GO-6976

Category	Influenza Virus
CAS	136194-77-9
Description	Go6976 is a potent PKC inhibitor with IC50 values of 2.3 and 6.2 nM for PKCα and PKCβ1, respectively. It also inhibits TrkA, TrkB, JAK2 and JAK3 tyrosine kinases (IC50 values are 5, 30, 130 and 370 nM respectively).

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Product Information

Synonyms	GO-6976; GO 6976; PD-406976; PD 406976; PD406976
Molecular Weight	378.435
Molecular Formula	C24H18N4O
Canonical SMILES	CN1C2=CC=CC=C2C3=C4C(=C5C6=CC=CC=C6N(C5=C31)CCC#N)CNC4=O
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)
InChIKey	VWVYILCFSYNJHF-UHFFFAOYSA-N
Boiling Point	652.3±55.0 °C at 760 mmHg
Flash Point	348.3±31.5 °C
Purity	>98%
Density	1.4±0.1 g/cm3
Solubility	In Vitro: DMSO : 50 mg/mL(132.12 mM;Need ultrasonic) In Vivo: 1.Add each solvent one by one:10% DMSO >> 90%corn oil Solubility: ≥ 3.25 mg/mL (8.59 mM); Clear solution 2.Add each solvent one by one:10% DMSO >> 40%PEG300 >> 5%Tween-80 >> 45% saline Solubility: 1.39 mg/mL (3.67 mM); Suspended solution; Need ultrasonic 3.Add each solvent one by one:10% DMSO >> 90% (20%SBE-β-CDin saline) Solubility: 1.39 mg/mL (3.67 mM); Suspended solution; Need ultrasonic
Appearance	White Solid
Storage	Powder: -20°C: 3 years 4°C: 2 years In solvent: -80°C: 6 months -20°C: 1 month
Complexity	730
Exact Mass	378.14806121
Index Of Refraction	1.774
In Vitro	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.
PSA	62.75000
Target	PKC; Influenza Virus
Vapor Pressure	0.0±2.0 mmHg at 25°C
XLogP3-AA	3.2