Go6976 is a potent PKC inhibitor with IC50 of 7.9 nM, 2.3 nM, and 6.2 nM for PKC (Rat brain), PKC, and PKC1, respectively. Also a potent inhibitor of JAK2 and Flt3.Go6976 have no effect on the kinase activity of the Ca(2+)-independent PKC subtypes delta, epsilon, and zeta. [1] Beside WT JAK2, Go6976 also inhibits the mutant forms (JAK2 V617F and TEL-JAK2) found in haematological malignancies, and has activity against mutant forms of FLT3. In AML cells, Go6976 reduces the survival to 55% of control in FLT3-ITD cases and to 69% in FLT3-WT samples.[2] Go 6976 potently inhibits HIV-1 induction by Bryostatin 1, tumor necrosis factor alpha, and interleukin 6.
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化学信息
名称 | Go6976 |
Iupac 化学名称 | 3-(13-methyl-5-oxo-6,7-dihydro-5H-indolo[2,3-a]pyrrolo[3,4-c]carbazol-12(13H)-yl)propanenitrile |
同义词 | GO6976; GO-6976; GO 6976; PD406976; PD 406976; PD-406976. |
英文同义词 | GO6976; GO-6976; GO 6976; PD406976; PD 406976; PD-406976. |
分子式 | C24H18N4O |
分子量 | 377.42 |
Smile | CN1C=2C=CC=CC2C2=C1C=1N(C3=CC=CC=C3C1C1=C2C(NC1)=O)CCC#N |
InChiKey | VWVYILCFSYNJHF-UHFFFAOYSA-N |
InChi | InChI=1S/C24H18N4O/c1-27-17-9-4-2-7-14(17)20-21-16(13-26-24(21)29)19-15-8-3-5-10-18(15)28(12-6-11-25)23(19)22(20)27/h2-5,7-10H,6,12-13H2,1H3,(H,26,29) |
Cas号 | 136194-77-9 |
相关CAS号 | |
外观性状 | crystalline solid |
纯度 | 98% |
存储 | 3 years -20ºCpowder |
可溶性 | Soluble in DMSO |
处理方式 | |
运输条件 | Shipped under ambient temperature as non-hazardous chemical. |
海关编码 | |
Targets | |
Mechanism | |
Cell study | |
Animal study | |
Clinical study | |