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145333-02-4

145333-02-4 structure
145333-02-4 structure
  • Name: Bisindolylmaleimide XI hydrochloride
  • Chemical Name: 3-[8-[(dimethylamino)methyl]-6,7,8,9-tetrahydropyrido[1,2-a]indol-3-yl]-4-(1-methylindol-3-yl)pyrrole-2,5-dione,hydrochloride
  • CAS Number: 145333-02-4
  • Molecular Formula: C28H29ClN4O2
  • Molecular Weight: 489.01
  • Catalog: Signaling Pathways Epigenetics PKC
  • Create Date: 2017-06-05 20:56:50
  • Modify Date: 2025-08-21 12:33:10
  • Bisindolylmaleimide XI hydrochloride (Ro 32-0432) is a potent, selective and orally active PKC inhibitor with IC50s of 9 nM, 28 nM, 31 nM, 37 nM, and 108 nM for PKCα, PKCβI, PKCβII, PKCγ, and PKCε, respectively[1][2].

Name 3-[8-[(dimethylamino)methyl]-6,7,8,9-tetrahydropyrido[1,2-a]indol-3-yl]-4-(1-methylindol-3-yl)pyrrole-2,5-dione,hydrochloride
Synonyms 3-{8-[(Dimethylamino)methyl]-6,7,8,9-tetrahydropyrido[1,2-a]indol-3-yl}-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione hydrochloride
3-{8-[(Dimethylamino)methyl]-6,7,8,9-tetrahydropyrido[1,2-a]indol-3-yl}-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione hydrochloride (1:1)
1H-Pyrrole-2,5-dione, 3-[8-[(dimethylamino)methyl]-6,7,8,9-tetrahydropyrido[1,2-a]indol-3-yl]-4-(1-methyl-1H-indol-3-yl)-, hydrochloride (1:1)
Description Bisindolylmaleimide XI hydrochloride (Ro 32-0432) is a potent, selective and orally active PKC inhibitor with IC50s of 9 nM, 28 nM, 31 nM, 37 nM, and 108 nM for PKCα, PKCβI, PKCβII, PKCγ, and PKCε, respectively[1][2].
Related Catalog
Target

PKC-α:9 nM (IC50)

PKC-βI:28 nM (IC50)

PKC-βII:31 nM (IC50)

PKC-γ:37 nM (IC50)

PKC-ε:108 nM (IC50)

In Vitro Bisindolylmaleimide XI hydrochloride (Ro 32-0432) inhibits IL-2 secretion, IL-2 receptor expression in, and proliferation of, peripheral human T-cells stimulated with phorbol ester together with phytohemagglutin or anti-CD3, but does not inhibit IL-2 induced proliferation in cells already stimulated to express IL-2 receptors. Proliferation of the influenza peptide antigen HA 307-319-specific human T-cell clone (HA27) after exposure to antigen-pulsed autologous presenting cells is also inhibited by Bisindolylmaleimide XI hydrochloride[2]. PKC inhibition with Bisindolylmaleimide XI hydrochloride (Ro 32-0432; 1 μM) decreases the proportion of apoptotic cells (-21%) in retinal progenitor cells (RPCs)[3].
In Vivo Oral administration of Bisindolylmaleimide XI hydrochloride inhibits subsequent phorbol ester-induced edema in ratss. Induction of more physiologically T-cell driven responses such as host vs. graft responses and the secondary paw swelling in adjuvant-induced arthritis are also inhibited by Bisindolylmaleimide XI hydrochloride[2].
References

[1]. S E Wilkinson, et al. Isoenzyme specificity of bisindolylmaleimides, selective inhibitors of protein kinase C. Biochem J. 1993 Sep 1;294 ( Pt 2)(Pt 2):335-7.

[2]. A M Birchall, et al. Ro 32-0432, a selective and orally active inhibitor of protein kinase C prevents T-cell activation. J Pharmacol Exp Ther. 1994 Feb;268(2):922-9.

[3]. Roman Kholodenko, et al. Anti-apoptotic effect of retinoic acid on retinal progenitor cells mediated by a protein kinase A-dependent mechanism. Cell Res. 2007 Feb;17(2):151-62.

Molecular Formula C28H29ClN4O2
Molecular Weight 489.01
Exact Mass 488.197906
PSA 59.27000
LogP 4.95500
Personal Protective Equipment Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter
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