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PAK Inhibitors

Cat.No. Product Name Information Product Use Citations Product Validations
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).
Discov Oncol, 2025, 16(1):364
Nat Commun, 2024, 15(1):2989
Biomolecules, 2024, 14(2)237
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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.
BMC Biol, 2025, 23(1):166
J Cell Physiol, 2024, 10.1002/jcp.31291
Sci Rep, 2024, 14(1):4060
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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 tumor model.
Cell Commun Signal, 2025, 23(1):135
Nat Commun, 2024, 15(1):3178
Oncogene, 2023, 42(39):2878-2891
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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.
Journal of Cell Science, February 26, 2025, JCS263636
Biochimica et Biophysica Acta (BBA) - Proteins and Proteomics, February 2018, 356-365
iScience, 2023, 26(8):107333
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.
bioRxiv, 2023, 10.1101/2023.12.15.571909
Cell Rep, 2022, 41(1):111442
Nature, 2021, 595(7869):730-734
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.
NPJ Breast Cancer, 2023, 9(1):48
J Med Chem, 2022, 65(23):15627-15641
Biomedicines, 2021, 1410
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. This compound causes successful inhibition of EGFR activity due to its inhibitory effect on PAK4.
Endocrinology, June 2023, bqad073
Journal of Experimental & Clinical Cancer Research, 2025, 134
J Exp Clin Cancer Res, 2025, 44(1):134
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.
British Journal of Cancer, August 11, 2023, 1071-1082
British Journal of Cancer, 2023, 1071-1082
E2484 Hydrastine Hydrastine ((-)-β-Hydrastine; (1R,9S)-β-Hydrastine), a natural alkaloid present in Hydrastis canadensis, is an inhibitor of PAK4.
S8139 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.
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.
Sci Adv, 2025, 11(31):eadu4270
Scientific Reports, 2024, 7739
Sci Rep, 2024, 14(1):7739
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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.
Cell Reports Medicine, January 08 2026, 102540
Blood Advances, December 22 2025, Online ahead of print
Clinical Cancer Research, April 15 2021, 2352-2366