Description
Cas:136194-77-9
Product Information:
Go6976 is a Protein Kinase C (PKC) inhibitor, with an IC50 of 20 nM.
Chemical Formula: C24H18N4O
Exact Mass: 378.14806
Molecular Weight: 378.43
Elemental Analysis: C, 76.17; H, 4.79; N, 14.81; O, 4.23
Synonym:
PD406976
Chemical Name: 3-(13-methyl-5-oxo-6,7-dihydro-5H-indolo[2,3-a]pyrrolo[3,4-c]carbazol-12(13H)-yl)propanenitrile
InChi Key:
VWVYILCFSYNJHF-UHFFFAOYSA-N
InChi Code: 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)
Smiles Code:
N#CCCN(C1=C2C(CNC3=O)=C3C4=C1N(C)C5=C4C=CC=C5)C6=C2C=CC=C6
Technical Data:
Appearance: white solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
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.
References:
- Qatsha KA, et al. Gö 6976, a selective inhibitor of protein kinase C, is a potent antagonist of human immunodeficiency virus 1 induction from latent/low-level-producing reservoir cells in vitro. Proc Natl Acad Sci U S A. 1993 May 15;90(10):4674-8.
- Hayamitsu Adachi, et al. Microbial metabolites and derivatives targeted at inflammation and bone diseases therapy: chemistry, biological activity and pharmacology. The Journal of Antibiotics volume 71, pages 60–71 (2018).
Products are for research use only. Not for human use.
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