Tutuilamide A 是一种有效的猪胰弹性蛋白酶 (PPE) 抑制剂，IC50 值为 1.2 nM。Tutuilamide A 还抑制人中性粒细胞弹性蛋白酶 (HNE; IC50=0.73 nM) 和激肽释放酶 7 (KLK7; IC50=5.0 nM)。
Tutuilamide A Chemical Structure
CAS No. : 2756129-42-5
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
Tutuilamide A is a potent porcine pancreatic elastase (PPE) inhibitor, with an IC50 of 1.2 nM. Tutuilamide A also inhibits human neutrophil elastase (HNE; IC50=0.73 nM) and kallikrein 7 (KLK7; IC50=5.0 nM)[1].
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]. Chen QY, et, al. Ahp-Cyclodepsipeptides as tunable inhibitors of human neutrophil elastase and kallikrein 7: Total synthesis of tutuilamide A, serine protease selectivity profile and comparison with lyngbyastatin 7. Bioorg Med Chem. 2020 Dec 1;28(23):115756.
PG-931, an analog of SHU 9119 (HY-P0227), is a potent melanocortin 4 (MC4) receptor (IC50=0.58 nM) agonist and is more selective than for the hMC3R (IC50=55 nM) or the hMC5R (IC50=2.4 nM). PG-931 can reverse haemorrhagic shock and prevent multiple organ damage in vivo[2].
PG-931 (intravenous injection; 13-108 nmol/kg; single dose) produces a dose-dependent restoration of cardiovascular and respiratory functions, and improved survival in Wistar rats with haemorrhagic shock[2].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
Wistar rats[2]
Dosage:
13-108 nmol/kg
Administration:
Intravenous injection; single dose
Result:
Exhibitd an anti-shock effect occurred at nanomolar doses.
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]. D Giuliani, et al. Selective melanocortin MC4 receptor agonists reverse haemorrhagic shock and prevent multiple organ damage. Br J Pharmacol
[2]. P Grieco, et al. Extensive structure-activity studies of lactam derivatives of MT-II and SHU-9119: their activity and selectivity at human melanocortin receptors 3, 4, and 5. J Pept Res
HDAC-IN-30 is a novel multi-target HDAC inhibitor, including HDAC1 (IC50=13.4 nM),HDAC2 (IC50=28.0 nM), HDAC3 (IC50=9.18 nM), HDAC6 (IC50=42.7 nM), HDAC8 (IC50=131 nM). HDAC-IN-30 exhibits potent antitumor efficacy[1].
IC50 Target
HDAC1
13.4 nM (IC50)
HDAC2
28.0 nM (IC50)
HDAC3
9.18 nM (IC50)
HDAC6
42.7 nM (IC50)
HDAC8
131 nM (IC50)
体外研究 (In Vitro)
HDAC-IN-30 (compound 8 h; 0.5, 1, 2 μM; 48 hours) can effectively activate the p53 pathway by promoting the phosphorylation of p53[1]. HDAC-IN-30 (0, 1, 2.5, 5 mM; 48 hours; HepG2 cells) induces cell cycle arrest at the G2 phase in a concentration-dependent manner[1]. HDAC-IN-30 (0, 1, 2.5, 5 mM; 48 hours) possesses prominent anticancer activity in HepG2 cells[1].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Western Blot Analysis[1]
Cell Line:
HepG2 cells
Concentration:
0.5, 1, 2 μM
Incubation Time:
24 hours
Result:
Could effectively activate the p53 pathway by promoting the phosphorylation of p53
Cell Cycle Analysis[1]
Cell Line:
HepG2 cells
Concentration:
0, 1, 2.5, 5 μM
Incubation Time:
48 hours
Result:
Cells were arrested at the G2 phase in a dose-dependent manner.
Apoptosis Analysis[1]
Cell Line:
HepG2 cells
Concentration:
0, 1, 2.5, 5 μM
Incubation Time:
24 hours
Result:
Possessed prominent anticancer activity in HepG2 cells.
体内研究 (In Vivo)
HDAC-IN-30 (12, 24 mg/kg; intraperitoneal injection, every two days for 4 weeks) exhibits potent anticancer activity and no side effects even at high dose (24 mg/kg)[1].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
HepG2 xenograft mouse model[1]
Dosage:
12, 24 mg/kg
Administration:
Intraperitoneal injection, every 2 days, 4 weeks
Result:
Exhibited potent anticancer activity
分子量
405.45
Formula
C22H23N5O3
CAS 号
2756809-34-2
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]. Liu Q, et al. Discovery of phthalazino [1, 2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway. Eur J Med Chem. 2022, 229:114058.
Garcinol, a polyisoprenylated benzophenone harvested from Garcinia indica, exerts anti-cholinesterase properties towards acetyl cholinesterase (AChE) and butyrylcholinesterase (BChE) with IC50s of 0.66 µM and 7.39 µM, respectively[1]. Garcinol also inhibits histone acetyltransferases (HATs, IC50= 7 μM) and p300/CPB-associated factor (PCAF, IC50 = 5 μM). Garcinol has anti-inflammatory and anti-cancer activity[2].
IC50 & Target
Human Endogenous Metabolite
体外研究 (In Vitro)
Garcinol (10-50 µM; 24-72 hours) can inhibit the proliferation of two HNSCC cell lines tested (CAL27 and UMSCC1) in a time- and dose-dependent manner[3]. Garcinol (10-50 µM; 24-72 hours) induces apoptosis in HNSCC cells[3]. Garcinol (50 µM; 1-6 hours) suppresses phosphorylation and degradation of the constitutive IκBα in a time-dependent manner[3].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Proliferation Assay[3]
Cell Line:
CAL27 and UMSCC1 cells
Concentration:
10, 25, 50 µM
Incubation Time:
24, 48, and 72 hours
Result:
Inhibited the proliferation of two HNSCC cell lines in a time- and dose-dependent manner.
Apoptosis Analysis[3]
Cell Line:
CAL27 and UMSCC1 cells
Concentration:
10, 25, 50 µM
Incubation Time:
24, 48, and 72 hours
Result:
Induced apoptosis in HNSCC cells.
Western Blot Analysis[3]
Cell Line:
CAL27 cells
Concentration:
50 µM
Incubation Time:
1, 2, 4, 6 hours
Result:
Suppressed phosphorylation and degradation of the constitutive IκBα in a time-dependent manner.
体内研究 (In Vivo)
Garcinol (i.p.; 1 and 2 mg/kg; five times/week for 4 consecutive weeks) induces significant inhibition of tumor growth[3].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
Five-week-old athymic nu/nu male mice bearing subcutaneous CAL27 tumors[3]
Dosage:
1 and 2 mg/kg
Administration:
I.p.; five times/week for 4 consecutive weeks
Result:
Induced significant inhibition of tumor growth.
分子量
602.80
Formula
C38H50O6
CAS 号
78824-30-3
中文名称
山竹子素
运输条件
Room temperature in continental US; may vary elsewhere.
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
*以上所有助溶剂都可在 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献
[1]. Lenta BN, et al. Leishmanicidal and cholinesterase inhibiting activities of phenolic compounds from Allanblackia monticola and Symphonia globulifera. Molecules. 2007 Jul 20;12(8):1548-57.
[3]. Li F, et al. Garcinol, a polyisoprenylated benzophenone modulates multiple proinflammatory signalingcascades leading to the suppression of growth and survival of head and neck carcinoma. Cancer Prev Res (Phila). 2013 Aug;6(8):843-54.
Icaritin (Anhydroicaritin) is a prenylflavonoid derivative from Epimedium Genusis and potently inhibits proliferation of K562 cells (IC50 of 8 µM) and primary CML cells (IC50 of 13.4 µM for CML-CP and 18 µM for CML-BC). Icaritin can regulate MAPK/ERK/JNK and JAK2/STAT3 /AKT signalings, also enhances osteogenesis[1][2][3.
体外研究 (In Vitro)
Icaritin (4-64 µM; 48 hours; K562, imatinib-resistant cells and primary CML cells) treatment inhibits proliferation of K562, imatinib-resistant cells and primary CML cells [1]. Icaritin (0-64 µM; 48 hours; K562 and primary cells) treatment induces K562 or primary cells apoptosis in an concentration dependent manner[1]. Icaritin (32 µM; K562 cells) treatment increases cell population in the sub-G1 phase in K562 cells[1]. Icaritin (0-64 µM; 48 hours; K562 cells) treatment inhibits MAPK/ERK/JNK downstream signaling and diminishes Jak2/Stat3/Akt expression. Icaritin treatment also significantly inhibits Bcl-2 protein expression and up-regulated Bax protein expression in K562 with a dose-dependent manner accompanied by the cleavage activation of caspase-3 or caspase-9, and a down-regulated expression of Apaf-1[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Proliferation Assay[1]
Cell Line:
K562, imatinib-resistant cells and primary CML cells
Concentration:
4 µM, 8 µM, 16 µM, 32 µM and 64 µM
Incubation Time:
48 hours
Result:
Inhibited cell proliferation.
Apoptosis Analysis[1]
Cell Line:
K562 or primary cells
Concentration:
0 µM, 4 µM, 8 µM, 16 µM, 32 µM and 64 µM
Incubation Time:
48 hours
Result:
Induced K562 or primary cells apoptosis.
Cell Cycle Analysis[1]
Cell Line:
K562 cells
Concentration:
32 µM
Incubation Time:
Result:
Cell population in the sub-G1 phase was increased.
Western Blot Analysis[1]
Cell Line:
K562 cells
Concentration:
0 µM, 4 µM, 8 µM, 16 µM, 32 µM and 64 µM
Incubation Time:
48 hours
Result:
Inhibited MAPK/ERK/JNK downstream signaling and diminishes Jak2/Stat3/Akt expression.
体内研究 (In Vivo)
Icaritin (4-8 mg/kg; intraperitoneal injection; daily; for 10 weeks; female NOD-SCID nude mice) treatment could prolong lifespan of NOD-SCID nude mice inoculated with K562 cells without suppression of bone marrow in mouse leukemia model[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
Female NOD-SCID nude mice (6-8 weeks old) with K562 cells[1]
Dosage:
4 mg/kg and 8 mg/kg
Administration:
Intraperitoneal injection; daily; for 10 weeks
Result:
Could prolong lifespan of NOD-SCID nude mice inoculated with K562 cells without suppression of bone marrow.
Clinical Trial
分子量
368.38
Formula
C21H20O6
CAS 号
118525-40-9
中文名称
去水淫羊藿黄素；三七淫羊藿素
运输条件
Room temperature in continental US; may vary elsewhere.
Solubility: 1.51 mg/mL (4.10 mM); Suspended solution; Need ultrasonic
*以上所有助溶剂都可在 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献
[1]. Zhu Jf, et al. Icaritin shows potent anti-leukemia activity on chronic myeloid leukemia in vitro and in vivo by regulating MAPK/ERK/JNK and JAK2/STAT3 /AKT signalings. PLoS One. 2011;6(8):e23720.
[2]. Yao D, et al. Icaritin, an exogenous phytomolecule, enhances osteogenesis but not angiogenesis–an in vitro efficacy study. PLoS One. 2012;7(8):e41264.
[3]. Guo Y, et al. An anticancer agent icaritin induces sustained activation of the extracellular signal-regulated kinase (ERK) pathway and inhibits growth of breast cancer cells. Eur J Pharmacol. 2011 May 11;658(2-3):114-22.
Momordin Ic is a principal saponin constituent of Fructus Kochiae, with with anti-cancer bioactivity. Momordin Ic induces apoptosis through oxidative stress-regulated mitochondrial dysfunction[1][2].
分子量
764.94
Formula
C41H64O13
CAS 号
96990-18-0
中文名称
地肤子皂苷Ic
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Mi Y, et al. Momordin Ic couples apoptosis with autophagy in human hepatoblastoma cancer cells by reactive oxygen species (ROS)-mediated PI3K/Akt and MAPK signaling pathways. Free Radic Biol Med. 2016 Jan;90:230-42.
[2]. Wang J, et al. Suppressive effects of Momordin Ic on HepG2 cell migration and invasion by regulating MMP-9 and adhesion molecules: Involvement of p38 and JNK pathways. Toxicol In Vitro. 2019 Apr;56:75-83.
Orobol is one of the major soy isoflavones and has various pharmacological activities, including anti-skin-aging and anti-obesity effects. Orobol inhibits CK1ε, VEGFR2, MAP4K5, MNK1, MUSK, TOPK, and TNIK (IC50=1.24-4.45 μM). Orobol also inhibits PI3K isoforms (IC50=3.46-5.27 μM for PI3K α/β/γ/K/δ)[1][2].
体外研究 (In Vitro)
Orobol binds to CK1ε in an ATP-competitive manner and exerts anti-obesity effects by targeting casein kinase 1 epsilon[2]. Orobol (5-20 μM) effectively suppresses MDI (isobutylmethylxanthine, dexamethasone and insulin (MDI))-induced phosphorylation of 4E-BP1[2].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)
Orobol attenuates high fat diet-induced weight gain and lipid accumulation without affecting food intake in C57BL/6J mice[2].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
HFD-induced obesity in C57BL/6J mice[2]
Dosage:
10 mg/kg
Administration:
Intragastrically; daily for 23 weeks
Result:
Significantly reduced body weight by 17.3% compared to the HFD group.
分子量
286.24
Formula
C15H10O6
CAS 号
480-23-9
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]. Kim MH, et al. Lipid Nanoparticles for Enhancing the Physicochemical Stability and Topical Skin Delivery of Orobol. Pharmaceutics. 2020;12(9):845. Published 2020 Sep 3.
AF12198 is a potent, selective and specific peptide antagonist for human type I interleukin-1 receptor (IL1-R1) (IC50=8 nM) but not the human type II receptor (IC50=6.7 µM) or the murine type I receptor (IC50>200 µM). AF12198 inhibits IL-1-induced IL-8 production (IC50=25 nM) and IL-1-induced intercellular adhesion molecule-1 (ICAM-1) expression (IC50=9 nM) in vitro. AF12198 has anti-inflammatory activities and blocks responses to IL-1 in vivo[1].
IC50 Target[1]
IL1R1
8 nM (IC50)
体外研究 (In Vitro)
AF12198 competes for binding of 125I-IL-1α with an IC50 of 8.0 nM, nearly equal to that of IL-1ra, IC50 of 4.0 nM for the type I receptor[1].AF12198 (0-5 ng; 8 hours) inhibits IL-6 induction with an IC50 of 15 μM whereas IL-1ra inhibits with an IC50 of 2 nM in heparinized human primate blood. Meanwhile, With blood from cynomolgus monkeys, the IC50 values are 17 μM for AF12198 and 30 nM for IL-1ra. Additionally, AF12198 or IL-1RA alone does not induce IL-6 in blood from either humans or cynomolgus monkeys[1].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)
AF12198 (intravenous infusion; 16 mg/kg; 30 min before LPS intravenous injection) significantly attenuates the increase in lung MPO activity induced by LPS in acute lung inflammation and it reduces the lung microvascular leakage from rats inflamed with LPS at the 4 h (32.6%), 12 h (50.1%) and 24 h (65.3%) after LPS[2].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
Male Wistar rats[2]
Dosage:
16 mg/kg
Administration:
Intravenous infusion; 30 min before LPS intravenous injection
Result:
Decreased pulmonary microvascular leakage in rats.
[1]. F Aimbire, et al. Low level laser therapy (LLLT) decreases pulmonary microvascular leakage, neutrophil influx and IL-1beta levels in airway and lung from rat subjected to LPS-induced inflammation. Inflammation
[2]. A L Akeson, et al.AF12198, a novel low molecular weight antagonist, selectively binds the human type I interleukin (IL)-1 receptor and blocks in vivo responses to IL-1. J Biol Chem. 1996 Nov 29;271(48):30517-23.
Dehydrobruceine A 是一个低活性的抗锥虫剂，对 Plasmodium falciparum 的 IC50 值为88.5 nM。
Dehydrobruceine A Chemical Structure
CAS No. : 73435-47-9
规格
是否有货
5 mg
询价
10 mg
询价
25 mg
询价
* Please select Quantity before adding items.
生物活性
Dehydrobruceine A is a low potent antitrypanosomal agent, with an IC50 of 88.5 nM for Plasmodium falciparum[1].
分子量
520.53
Formula
C26H32O11
CAS 号
73435-47-9
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]. Saw Bawm, et al. In vitro antitrypanosomal activities of quassinoid compounds from the fruits of a medicinal plant, Brucea javanica. Vet Parasitol. 2008 Dec 20;158(4):288-94.
8-Deoxygartanin, a prenylated xanthones from G. mangostana, is a selective inhibitor of butyrylcholinesterase (BChE)[1]. 8-Deoxygartanin exhibits antiplasmodial activity with an IC50 of 11.8 μM for the W2 strain of Plasmodium falciparum[2]. 8-Deoxygartanin inhibits NF-κB (p65) activation with an IC50 of 11.3 μM[3].
IC50 & Target
p65
11.3 μM (IC50)
分子量
380.43
Formula
C23H24O5
CAS 号
33390-41-9
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moisture and light
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
参考文献
[1]. Khaw KY, et al. Prenylated xanthones from mangosteen as promising cholinesterase inhibitors and their molecular docking studies. Phytomedicine. 2014 Sep 25;21(11):1303-9.
[2]. Ngouamegne ET, et al. Endodesmiadiol, a friedelane triterpenoid, and other antiplasmodial compounds from Endodesmia calophylloides. Chem Pharm Bull (Tokyo). 2008 Mar;56(3):374-7.
[3]. Han AR, et al. Cytotoxic xanthone constituents of the stem bark of Garcinia mangostana (mangosteen). J Nat Prod. 2009 Nov;72(11):2028-31.
