PAK Inhibitors
| Cat.No. | Product Name | Information | Product Use Citations | Product Validations |
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| S7093 | IPA-3 | IPA-3 is a selective non-ATP competitive Pak1 inhibitor with IC50 of 2.5 μM in a cell-free assay, no inhibition to group II PAKs (PAKs 4-6). |
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| S7271 | FRAX597 | FRAX597 is a potent, ATP-competitive inhibitor of group I PAKs with IC50 of 8 nM, 13 nM, and 19 nM for PAK1, PAK2, and PAK3, respectively. |
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| S7094 | PF-3758309 | PF-03758309 (PF-03758309) is a potent, ATP-competitive, pyrrolopyrazole inhibitor of PAK4 with Kd of 2.7 nM. This compound is antiproliferative and induces apoptosis in a HCT116 tumour model. |
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| S7807 | FRAX486 | FRAX486 is a potent p21-activated kinase (PAK) inhibitor with IC50 values of 14, 33, 39 and 575 nM for PAK1, PAK2, PAK3 and PAK4 respectively. |
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| S7989 | FRAX1036 | FRAX-1036 is a potent and selective PAK inhibitor with biochemical potency (Ki) of 23.3 nM and 72.4 nM against PAK1 and PAK2. |
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| S8264 | NVS-PAK1-1 | NVS-PAK1-1 is a potent and selective allosteric p21-activated kinase 1 (PAK1) inhibitor with an IC50 of 5 nM. |
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| S1976 | LCH-7749944 | LCH-7749944 (GNF-PF-2356) is a novel and potent p21-activated kinase 4 (PAK4) inhibitor with an IC50 of 14.93 μM and has a less potent inhibitory effect against PAK1, PAK5 and PAK6. This compound causes successful inhibition of EGFR activity due to its inhibitory effect on PAK4. |
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| E2484 | Hydrastine | Hydrastine ((-)-β-Hydrastine; (1R,9S)-β-Hydrastine), a natural alkaloid present in Hydrastis canadensis, is an inhibitor of PAK4. | ||
| S8139New | G-5555 | G-5555 is a selective inhibitor of Group I p21-activated kinases (PAKs), including PAK1, PAK2, and PAK3, with Ki values of 3.7 nM for PAK1 and 11 nM for PAK2. | ||
| E2380 | GNE 2861 | GNE 2861, a PAK inhibitor that displays group II selectivity, inhibits PAK4, PAK5 and PAK6 with IC50s of 7.5, 36, 126 nM, respectively. | ||
| S8032 | PRT062607 (P505-15) HCl | PRT062607 (P505-15, BIIB057, PRT-2607) HCl is a novel, highly selective Syk inhibitor with IC50 of 1 nM in cell-free assays, >80-fold selective for Syk than Fgr, PAK5, Lyn, FAK, Pyk2, FLT3, MLK1 and Zap70. |
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| S8444 | Padnarsertib (KPT-9274, ATG-019) | Padnarsertib (KPT 9274) is an orally bioavailable small molecule that is a non-competitive dual inhibitor of PAK4 and NAMPT. It shows an IC50 of ~120 nM for NAMPT in a cell-free enzymatic assay. |
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