| S7093 |
IPA-3
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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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Discov Oncol, 2025, 16(1):364
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Nat Commun, 2024, 15(1):2989
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Biomolecules, 2024, 14(2)237
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| S7271 |
FRAX597
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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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BMC Biol, 2025, 23(1):166
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J Cell Physiol, 2024, 10.1002/jcp.31291
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Sci Rep, 2024, 14(1):4060
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| S7094 |
PF-3758309
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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 tumor model.
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Cell Commun Signal, 2025, 23(1):135
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Nat Commun, 2024, 15(1):3178
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Oncogene, 2023, 42(39):2878-2891
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| S7807 |
FRAX486
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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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iScience, 2023, 26(8):107333
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Biochim Biophys Acta Mol Cell Res, 2022, 1869(8):119264
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J Mol Cell Biol, 2021, 13(1):41-58
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| S7989 |
FRAX1036
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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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bioRxiv, 2023, 10.1101/2023.12.15.571909
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Cell Rep, 2022, 41(1):111442
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Nature, 2021, 595(7869):730-734
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| S8264 |
NVS-PAK1-1
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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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NPJ Breast Cancer, 2023, 9(1):48
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J Med Chem, 2022, 65(23):15627-15641
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| S1976 |
LCH-7749944
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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. This compound causes successful inhibition of EGFR activity due to its inhibitory effect on PAK4.
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J Exp Clin Cancer Res, 2025, 44(1):134
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Endocrinology, 2023, 164(6)bqad073
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| E2484 |
Hydrastine
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Hydrastine ((-)-β-Hydrastine; (1R,9S)-β-Hydrastine), a natural alkaloid present in Hydrastis canadensis, is an inhibitor of PAK4.
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| S8139New |
G-5555
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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.
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| E2380 |
GNE 2861
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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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| S8032 |
PRT062607 (P505-15) HCl
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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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Sci Adv, 2025, 11(31):eadu4270
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Sci Rep, 2024, 14(1):7739
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J Exp Med, 2023, 220(9)e20230054
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| S8444 |
Padnarsertib (KPT-9274, ATG-019)
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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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Signal Transduct Target Ther, 2025, 10(1):222
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Cell Rep Med, 2024, 5(2):101416
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Sci Rep, 2023, 13(1):3334
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