Go 6976

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的选择性蛋白激酶 C (PKC) 抑制剂，选择性抑制 PKCα 和 PKCβ1，IC50 分别为 2.3 和 6.2 nM。

A potent, selective protein kinase C (PKC) inhibitor that selectively inhibits PKCα and PKCβ1 with IC50 of 2.3 and 6.2 nM, respectively; shows no effect on the kinase activity of PKCδ, -ε and -ζ (IC50>3 uM); also inhibits JAK2, FLT3 and mutant FLT3 with significant activity in primary acute myeloid leukaemia cells; inhibits HIV-1 proviral induction from latent/low-level-producing infectious states, inhibits signalling, survival and proliferation in cells expressing the leukaemia-associated TEL-JAK2 fusion protein and the MPD-associated JAK2 V617F mutant.HIV Infection Discontinued.

Go6976 is a potent inhibitor of PKC in vitro (IC50 is 20 nM. This compound is structurally related to staurosporine, which is the most potent PKC inhibitor. UCN-01 is originally identified as a PKC inhibitor. Surprisingly, Go6976 is found to abrogate S and G2 arrest. Dose-response studies reveal that 30 nM Go6976 is sufficient to cause abrogation of S-phase arrest in 6 h and abrogation of G2 arrest followed by lethal mitosis in 24 h. Incubation of cells with 100 nM Go6976 is sufficient to cause complete abrogation of S and G2 arrest at 6 and 24 h, respectively, which is only slightly less potent than in bovine serum. Incubation of cells with UCN-01 or Go6976 alone do not decrease viability compared with control at the concentrations used. Incubation of cells with 5 ng/mL SN38 result in cytostasis, and addition of 50 nM UCN-01 or 100 nM Go6976 to arrested MDA-MB-231 cells cause a dramatic decrease in viable cell number by 96 h.

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Go-6976 | Go6976

Angiogenesis

PKC

PKC

Infection

HIV Infection

136194-77-9

378.43

C24H18N4O

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (132.12 mM)

N#CCCN(C1=C2C(CNC3=O)=C3C4=C1N(C)C5=C4C=CC=C5)C6=C2C=CC=C6

5,6,7,13-Tetrahydro-13-methyl-5-oxo-12H-indolo[2,3-a]pyrrolo[3,4-c]carbazole-12-propanenitrile

(-20℃)

With Ice Pack

≥ 2 years