BIP-135

Names

[ Name ]:
BIP-135

[Synonym ]:
3-(Benzofuran-3-yl)-4-(5-bromo-1-methyl-1H-indol-3-yl)pyrrole-2,5-dione
3-(5-Bromo-1-methyl-1H-indol-3-yl)-4-(benzofuran-3-yl)pyrrole-2,5-dione
BIP 135

Biological Activity

[Description]:

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[1].

[Related Catalog]:

Signaling Pathways >> Stem Cell/Wnt >> GSK-3

Research Areas >> Neurological Disease

Signaling Pathways >> PI3K/Akt/mTOR >> GSK-3

[Target]

IC50: 16 nM (GSK-3α), 21 nM (GSK-3β)[1]

[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[1]. BIP-135 (20 μM; 48 hours) is a superior neuroprotective agent in the model of oxidative stress[1]. Western Blot Analysis[1] Cell Line: Human SMA fibroblasts Concentration: 20 μM, 25 μM, 30 μM Incubation Time: 72 hours Result: Led to a 7-fold increase in SMN levels at 25 μM.

[In Vivo]

BIP-135 does not appear to be toxic and was well-tolerated by the animals (no decrease in body weight)[1]. 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[1]. Animal Model: Male and female SMN2+/+, SMN2Δ7+/+, Smn+/– mice[1] Dosage: 75 mg/kg Administration: Intraperitoneal injection; daily; from postnatal day 0 to 21 Result: Caused a modest extension in the median survival of SMA KO animals by two days.

[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.

Chemical & Physical Properties

[ Density]:
1.64±0.1 g/cm3 (20 °C, 760 mmHg)

[ Boiling Point ]:
643.5±55.0 °C (760 mmHg)

[ Molecular Formula ]:
C₂₁H₁₃BrN₂O₃

[ Molecular Weight ]:
421.24400

[ Exact Mass ]:
420.01100

[ PSA ]:
64.24000

[ LogP ]:
4.58300

[ Storage condition ]:
-20°C

Safety Information

[ Symbol ]:

GHS06

[ Signal Word ]:
Danger

[ Hazard Statements ]:
H301

[ Precautionary Statements ]:
P301 + P310

[ Hazard Codes ]:
T+

[ RIDADR ]:
UN 2811 6.1 / PGIII

Related Compounds

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