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Merck
CN

203811

苔藓抑素1

≥98% (HPLC), solid,film, protein kinase C activator, Calbiochem®

别名:

苔藓抑素1, Bryo 1,PKC活化剂VII,PKC活化剂VI

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关于此项目

经验公式(希尔记法):
C47H68O17
化学文摘社编号:
分子量:
905.03
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
film, solid
Quality level:
Storage condition:
OK to freeze, protect from light
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产品名称

苔藓抑素1, A macrocyclic lactone with antitumor properties.

Quality Level

description

Merck USA index - 14, 1457

assay

≥98% (HPLC)

form

film, solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

color

white to colorless

solubility

DMSO: 25 mg/mL, ethanol: 25 mg/mL

shipped in

ambient

storage temp.

−20°C

SMILES string

O1[C@@]2([C@H](\C(=C\C(=O)OC)\C[C@H]1CC(OC(=O)C[C@@H](CC3O[C@@](CC4O[C@H](C\C(=C/C(=O)OC)\C4)\C=C\C2(C)C)(C(C(C3)OC(=O)C)(C)C)O)O)[C@H](O)C)OC(=O)\C=C\C=C\CCC)O

InChI

1S/C47H68O17/c1-10-11-12-13-14-15-39(51)62-43-31(22-41(53)58-9)21-34-25-37(28(2)48)61-42(54)24-32(50)23-35-26-38(59-29(3)49)45(6,7)46(55,63-35)27-36-19-30(20-40(52)57-8)18-33(60-36)16-17-44(4,5)47(43,56)64-34/h12-17,20,22,28,32-38,43,48,50,55-56H,10-11,18-19,21,23-27H2,1-9H3/b13-12+,15-14+,17-16+,30-20+,31-22+/t28-,32-,33+,34+,35?,36?,37?,38?,43+,46+,47-/m1/s1

InChI key

MJQUEDHRCUIRLF-BXOMOELISA-N

General description

一种具有抗肿瘤特性的大环内酯。有效激活蛋白激酶C并表现出高结合亲和力(Ki = 1.35 nM)。有效地转移和下调PKC同工酶α,δ和ε。在完整细胞中通过PKC依赖性途径诱导PKD的双相激活。还显示可以激活Jurkat T细胞和rat2细胞中的Ras。
一种具有抗肿瘤特性的大环内酯。有效激活蛋白激酶C并表现出高结合亲和力(Ki = 1.35 nM)。有效地转移蛋白激酶C(PKC)同工酶α,β和ε,并诱导PKCδ的双相,浓度依赖性下调。据报道与佛波酯竞争结合PKC。在完整细胞中以双相,PKC依赖性方式刺激蛋白激酶D(PKD)活性。还激活Jurkat T细胞和rat2细胞中的Ras。

Biochem/physiol Actions

主要靶标
蛋白激酶C
产物不与ATP竞争。
可逆:否
细胞渗透性:否
靶标Ki:1.35 nM,对于蛋白激酶C

Preparation Note

复溶后,等分并冷冻(-20°C)。储备液在-20°C条件下可稳定保存3个月。

Other Notes

Clamp, A., and Jayson, G. 2002.Anticancer Drugs13, 673.
Lorenzo, P.S., et al. 1999.Cancer Res.59, 6137.
Wang, Q.J., et al. 1999.J. Biol. Chem.274, 37233.
Wender, P.A., et al. 1998.Proc.Natl.Acad.Sci. USA95, 6624.
Matthews, S.A., et al. 1997.J. Biol. Chem.272, 20245.
Szallasi, Z., et al. 1994.Mol.Pharmacol.46, 840.
Berkow, R.L., and Kratt, A.S.1985.Biochem.Biophys.Res. Commun.3, 1109.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

毒性:标准处理(A)


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存储类别

11 - Combustible Solids

flash_point_f

Not applicable

flash_point_c

Not applicable



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全球贸易项目编号

货号GTIN
203811-10UG04055977204025