257879-35-9

257879-35-9 structure

Name: PKCβ inhibitor 1
Chemical Name: 3-anilino-4-[1-(3-imidazol-1-ylpropyl)indol-3-yl]pyrrole-2,5-dione
CAS Number: 257879-35-9
Molecular Formula: C₂₄H₂₁N₅O₂
Molecular Weight: 411.45600
Catalog: Signaling Pathways Apoptosis Apoptosis
Create Date: 2018-12-17 14:24:38
Modify Date: 2024-01-10 12:15:16
PKCβ inhibitor 1 is a potent, ATP-competitive, and selective PKCβ inhibitor with IC50s of 21 and 5 nM for human PKCβ1 and PKCβ2, respectively. PKCβ inhibitor 1 exhibits selectivity of more than 60-fold in favor of PKCβ2 relative to other PKC isozymes (PKCα, PKCγ, and PKCε)[1][2].

Name	3-anilino-4-[1-(3-imidazol-1-ylpropyl)indol-3-yl]pyrrole-2,5-dione
Synonyms	IN1136 HMS3229K09 PKCbeta Inhibitor

Description	PKCβ inhibitor 1 is a potent, ATP-competitive, and selective PKCβ inhibitor with IC50s of 21 and 5 nM for human PKCβ1 and PKCβ2, respectively. PKCβ inhibitor 1 exhibits selectivity of more than 60-fold in favor of PKCβ2 relative to other PKC isozymes (PKCα, PKCγ, and PKCε)[1][2].
Related Catalog	Signaling Pathways >> Epigenetics >> PKC Signaling Pathways >> Apoptosis >> Apoptosis Research Areas >> Cancer Signaling Pathways >> TGF-beta/Smad >> PKC
Target	human PKCβ1:21 nM (IC50) human PKCβ2:5 nM (IC50) PKCα:331 nM (IC50)
In Vitro	PKCβ inhibitor 1 (0-30 μM; 48 hours) suppresses tumor cell proliferation in a time- and dose-dependent manner[2]. PKCβ inhibitor 1 (14 μM; 2-48 hours) induces apoptosis in 2F7 cells[2]. PKCβ inhibitor 1 (15 μM; 2-48 hours) inhibits cell cycle progression in 2F7 and BCBL-1 cells[2]. PKCβ (15 or 14 μM, respectively; 2-48 hours) inhibitor 1 reduces the expression of phospho-PKCβ in BCBL-1 and 2F7 cells[2]. PKCβ inhibitor 1(0-48 hours) suppresses GSK3β, mTOR, and S6 phosphorylation[2]. Cell Proliferation Assay[2] Cell Line: 2F7, BCBL-1 cells Concentration: 0, 5, 10, 20, and 30 μM Incubation Time: 48 hours Result: A dose-dependent reduction in viability of the 2F7 and BCBL-1 cells starting at 5 μM and increasing with elevated inhibitor concentration. Apoptosis Analysis[2] Cell Line: 2F7 cells Concentration: 14 μM Incubation Time: 2-48 hours Result: Apoptotic induction in 2.1% of the 2F7 cells above background after 2 hours of treatment, increasing through 48 hours of treatment. Cell Cycle Analysis[2] Cell Line: BCBL-1 Cells Concentration: 15 μM (the IC50) Incubation Time: 2-48 hours Result: Inhibits cell cycle progression in 2F7 and BCBL-1 cells. Western Blot Analysis[2] Cell Line: BCBL-1 and 2F7 cell lines Concentration: 15 or 14 μM (at the IC50 respectively) Incubation Time: 2-48 hours Result: The expression of phospho-PKCβ in BCBL-1 and 2F7 cells reduced.
References	[1]. Tanaka M, et al. Synthesis of anilino-monoindolylmaleimides as potent and selective PKCbeta inhibitors. Bioorg Med Chem Lett. 2004 Oct 18;14(20):5171-4. [2]. Saba NS, et al. Protein kinase C-beta inhibition induces apoptosis and inhibits cell cycle progression in acquired immunodeficiency syndrome-related non-hodgkin lymphoma cells. J Investig Med. 2012 Jan;60(1):29-38.

Molecular Formula	C₂₄H₂₁N₅O₂
Molecular Weight	411.45600
Exact Mass	411.17000
PSA	84.44000
LogP	3.75660

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