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AB143783

Bisindolylmaleimide XI hydrochloride, PKC inhibitor

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MW 489 Da, Purity >98%. Selective, cell-​permeable protein kinase C (PKC) inhibitor that displays 10-​fold greater selectivity for PKCα (IC50 = 9 nM) and 4-​fold greater selectivity for PKCβI (IC50 = 28 nM) over Ca2+-​independent PKCε (IC50 = 108 nM). Enhances cardiac contractility and protection from heart failure. Prevents T-​cell activation and proliferation (IC50s ranging from 30-​150 nM) associated with chronic inflammatory responses in vivo. Also inhibits GRK2, GRK5, and GRK6 (IC50 values are 29, 3.6, and 16 μM, respectively).

View Alternative Names

CVID9, D14Ertd420e, KPCA_HUMAN, KPCD_HUMAN, KPCE_HUMAN, KPCL_HUMAN, Kinase PKC delta, May-01, MGC 5363, MGC125656, MGC125657, MGC26269, MGC49908, PCKd, PKC 2, PKC ZETA, PKC d, PKC delta, PKC epsilon, PKC h, PKC-A, PKC-B, PKC-L, PKC-alpha, PKC-beta, PKC-gamma, PKCE, PKCG, PRKC D, PRKC delta, PRKCA, PRKCB, PRKCB1, PRKCB2, PRKCE, PRKCG, PRKCL, PRKCZ, Pkcea, Prkch, Protein Kinase C alpha, Protein Kinase C delta, Protein kinase C, Protein kinase C alpha type, Protein kinase C beta, Protein kinase C delta VIII, Protein kinase C delta type, Protein kinase C epsilon, Protein kinase C epsilon type, Protein kinase C eta, Protein kinase C eta type, Protein kinase C gamma, Protein kinase C zeta, Tyrosine protein kinase PRKCD, nPKC-delta, nPKC-epsilon, nPKC-eta

1 Images
Chemical Structure - Bisindolylmaleimide XI hydrochloride, PKC inhibitor (AB143783)
  • Chemical Structure

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Chemical Structure - Bisindolylmaleimide XI hydrochloride, PKC inhibitor (AB143783)

2D chemical structure image of ab143783, Bisindolylmaleimide XI hydrochloride, PKC inhibitor

Key facts

CAS number

151342-35-7

Purity

>98%

Form

Solid

form

Molecular weight

489 Da

Molecular formula

C<sub>2</sub><sub>8</sub>H<sub>2</sub><sub>9</sub>ClN<sub>4</sub>O<sub>2</sub>

PubChem

11605551

Nature

Synthetic

Solubility

Soluble in DMSO to 10 mM (with warming)

Biochemical name

Bisindolylmaleimide XI, HCl

Biological description

Selective, cell-​permeable protein kinase C (PKC) inhibitor that displays 10-​fold greater selectivity for PKCα (IC50 = 9 nM) and 4-​fold greater selectivity for PKCβI (IC50 = 28 nM) over Ca2+-​independent PKCε (IC50 = 108 nM). Enhances cardiac contractility and protection from heart failure. Prevents T-​cell activation and proliferation (IC50s ranging from 30-​150 nM) associated with chronic inflammatory responses in vivo. Also inhibits GRK2, GRK5, and GRK6 (IC50 values are 29, 3.6, and 16 μM, respectively).

Canonical smiles

CN1C=C(C2=CC=CC=C21)C3=C(C(=O)NC3=O)C4=C5CC(CCN5C6=CC=CC=C64)CN(C)C.Cl

InChi

InChI=1S/C28H28N4O2.ClH/c1-30(2)15-17-12-13-32-22-11-7-5-9-19(22)24(23(32)14-17)26-25(27(33)29-28(26)34)20-16-31(3)21-10-6-4-8-18(20)21;/h4-11,16-17H,12-15H2,1-3H3,(H,29,33,34);1H

InChiKey

HSPRASOZRZDELU-UHFFFAOYSA-N

IUPAC Name

3-[8-[(dimethylamino)methyl]-6,7,8,9-tetrahydropyrido[1,2-a]indol-10-yl]-4-(1-methylindol-3-yl)pyrrole-2,5-dione;hydrochloride

Properties and storage information

Shipped at conditions
Ambient - Can Ship with Ice
Appropriate short-term storage conditions
-20°C
Appropriate long-term storage conditions
-20°C
Storage information
Store under desiccating conditions

Supplementary information

This supplementary information is collated from multiple sources and compiled automatically.

Protein Kinase C (PKC) is a family of serine/threonine kinases important in cellular signaling. PKC isoforms including PKC delta PKC epsilon and PKC eta have distinct molecular weights and expression patterns. PKC delta also known as PRKCD has a mass of approximately 78 kDa and is expressed in many tissues such as the heart lungs and brain. PKC epsilon has a mass close to 83 kDa and is found in skeletal muscle and epithelial tissues. PKC eta weighs around 80 kDa and is expressed in skin and keratinocytes. These isoforms play an active role in modulating various cellular responses.
Biological function summary

PKC isoforms regulate a range of functions like cell proliferation differentiation and apoptosis. They often act as part of larger protein complexes modulating cellular responses to extracellular signals. PKC delta has a role in the control of cell cycle and apoptosis while PKC epsilon is involved in cell survival pathways. PKC eta contributes to keratinocyte differentiation and skin integrity. Collectively they influence cellular functions by phosphorylating target proteins on serine and threonine residues.

Pathways

PKC isoforms integrate into major signaling pathways like MAPK/ERK and PI3K/Akt. PKC delta participates in the MAPK/ERK pathway interacting with Ras and Raf proteins to modulate cell survival and differentiation. PKC epsilon interacts with proteins in the PI3K/Akt pathway influencing cell survival and metabolism. These pathways place PKC isoforms in pivotal roles for processing various external signals allowing cells to adapt dynamically to their environments.

Multiple PKC isoforms link to pathological conditions such as cancer and cardiovascular diseases. PKC delta is associated with the progression of some cancers by its influence on cell proliferation and apoptosis. Its activity can impact proteins like Bcl-2 involved in apoptotic pathways. PKC epsilon has connections to cardiovascular disorders through its regulatory effects on cardiac muscle cells where it interfaces with proteins such as troponin in contractility pathways. Understanding these links can help develop therapeutic approaches targeting PKC isoforms.

Product protocols

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