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PKC&ROCK

Ro 31-8220 (138489-18-6)

Ro 31-8220 is a pan-PKC inhibitor with IC50 of 5 nM, 24 nM, 14 nM, 27 nM, an 24 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, and PKC-ε, respectively, and also shows potent inhibition against MAPKAP-K1b, MSK1, GSK3β and S6K1.

Not Intended for Therapeutic Use. For research use only.

CAS: 138489-18-6 Category

Ro 31-8220 (138489-18-6) Description:

Ro 31-8220 is a PKC-inhibitor, which inhibits stimulated fluid pinocytosis of human PMNs induced by the PKC-activators phorbol myristate acetate (PMA, IC50 = 1.35 x 10(-6) M) or diacylglycerols (OAG, diC8) by 95%. Ro-31-8220 showed the apoptotic effect on HL-60 cells, which was mediated by a well-characterized transduction process of apoptotic signals: i.e., mitochondrial cytochrome c efflux and the activation of caspase-3 in the cytosol. Moreover, the ability of Ro-31-8220 to induce apoptotic activation was completely inhibited by the over-expression of the apoptotic suppressor gene, Bcl-2, in the cells. Ro 31-8220 is also a staurosporine (sc-3510) analog, is a cell-permeable inhibitor of PKC (protein kinase C) isoforms PKC α, PKC βI, PKC βII, PKC γ, and PKC ε (IC50 = 5, 24, 14, 27, and 24 nM, respectively). Ro 31-8220 has also been shown to induce apoptosis in various cell lines, independent of its PKC activity, and to inhibit GSK 3 (IC50 = 6.8nM). Ro 31-8220 is an inhibitor of Cdk2, cyclin A, GSK-3β, MSK1, Pim-3, Polycystin-1, PRK2, Rsk-1 and Rsk-2 and an activator of JNK1.

Ro 31-8220 (138489-18-6) Specifications:

Product Name Ro 31-8220
Synonym RO31-8220; RO 31-8220; RO31-8220; RO318220; RO-318220; RO 318220; RO31-8220 mesylate; Bisindolylmaleimide IX; BIM IX.
Chemical Name 3-(3-(4-(1-methyl-1H-indol-3-yl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl)-1H-indol-1-yl)propylcarbamimidothioate methanesulfonate
Drug Class Inhibitor
Purity ≥98% (HPLC)
CAS Number 138489-18-6
Molecular Formula C26H27N5O5S2
Molecular Weight 553.652
Monoisotopic Mass 553.145g/mol
MDL number MFCD03788207
InChIKey SAWVGDJBSPLRRB-UHFFFAOYSA-N
InChi Code InChI=1S/C25H23N5O2S.CH4O3S/c1-29-13-17(15-7-2-4-9-19(15)29)21-22(24(32)28-23(21)31)18-14-30(11-6-12-33-25(26)27)20-10-5-3-8-16(18)20;1-5(2,3)4/h2-5,7-10,13-14H,6,11-12H2,1H3,(H3,26,27)(H,28,31,32);1H3,(H,2,3,4)
SMILES CN1C=C(C2=CC=CC=C21)C3=C(C(=O)NC3=O)C4=CN(C5=CC=CC=C54)CCCSC(=N)N.CS(=O)(=O)O
Form Solid Powder
Color Red
Solubility  Soluble in DMSO (~ 100 mg/ml) or water (~ 5 mg/ml), not in water
Storage Temp.  -20°C
Shelf life >2 years if stored properly
Handling Protect from light and air
Application A PKC-inhibitor

 


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RIDADR NONH for all modes of transport

References:

[1]. Kim SY, Kim S, Kim JM, Jho EH, Park S, Oh D, Yun-Choi HS. PKC inhibitors RO 31-8220 and Gö 6983 enhance epinephrine-induced platelet aggregation in catecholamine hypo-responsive platelets by enhancing Akt phosphorylation. BMB Rep. 2011 Feb;44(2):140-5. doi: 10.5483/BMBRep.2011.44.2.140. PubMed PMID: 21345315.

[2]. Marmy-Conus N, Hannan KM, Pearson RB. Ro 31-6045, the inactive analogue of the protein kinase C inhibitor Ro 31-8220, blocks in vivo activation of p70(s6k)/p85(s6k): implications for the analysis of S6K signalling. FEBS Lett. 2002 May 22;519(1-3):135-40. PubMed PMID: 12023032.

[3].Chepurny OG, Hussain MA, Holz GG. Exendin-4 as a stimulator of rat insulin I gene promoter activity via bZIP/CRE interactions sensitive to serine/threonine protein kinase inhibitor Ro 31-8220. Endocrinology. 2002 Jun;143(6):2303-13. PubMed PMID: 12021195; PubMed Central PMCID: PMC3500996.

[4]. Han Z, Pantazis P, Lange TS, Wyche JH, Hendrickson EA. The staurosporine analog, Ro-31-8220, induces apoptosis independently of its ability to inhibit protein kinase C. Cell Death Differ. 2000 Jun;7(6):521-30. PubMed PMID: 10822275.

[5]. Zhou B, Zhang JP, Hu ZL, Tan YX, Qian DH. Ro 31-8220 inhibits release of interleukin-1 and interleukin-6 from mouse peritoneal macrophages induced by fibrin fibrinogen degradation products. Zhongguo Yao Li Xue Bao. 1999 May;20(5):449-51. PubMed PMID: 10678095.

1 review for Ro 31-8220 (138489-18-6)

  1. Rated 5 out of 5

    Cofttek

    Never had such good experience before,The Ro 31-8220 (138489-18-6) is high purity,also customer service is pretty nice !gotta try!!

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