941575-71-9
941575-71-9 structure
- Name: BIP-135
- Chemical Name: 1H-Pyrrole-2,5-dione, 3-(3-benzofuranyl)-4-(5-bromo-1-methyl-1H-indol-3-yl)
- CAS Number: 941575-71-9
- Molecular Formula: C21H13BrN2O3
- Molecular Weight: 421.24400
- Catalog: Signaling Pathways PI3K/Akt/mTOR GSK-3
- Create Date: 2016-02-22 06:54:04
- Modify Date: 2024-01-09 23:21:33
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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].
| Name | 1H-Pyrrole-2,5-dione, 3-(3-benzofuranyl)-4-(5-bromo-1-methyl-1H-indol-3-yl) |
|---|---|
| Synonyms |
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 |
| 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 | |
| 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 |
| 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 |
| Symbol |
GHS06 |
|---|---|
| Signal Word | Danger |
| Hazard Statements | H301 |
| Precautionary Statements | P301 + P310 |
| Hazard Codes | T+ |
| RIDADR | UN 2811 6.1 / PGIII |