Ro-31-8220

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首页克隆与表达Millipore 密理博>

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货号：557520-500UG

品牌：Millipore 密理博

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北京朝阳

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EA (预计3-5工作日到货)

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Replacement Information

重要规格表

Empirical Formula	CAS #
C₂₅H₂₃N₅O₂S · CH₄O₃S	138489-18-6

Description
Overview	A cell-permeable, reversible, competitive, and selective inhibitor of protein kinase C (PKC; IC₅₀ = 10 nM) over CaM kinase II (IC₅₀ = 17 µM) and protein kinase A (IC₅₀ = 900 nM). Potently inhibits GSK-3 in primary adipocytes (IC₅₀ = 6.8 nM) and in GSK-3β immunoprecipitates (IC₅₀ = 2.8 nM). An inhibitor of MAP kinase phosphatase-1 expression and an activator of JNK1. Inhibits the phosphorylation of Raf-1 and induces apoptosis, independent of its effects on PKC, in HL-60 cells. Also inhibits sirtuin in a NAD-competitive manner (IC₅₀ = 3.5 µM and 0.8 µM for SIRT1 and SIRT2, respectively), and induces hyperacetylation of tubulin in A549 cells. A 5 mM (500 µg/181 µl) solution of Ro-31-8220 (Cat. No. 557521) in H₂O is also available.
Catalogue Number	557520
Brand Family	Calbiochem®
Synonyms	3-[1-[3-(Amidinothio)propyl-1H-indol-3-yl]-3-(1-methyl-1H-indol-3-yl)maleimide, Bisindolylmaleimide IX, Methanesulfonate

References
References	Trapp, J., et al. 2006. J. Med. Chem. In press. Powell, D.J., et al. 2003. Mol. Cell Biol. 23, 7794. Han, Z., et al. 2000. Cell Death Differ. 7, 521. Hers, I., et al. 1999. FEBS Lett. 460, 433. Beltman, J., et al. 1996. J. Biol. Chem. 271, 27018. Keller, H.U., and Niggli, V. 1993. Biochem. Biophys. Res. Commun. 194, 1111. McKenna, J.P., and Hanson, P.J. 1993. Biochem. Pharmacol. 46, 583. Davis, P.D., et al. 1992. J. Med. Chem. 35, 994.

References

Trapp, J., et al. 2006. J. Med. Chem. In press.
Powell, D.J., et al. 2003. Mol. Cell Biol. 23, 7794.
Han, Z., et al. 2000. Cell Death Differ. 7, 521.
Hers, I., et al. 1999. FEBS Lett. 460, 433.
Beltman, J., et al. 1996. J. Biol. Chem. 271, 27018.
Keller, H.U., and Niggli, V. 1993. Biochem. Biophys. Res. Commun. 194, 1111.
McKenna, J.P., and Hanson, P.J. 1993. Biochem. Pharmacol. 46, 583.
Davis, P.D., et al. 1992. J. Med. Chem. 35, 994.

Product Information
CAS number	138489-18-6
ATP Competitive	Y
Form	Red solid
Hill Formula	C₂₅H₂₃N₅O₂S · CH₄O₃S
Chemical formula	C₂₅H₂₃N₅O₂S · CH₄O₃S
Hygroscopic	Hygroscopic
Reversible	Y
Structure formula Image

Applications

Biological Information
Primary Target	PKC
Primary Target IC<sub>50</sub>	10 nM, 17 µM, 900 nM against PKC, CaM kinase II, and protein kinase A, respectively; 6.8 nM against GSK-3 in primary adipocytes; 2.8 nM against GSK-3β immunoprecipitates)
Purity	≥95% by HPLC

Physicochemical Information
Cell permeable	Y

Dimensions

Materials Information

Toxicological Information

Safety Information according to GHS

Safety Information

Product Usage Statements

Storage and Shipping Information
Ship Code	Ambient Temperature Only
Toxicity	Standard Handling
Storage	+2°C to +8°C
Protect from Light	Protect from light
Hygroscopic	Hygroscopic
Do not freeze	Ok to freeze
Special Instructions	Following reconstitution, aliquot and freeze (-20°C). DMSO stock solutions are stable for up to 4 months at -20°C.