [4]. Newman ZL, et al. CA-074Me protection against anthrax lethal toxin.Infect Immun. 2009 Oct;77(10):4327-36.

荧光染料FITC-C6-DEVD-FMK

发表于由

荧光染料Dye Reagents FITC-C6-DEVD-FMK;

FITC-C6-DEVD-FMK 是一种 Caspase-3 荧光标记抑制剂。可用于检测哺乳动物细胞凋亡中的活性 caspase-3。Z-DEVD-FMK 是一种特异性 caspase-3 抑制剂。

FITC-C6-DEVD-FMK

FITC-C6-DEVD-FMK Chemical Structure

规格 是否有货
100 mg ; 询价 ;
250 mg ; 询价 ;
500 mg ; 询价 ;

* Please select Quantity before adding items.

生物活性

FITC-C6-DEVD-FMK, a fluorescently labeled caspase-3 inhibitor, can be used for detection of active caspase-3 in mammalian cells undergoing apoptosis. FITC-C6-DEVD-FMK provides a convenient means for sensitive detection of activated caspase-3 in living cells. Z-DEVD-FMK is a specific caspase-3 inhibitor[1].

分子量

994.99

Formula

C46H51FN6O16S
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Kanthasamy AG, et al. A novel peptide inhibitor targeted to caspase-3 cleavage site of a proapoptotic kinase protein kinase C delta (PKCdelta) protects against dopaminergic neuronal degeneration in Parkinson’s disease models. Free Radic Biol Med. 2006 Nov

Z-YVAD-FMK

发表于由

Z-YVAD-FMK; 纯度: ge;98.0%

Z-YVAD-FMK 是一种具有细胞通透性 caspase-1 和 caspase-4 抑制剂，具有抗炎和抗肿瘤活性。

Z-YVAD-FMKamp;;

Z-YVAD-FMK Chemical Structure

CAS No. : 210344-97-1

规格 价格 是否有货 数量
10;mM;*;1 mL in DMSO ￥6940 In-stock
1 mg ￥2200 In-stock
5 mg ￥5000 In-stock
10 mg ￥8200 In-stock
50 mg ; 询价 ;
100 mg ; 询价 ;

* Please select Quantity before adding items.

Z-YVAD-FMK 相关产品

bull;相关化合物库:

  • Bioactive Compound Library Plus
  • Peptide Library

生物活性

Z-YVAD-FMK is a cell-permeable caspase-1 and -4 inhibitor with anti-inflammatory and anti-tumor activities[1].

IC50 Target

Caspase

;

体外研究
(In Vitro)

Z-YVAD-FMK (100 μM; 24 hours) significantly downregulated the growth inhibition induced by butyrate in Caco-2 cells[1].
Z-YVAD-FMK (20 μM; pre 1 hour; 24 hours) attenuates the apoptotic induction of III-10 on both HepG2 and BEL-7402 cells, the apoptotic rate of -10 on HepG2 cells is reduced by Z-VAD-FMK from 19.88% to 8.34%, while that on BEL-7402 cells is reduced from 17.56% to 11.98%[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: Caco-2 cells
Concentration: 0-100 μM
Incubation Time: 24 hours
Result: Inhibited Caco-2 cells growth.

Apoptosis Analysis[1]

Cell Line: BEL-7402 and HepG2 cells
Concentration: 20 μM
Incubation Time: Pre 1 hour; 24 hours
Result: Induced a caspase-dependent apoptosis in cells.

分子量

630.66

Formula

C31H39FN4O9
CAS 号

210344-97-1
Sequence

Z-Tyr-Val-Ala-Asp-FMK
Sequence Shortening

Z-YVAD-FMK
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -80deg;C 2 years
-20deg;C 1 year
In solvent -80deg;C 6 months
-20deg;C 1 month
溶解性数据
In Vitro:;

DMSO : 125 mg/mL (198.21 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.5856 mL 7.9282 mL 15.8564 mL
5 mM 0.3171 mL 1.5856 mL 3.1713 mL
10 mM 0.1586 mL 0.7928 mL 1.5856 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂：;10% DMSO ;; 40% PEG300 ;; 5% Tween-80 ;; 45% saline

    Solubility: ≥ 2.08 mg/mL (3.30 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.30 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂：;10% DMSO ;; 90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (3.30 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.30 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 3.

    请依序添加每种溶剂：;10% DMSO ;; 90% corn oil

    Solubility: ≥ 2.08 mg/mL (3.30 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.30 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 MCE 网站选购。
参考文献

  • [1]. Li H1,et al.Aluminum hydroxide adjuvants activate caspase-1 and induce IL-1beta and IL-18 release.J Immunol. 2007 Apr 15;178(8):5271-6.

    [2]. Avivi-Green C, et al. Different molecular events account for butyrate-induced apoptosis in two human colon cancer cell lines.J Nutr. 2002 Jul;132(7):1812-8.

荧光染料FITC-C6-LEHD-FMK

发表于由

荧光染料Dye Reagents FITC-C6-LEHD-FMK;

FITC-C6-LEHD-FMK 是一种 caspase-9 荧光标记抑制剂。可用于检测哺乳动物细胞凋亡中的活性 caspase-9。Z-DEVD-FMK 是一种特异性 caspase-9 抑制剂。

FITC-C6-LEHD-FMK

FITC-C6-LEHD-FMK Chemical Structure

规格 是否有货
100 mg ; 询价 ;
250 mg ; 询价 ;
500 mg ; 询价 ;

* Please select Quantity before adding items.

生物活性

FITC-C6-LEHD-FMK, a fluorescently labeled caspase-9 inhibitor, can be used for detection of active caspase-9 in mammalian cells undergoing apoptosis. FITC-C6-DEVD-FMK provides a convenient means for sensitive detection of activated caspase-9 in living cells. Z-LEHD-FMK is a specific caspase-9 inhibitor[1].

分子量

1031.07

Formula

C49H55FN8O14S
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Ozoren N, et, al. The caspase 9 inhibitor Z-LEHD-FMK protects human liver cells while permitting death of cancer cells exposed to tumor necrosis factor-related apoptosis-inducing ligand. Cancer Res. 2000 Nov 15; 60(22): 6259-65.

Biotin-VAD-FMK

发表于由

生化分析试剂 Biochemical Assay Reagents
Biotin-VAD-FMK; 纯度: ge;98.0%

Biotin-VAD-FMK是可渗透细胞的，不可逆的，由生物素标记的胱天蛋白酶抑制剂，用于鉴定细胞裂解物中的半胱天冬酶活性。

Biotin-VAD-FMK

Biotin-VAD-FMK Chemical Structure

CAS No. : 1135688-15-1

规格 价格 是否有货 数量
1 mg ￥7000 In-stock
5 mg ￥25000 In-stock
10 mg ; 询价 ;
50 mg ; 询价 ;

* Please select Quantity before adding items.

Biotin-VAD-FMK 相关产品

bull;相关化合物库:

  • Bioactive Compound Library Plus
  • Peptidomimetic Library

生物活性

Biotin-VAD-FMK is a cell permeable, irreversible biotin-labeled caspase inhibitor, used to identify active caspases in cell lysates.

IC50 Target

Caspase

;

体外研究
(In Vitro)

Biotin-VAD-FMK is a synthetic peptide designed as a methyl ester to facilitate cell permeability.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

To examine whether caspase-2 is activated in the absence of proteolytic cleavage, an in vivo affinity labeling approach is used, using the biotinylated caspase inhibitor biotin-VAD-fmk that detects only active caspases[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

672.81

Formula

C30H49FN6O8S
CAS 号

1135688-15-1
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20deg;C 3 years
4deg;C 2 years
In solvent -80deg;C 6 months
-20deg;C 1 month
溶解性数据
In Vitro:;

DMSO : ≥ 27.3 mg/mL (40.58 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.4863 mL 7.4315 mL 14.8630 mL
5 mM 0.2973 mL 1.4863 mL 2.9726 mL
10 mM 0.1486 mL 0.7432 mL 1.4863 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
参考文献

  • [1]. Li J, et al. Nitric oxide suppresses apoptosis via interrupting caspase activation and mitochondrial dysfunction in cultured hepatocytes. J Biol Chem. 1999 Jun 11;274(24):17325-33.

    [2]. Samraj AK, et al. Loss of caspase-9 reveals its essential role for caspase-2 activation and mitochondrial membranedepolarization. Mol Biol Cell. 2007 Jan;18(1):84-93.

Z-LEHD-FMK

发表于由

Z-LEHD-FMK; 纯度: ge;98.0%

Z-LEHD-FMK 是一种选择性和不可逆的 caspase-9 抑制剂，可防止致命的再灌注损伤并减弱细胞凋亡。Z-LEHD-FMK 在大鼠脊髓损伤模型中也表现出神经保护作用。

Z-LEHD-FMKamp;;

Z-LEHD-FMK Chemical Structure

CAS No. : 210345-04-3

规格 价格 是否有货 数量
1 mg ￥9800 In-stock
5 mg ; 询价 ;
10 mg ; 询价 ;

* Please select Quantity before adding items.

生物活性

Z-LEHD-FMK is a selective and irreversible inhibitor of caspase-9, protects against lethal reperfusion injury and attenuates apoptosis. Z-LEHD-FMK exhibits the neuroprotective effect in a rat model of spinal cord trauma[1][2][3].

IC50 Target[1]

Caspase-9

;

体外研究
(In Vitro)

Z-LEHD-FMK (20 μM; pretreated for 30 min) completely protects HCT116 and 293 cells from TRAIL-induced toxicity[1].
Z-LEHD-FMK (20 μM ; 6 h) protects normal human hepatocytes from TRAIL-induced apoptosis[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis[1]

Cell Line: SW480, H460, HCT116 and 293 cells
Concentration: 20 μM
Incubation Time: Pretreated for 30 min
Result: Protected HCT116 and 293 cells from TRAIL-induced apoptosis.

Western Blot Analysis[1]

Cell Line: HCT116, SW480 cells
Concentration: 20 μM
Incubation Time: 2 h
Result: Protected procaspase 3 from cleavage in HCT116 cells but not in SW480 cells, especially at the 16-h time point.

体内研究
(In Vivo)

Z-LEHD-FMK (0.8 μmol/kg; i.v. for 7 d) protects neurons, glia, myelin, axons, and intracellular organelles in spinal cord injury (SCI) rats[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Wistar albino rats (250-350 g) with SCI[2]
Dosage: 0.8 μmol/kg
Administration: I.v. for 1 or 7 days
Result: Decreased the mean apoptotic cell count at 24 hours and 7 days postinjury.

分子量

690.72

Formula

C32H43FN6O10
CAS 号

210345-04-3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -80deg;C 2 years
-20deg;C 1 year
In solvent -80deg;C 6 months
-20deg;C 1 month
溶解性数据
In Vitro:;

DMSO : 100 mg/mL (144.78 mM; Need ultrasonic and warming)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.4478 mL 7.2388 mL 14.4776 mL
5 mM 0.2896 mL 1.4478 mL 2.8955 mL
10 mM 0.1448 mL 0.7239 mL 1.4478 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
参考文献

  • [1]. Ozoren N, et, al. The caspase 9 inhibitor Z-LEHD-FMK protects human liver cells while permitting death of cancer cells exposed to tumor necrosis factor-related apoptosis-inducing ligand. Cancer Res. 2000 Nov 15; 60(22): 6259-65.

    [2]. Colak A, et, al. Neuroprotection and functional recovery after application of the caspase-9 inhibitor z-LEHD-fmk in a rat model of traumatic spinal cord injury. J Neurosurg Spine. 2005 Mar; 2(3): 327-34.

    [3]. Mocanu MM, et, al. Caspase inhibition and limitation of myocardial infarct size: protection against lethal reperfusion injury. Br J Pharmacol. 2000 May; 130(2): 197-200.

Z-VRPR-FMK TFA(Synonyms: VRPR)

发表于由

Z-VRPR-FMK TFA;(Synonyms: VRPR) 纯度: 95.92%

Z-VRPR-FMK (TFA) (VRPR) 是一种四肽，也是选择性和不可逆的粘膜相关淋巴组织淋巴瘤易位蛋白1 (MALT1) 抑制剂。Z-VRPR-FMK (TFA) 有抗甲型流感病毒 (IAV) 感染的作用。

Z-VRPR-FMK TFAamp;;(Synonyms: VRPR)

Z-VRPR-FMK TFA Chemical Structure

规格 价格 是否有货 数量
500 μg ￥7800 In-stock

* Please select Quantity before adding items.

生物活性

Z-VRPR-FMK (TFA) (VRPR), a tetrapeptide, is a selective and irreversible MALT1 (Mucosa-associated lymphoid tissue lymphoma translocation protein 1) inhibitor. Z-VRPR-FMK (TFA) can protect against influenza A virus (IAV) infection[1].

分子量

790.81

Formula

C33H50F4N10O8
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Sealed storage, away from moisture

Pure form -80deg;C 2 years
-20deg;C 1 year

*In solvent : -80deg;C, 6 months; -20deg;C, 1 month (sealed storage, away from moisture)
参考文献

  • [1]. Hatcher JM, et al. Peptide-based covalent inhibitors of MALT1 paracaspase. Bioorg Med Chem Lett. 2019 Jun 1;29(11):1336-1339.