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Drug intelligence / Profile preview
3-(1H-indol-3-yl)-4-{1-[2-(1-methylpyrrolidin-2-yl)ethyl]-1H-indol-3-yl}-1H-pyrrole-2,5-dione
- Development stage
- Unknown
- Modality
- Small Molecules
01
Overview
This compound is a synthetic small molecule belonging to the bisindolylmaleimide class. It features two indole moieties and a maleimide core with an N-methylpyrrolidine substituent. The molecule is primarily known as bisindolylmaleimide II (BIM 2), an experimental inhibitor of protein kinases, especially protein kinase C (PKC) and cAMP-dependent protein kinase catalytic subunit alpha (PKA). It has been used in biochemical research to study kinase signaling pathways but has not advanced into clinical development or approval for therapeutic use. Its mechanism involves competitive inhibition at the ATP-binding site of target kinases[6][1].
- Other names
- 3-(1H-Indol-3-yl)-4-(1-{2-[(2S)-1-methylpyrrolidin-2-yl]ethyl}-1H-indol-3-yl)-1H-pyrrole-2,5-dioneBIM 2BIM2BIM-2bisindolylmaleimide IICAS RN 137592–45–1
02
Targets
PRKCA (Protein kinase C alpha)PRKCD (Protein kinase C delta)PRKCZ (Protein kinase C zeta)AKT1 (Proto-oncogene serine/threonine-protein kinase Akt1)AKT2 (Rac-beta serine/threonine-protein kinase)AKT3 (RAC-gamma serine/threonine-protein kinase)RPS6KB1 (Ribosomal protein S6 kinase beta-1)PAK1 (p21-activated kinase 1)PKN2 (Protein kinase N2)SGK1SGK2 (Serum/glucocorticoid regulated kinase 2)SGK3 (Serum/glucocorticoid regulated kinase family member 3)TSSK3 (Testis-specific serine/threonine-protein kinase 3)PKA (Cyclic amp-dependent protein kinase)PAK (p21-activated kinase family)PKC (Protein kinase C family)
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