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  • PAK Inhibitors (9)
  • New PAK Products
Catalog No. Product Name Information Product Use Citations Product Validations
E2380New 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.
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 less potently inhibitory effect against PAK1, PAK5 and PAK6. LCH-7749944 causes successful inhibition of EGFR activity due to its inhibitory effect on PAK4.
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).
NPJ Precis Oncol, 2022, 6(1):52
Front Pharmacol, 2022, 13:778680
Virus Res, 2022, 315:198794
S7094 PF-3758309 PF-03758309 (PF-03758309) is a potent, ATP-competitive, pyrrolopyrazole inhibitor of PAK4 with IC50 of 1.3 nM. PF-3758309 is antiproliferative and induces apoptosis in a HCT116 tumor model.
Front Microbiol, 2022, 13:845259
Cancers (Basel), 2021, 14(1)160
Curr Biol, 2021, S0960-9822(21)00626-6
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.
Cell Rep, 2022, 38(4):110306
NPJ Precis Oncol, 2022, 6(1):52
J Cell Mol Med, 2022, 26(10):2895-2907
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.
Biochim Biophys Acta Mol Cell Res, 2022, 1869(8):119264
Mol Cell, 2020, 80(6):1104-1122.e9
Mol Syst Biol, 2019, 15(8):e8828
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.
Nature, 2021, 595(7869):730-734
Sci Signal, 2020, 13(619)
Cell Death Differ, 2019, 10.1038/s41418-019-0342-5
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.
Cancer Cell, 2022, S1535-6108(22)00312-9
Cell Rep, 2022, 38(8):110414
Mol Cell, 2021, S1097-2765(21)00264-1
S8444 KPT 9274 ( ATG-019) KPT 9274 ( ATG-019) 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.
NAT CANCER, 2021, 2, 83–97
E2380New 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.
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 less potently inhibitory effect against PAK1, PAK5 and PAK6. LCH-7749944 causes successful inhibition of EGFR activity due to its inhibitory effect on PAK4.
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).
NPJ Precis Oncol, 2022, 6(1):52
Front Pharmacol, 2022, 13:778680
Virus Res, 2022, 315:198794
S7094 PF-3758309 PF-03758309 (PF-03758309) is a potent, ATP-competitive, pyrrolopyrazole inhibitor of PAK4 with IC50 of 1.3 nM. PF-3758309 is antiproliferative and induces apoptosis in a HCT116 tumor model.
Front Microbiol, 2022, 13:845259
Cancers (Basel), 2021, 14(1)160
Curr Biol, 2021, S0960-9822(21)00626-6
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.
Cell Rep, 2022, 38(4):110306
NPJ Precis Oncol, 2022, 6(1):52
J Cell Mol Med, 2022, 26(10):2895-2907
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.
Biochim Biophys Acta Mol Cell Res, 2022, 1869(8):119264
Mol Cell, 2020, 80(6):1104-1122.e9
Mol Syst Biol, 2019, 15(8):e8828
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.
Nature, 2021, 595(7869):730-734
Sci Signal, 2020, 13(619)
Cell Death Differ, 2019, 10.1038/s41418-019-0342-5
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.
Cancer Cell, 2022, S1535-6108(22)00312-9
Cell Rep, 2022, 38(8):110414
Mol Cell, 2021, S1097-2765(21)00264-1
S8444 KPT 9274 ( ATG-019) KPT 9274 ( ATG-019) 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.
NAT CANCER, 2021, 2, 83–97
E2380New 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.
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