WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 406713
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.
MedKoo Cat#: 406713
Name: RO31-8220 mesylate
Chemical Formula: C26H27N5O5S2
Molecular Weight: 553.652
Elemental Analysis: C, 56.40; H, 4.92; N, 12.65; O, 14.45; S, 11.58
RO31-8220 meyslate, purity > 98%, is in stock. The same day shipping after order is received.
Related CAS #: 138489-18-6 (mesylate) 125314-64-9 (free base)
Synonym: RO31-8220; RO 31-8220; RO31-8220; RO318220; RO-318220; RO 318220; RO31-8220 mesylate; Bisindolylmaleimide IX; BIM IX.
IUPAC/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)propyl carbamimidothioate methanesulfonate
InChi Key: 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 Code: NC(SCCCN1C=C(C2=C(C3=CN(C)C4=C3C=CC=C4)C(NC2=O)=O)C5=C1C=CC=C5)=N.CS(=O)(O)=O
The following data is based on the product molecular weight 553.652 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.15 mL||5.76 mL||11.51 mL|
|5 mM||0.23 mL||1.15 mL||2.3 mL|
|10 mM||0.12 mL||0.58 mL||1.15 mL|
|50 mM||0.02 mL||0.12 mL||0.23 mL|
1: Kim SY, Kim S, Kim JM, Jho EH, Park S, Oh D, Yun-Choi HS. PKC inhibitors RO 31-8220 and GÃ¶ 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.
6: Lingameneni R, Vysotskaya TN, Duch DS, Hemmings HC Jr. Inhibition of voltage-dependent sodium channels by Ro 31-8220, a 'specific' protein kinase C inhibitor. FEBS Lett. 2000 May 12;473(2):265-8. PubMed PMID: 10812087.
7: Kuz'mina TI, Denisenko VIu, Shapiev ISh. [Effect of the protein kinase C inhibitor Ro 31-8220 on Ca2+-responses, induced by somatotropin, in swine granulosa cells]. Tsitologiia. 1999;41(11):992-6. Russian. PubMed PMID: 10643054.
8: Hers I, TavarÃ© JM, Denton RM. The protein kinase C inhibitors bisindolylmaleimide I (GF 109203x) and IX (Ro 31-8220) are potent inhibitors of glycogen synthase kinase-3 activity. FEBS Lett. 1999 Nov 5;460(3):433-6. PubMed PMID: 10556511.
9: Zhou B, Zhang JP, Hu ZL, Tao XB, Qian DH. Effects of Ro 31-8220 on smooth muscle cell proliferation induced by fibrinogen degradation products. Zhongguo Yao Li Xue Bao. 1997 Sep;18(5):463-5. PubMed PMID: 10322943.
10: Standaert ML, Bandyopadhyay G, Antwi EK, Farese RV. RO 31-8220 activates c-Jun N-terminal kinase and glycogen synthase in rat adipocytes and L6 myotubes. Comparison to actions of insulin. Endocrinology. 1999 May;140(5):2145-51. PubMed PMID: 10218965.
11: Begemann M, Kashimawo SA, Lunn RM, Delohery T, Choi YJ, Kim S, Heitjan DF, Santella RM, Schiff PB, Bruce JN, Weinstein IB. Growth inhibition induced by Ro 31-8220 and calphostin C in human glioblastoma cell lines is associated with apoptosis and inhibition of CDC2 kinase. Anticancer Res. 1998 Sep-Oct;18(5A):3139-52. PubMed PMID: 9858877.
12: Barrett P, Davidson G, Hazlerigg DG, Morris MA, Ross AW, Morgan PJ. Mel 1a melatonin receptor expression is regulated by protein kinase C and an additional pathway addressed by the protein kinase C inhibitor Ro 31-8220 in ovine pars tuberalis cells. Endocrinology. 1998 Jan;139(1):163-71. PubMed PMID: 9421411.
13: Mahon TM, Matthews JS, O'Neill LA. Staurosporine, but not Ro 31-8220, induces interleukin 2 production and synergizes with interleukin 1alpha in EL4 thymoma cells. Biochem J. 1997 Jul 1;325 ( Pt 1):39-45. PubMed PMID: 9224627; PubMed Central PMCID: PMC1218526.
14: Yeo EJ, Provost JJ, Exton JH. Dissociation of tyrosine phosphorylation and activation of phosphoinositide phospholipase C induced by the protein kinase C inhibitor Ro-31-8220 in Swiss 3T3 cells treated with platelet-derived growth factor. Biochim Biophys Acta. 1997 May 27;1356(3):308-20. PubMed PMID: 9194574.
15: Lin W, Zhang JP, Hu ZL, Feng ZH, Qian DH. Effects of Ro 31-8220 on lipopolysaccharides-induced hepatotoxicity and release of tumor necrosis factor from rat Kupffer cells. Zhongguo Yao Li Xue Bao. 1997 Jan;18(1):85-7. PubMed PMID: 10072903.
16: Heiskanen KM, Savolainen KM. Palmitic acid anilide-induced respiratory burst in human polymorphonuclear leukocytes is inhibited by a protein kinase C inhibitor, Ro 31-8220. Free Radic Biol Med. 1997;22(7):1175-82. PubMed PMID: 9098091.
17: Beltman J, McCormick F, Cook SJ. The selective protein kinase C inhibitor, Ro-31-8220, inhibits mitogen-activated protein kinase phosphatase-1 (MKP-1) expression, induces c-Jun expression, and activates Jun N-terminal kinase. J Biol Chem. 1996 Oct 25;271(43):27018-24. PubMed PMID: 8900190.
18: Harris TE, Persaud SJ, Jones PM. Atypical isoforms of pKc and insulin secretion from pancreatic beta-cells: evidence using GÃ¶ 6976 and Ro 31-8220 as Pkc inhibitors. Biochem Biophys Res Commun. 1996 Oct 23;227(3):672-6. PubMed PMID: 8885992.
19: Marley PD, Thomson KA. Inhibition of nicotinic responses of bovine adrenal chromaffin cells by the protein kinase C inhibitor, Ro 31-8220. Br J Pharmacol. 1996 Sep;119(2):416-22. PubMed PMID: 8886429; PubMed Central PMCID: PMC1915873.
20: Geiselhart L, Conti DJ, Freed BM. RO 31-8220, a novel protein kinase C inhibitor, inhibits early and late T cell activation events. Transplantation. 1996 Jun 15;61(11):1637-42. PubMed PMID: 8669110.
125314-64-9 (free base).