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
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询价
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250 mg
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500 mg
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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.