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G-6203 Gö 6976, >99%

[PD 406976] [Go 6976] [Gö6976] [Go6976] [Gö-6976] [Go-6976]

M.W. 378.43

C24H18N4O

[136194-77-9]

Storage:  Store at or below -20 ºC.  Solubility:  Soluble in DMSO at 25 mg/mL; very poorly soluble in ethanol; very poorly soluble in water; maximum solubility in plain water is estimated to be about 1-5 µM; buffers, serum, or other additives may increase or decrease the aqueous solubility.  Appearance:  Off-white to yellow solid.  Disposal:  A

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• Novel, very potent PKC inhibitor with high selectivity for the A-group of PKC isotypes (α, β, and γ), with IC50 values in the 2-10 nM range.  Little or no inhibition of the B- and C-groups of PKC isotypes, even at much higher concentrations.  Kleinschroth, J., Hartenstein, J., Rudolph, C. and Schächtele, C.  "Non-glycosidic/non-aminoalkyl-substituted indolocarbazoles as inhibitors of protein kinase C."   Bioorg. Med. Chem. Lett. 3:  1959-1964 (1993).  Martiny-Baron, G., Kazanietz, M.G., Mischak, H., Blumberg, P., Kochs, G., Hug, H., Marme, D. and Schächtele, C.  "Selective inhibition of protein kinase C isozymes by the indolocarbazole Gö 6976."  J. Biol. Chem. 268:  9194-9197 (1993).

• Our Gö 6976 product contains less than 0.5% of the "wrong" isomer (in which the methyl and cyanoethyl groups are reversed).

• IMPORTANT:  we have recently found that Gö 6976 from several other vendors contains as much as 10% of the wrong isomer.  This is a serious problem because the incorrect isomer may inhibit kinases that Gö 6976 does not inhibit, thus leading to incorrect interpretations regarding the role of PKCα, β, and γ in cells or tissues being tested.  We are working to define the scope of this problem and to determine the kinase inhibitory profile of the wrong isomer.  (This entry last updated May 7, 2007).

• Please request Technical Note #2 for additional information about the nomenclature of PKC isotypes.

• This product is offered for R&D use in accordance with (i) 35 USC 271(e)+A13(1) in the U.S.; (ii) Section 69.1 of Japanese Patent Law in Japan; (iii) Section 11, No. 2 of the German Patent Act of 1981 in Germany; (iv) Section 60, Paragraph 5b of the U.K. Patents Act of 1977 in the U.K.; (v) Sections 55.2(1) and 55.2(6) and other common law exemptions of Canadian patent law; (vi) Section 68B of the Patents Act of 1953 in New Zealand together with the amendment of same by the Statutes Amendment Bill of 2002; (vii) such related legislation and/or case law as may be or become applicable in the aforementioned countries; and (viii) such similar laws and rules as may apply in various other countries.

• Sold for laboratory or manufacturing purposes only; not for human, medical, veterinary, food, or household use.