[CAS NO. 136194-77-9] Go6976

Name: Go6976
Brand: Arctom Scientific
SKU: SLK-S7119

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PRODUCTS SPECIFICATIONS [136194-77-9]

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Catalog

SLK-S7119

Brand

Selleck

CAS

136194-77-9

DESCRIPTION [136194-77-9]

Overview

MDL	MFCD00236434
Molecular Weight	377.42
Molecular Formula	C24H18N4O
SMILES	C(CC#N)N1C=2C(=C3C(=C4C2N(C)C=5C4=CC=CC5)C(=O)NC3)C=6C1=CC=CC6

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.6496 mL	13.2478 mL	26.4957 mL
5 mM	0.5299 mL	2.6496 mL	5.2991 mL
10 mM	0.2650 mL	1.3248 mL	2.6496 mL
50 mM	-	-	-

Description

Go6976 (PD406976) is a potent inhibitor with of 7.9 nM, 2.3 nM, and 6.2 nM for PKC (Rat brain), PKCα, and PKCβ1, respectively. Also a potent inhibitor of and .

Targets

JAK2 ^[2] (Cell-free assay)	FLT3 ^[2] (Cell-free assay)	PKCα ^[1] (Cell-free assay)	PKCβ1 ^[1] (Cell-free assay)	PKC ^[1] (Rat brain)
		2.3 nM	6.2 nM	7.9 nM

In vitro

Go6976 have no effect on the kinase activity of the Ca(2+)-independent PKC subtypes delta, epsilon, and zeta. 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. Go 6976 potently inhibits HIV-1 induction by Bryostatin 1, tumor necrosis factor alpha, and interleukin 6.

In vivo

Go6976 (2.5 mg/kg i.p.), as a PKD inhibitor, effectively prevents LPS/D: -GalN-induced acute liver injury by inhibition of MAPKs activation to reduce TNF-α production, and significantly improves the survival of LPS/D-GalN-challenged mice.

References

[1] Martiny-Baron G, er al. J Biol Chem. 1993, 268(13), 9194-9197.
[2] Grandage VL, et al. Br J Haematol. 2006, 135(3), 303-316.
[3] Qatsha KA, et al. Proc Natl Acad Sci U S A. 1993, 90(10), 4674-4678.
[4] Duan GJ, et al. Inflamm Res. 2011, 60(4), 357-366.

Synonyms

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

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

Go 6976

Goe 6976

12-(2-Cyanoethyl)-6,7,12,13-tetrahydro-13-methyl-5-oxo-5H-indolo[2,3-a]pyrrolo[3,4-c]carbazole