A-1211212

Inhibitor of BCL2

Structure

SERP Rating

Probe A-1211212 is in the process of SERP review.

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Information

BCL2

Inhibitor

up to 5 uM

Additional Data

SGC image SGC Chemical Probe Collection

Probe Availability:

In Vitro Validations

Uniprot ID: P10415

Target Class: Enzyme

Target SubClass: Apoptosis Regulator

Potency: IC50

Potency Value: 1.4 nM

Potency Assay: Time-resolved fluorescence energy transfer (TR-FRET)

PDB ID for probe-target interaction (3D structure): --

Target aliases:

Apoptosis regulator Bcl-2, BCL2, BCL2_HUMAN

DOI Reference: 10.1126/scitranslmed.aaa4642

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

Selectivity within target family: BCL2L1: IC50 = 753 nM (TR-FRET); MCL1: IC50 = 2050 nM (TR-FRET). Selectivity outside target family: Closest off target for the probe at 10 µM is the CACNA1S (Ca2+ channel (L, dihydropyridine site)) with 63.2 % inhibition (Eurofins-Cerep screen). One off-target in GPCR scan: TMEM97 (Ki = 1491.08 nM)

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