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GNE-495 is a potent and selective MAP4K4 Inhibitor with efficacy in retinal angiogenesis. GNE-495 showed excellent potency and good PK and was used to demonstrate in vivo efficacy in a retinal angiogenesis model recapitulating effects that were observed in the inducible Map4k4 knockout mice. GNE-495 is administered intraperitoneally to neonatal mouse pups at high doses: 25 and 50 mg/kg.
| Molecular Weight | 405.42 |
| Formula | C22H20FN5O2 |
| CAS Number | 1449277-10-4 |
| Solubility (25°C) | DMSO 2 mg/mL (Need ultrasonic) |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related MAPKAPK2/MAP3K/MAP4K Products |
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| Takinib
Takinib is a potent and selective TAK1 inhibitor with an IC50 of 9.5 nM, more than 1.5 log more potent than the second and third ranked targets, IRAK4 (120 nM) and IRAK1 (390 nM), respectively. |
| NG25
NG25 is a potent dual TAK1 and MAP4K2 inhibitor with IC50s of 149 nM and 21.7 nM, respectively. |
| PF-06260933
PF-06260933 is a potent inhibitor of MAP4K4 with an IC50 of 3.7 nM, possessing excellent kinome selectivity. |
| MAP4K4-IN-3
MAP4K4-IN-3 is a potent and selective MAP4K4 inhibitor with an IC50 of 14.9 nM in kinase assay, and an IC50 of 470 nM in cell assay. |
| INS018 055
INS018 055 is a TNIK and MAP4K4 inhibitor with IC50 values of 12-120 nM, respectively. INS018 055 exhibits anti-fibrotic activity across different organs in vivo through oral, inhaled or topical administration. INS018 055 possesses anti-inflammatory effects in addition to its anti-fibrotic profile, validated in multiple in vivo studies. |
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