BIP-135

BIP-135 is a potent and selective ATP-competitive GSK-3 inhibitor, with IC50s of 16 nM and 21 nM for GSK-3α and GSK-3β, respectively. BIP 135 exhibits neuroprotective effect.

Product information

CAS Number: 941575-71-9

Molecular Weight: 421.24

Formula: C21H13BrN2O3

Chemical Name: 3-(1-benzofuran-3-yl)-4-(5-bromo-1-methyl-1H-indol-3-yl)-2, 5-dihydro-1H-pyrrole-2, 5-dione

Smiles: CN1C=C(C2=C(C3=COC4=CC=CC=C34)C(=O)NC2=O)C2=CC(Br)=CC=C12

InChiKey: QKQJCKAXFJBYKJ-UHFFFAOYSA-N

InChi: InChI=1S/C21H13BrN2O3/c1-24-9-14(13-8-11(22)6-7-16(13)24)18-19(21(26)23-20(18)25)15-10-27-17-5-3-2-4-12(15)17/h2-10H,1H3,(H,23,25,26)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

BIP-135 (20-30 μM; 72 hours) increases the survival motor neuron (SMN) protein levels at a dose of 25 μM in human SMA fibroblasts. And the typical bell-shaped dose-response curve is observed due to some toxicity at higher concentrations. BIP-135 (20 μM; 48 hours) is a superior neuroprotective agent in the model of oxidative stress.

In Vivo:

BIP-135 does not appear to be toxic and was well-tolerated by the animals (no decrease in body weight). BIP-135 (75 mg/kg; i.p.; daily; from postnatal day 0 to 21) prolongs the median survival time of Δ7 SMA KO mouse model of spinal muscular atrophy.

References:

1. Chen PC, et al. Identification of a Maleimide-Based Glycogen Synthase Kinase-3 (GSK-3) Inhibitor, BIP-135, that Prolongs the Median Survival Time of Δ7 SMA KO Mouse Model of Spinal Muscular Atrophy. ACS Chem Neurosci. 2012 Jan 18;3(1):5-11.

Products are for research use only. Not for human use.