PAK

Isoform-selective Products

PAK1 PAK3 PAK2 PAK4 PAK5 PAK6

Signaling Pathway

PAK Products

All (11)
PAK Inhibitors (11)
New PAK Products

Catalog No.	Product Name	Information	Product Use Citations
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 Rep, 2024, 14(1):7739 J Exp Med, 2023, 220(9)e20230054 J Exp Med, 2023, 220(9)e20230054
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).	Nat Commun, 2024, 15(1):2989 Biomolecules, 2024, 14(2)237 Cell Death Dis, 2023, 14(7):463
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.	J Cell Physiol, 2024, 10.1002/jcp.31291 Sci Rep, 2024, 14(1):4060 Nat Commun, 2023, 14(1):700
S7094	PF-3758309	PF-03758309 (PF-03758309) is a potent, ATP-competitive, pyrrolopyrazole inhibitor of PAK4 with Kd of 2.7 nM. PF-3758309 is antiproliferative and induces apoptosis in a HCT116 tumor model.	Oncogene, 2023, 42(39):2878-2891 Oncogene, 2023, 10.1038/s41388-023-02809-0 Biomolecules, 2023, 13(1)100
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.	iScience, 2023, 26(8):107333 Biochim Biophys Acta Mol Cell Res, 2022, 1869(8):119264 Mol Cell, 2020, 80(6):1104-1122.e9
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.	Cell Rep Med, 2024, 5(2):101416 Sci Rep, 2023, 13(1):3334 Sci Adv, 2023, 9(15):eadf8522
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
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.	Endocrinology, 2023, 164(6)bqad073
E2484	Hydrastine	Hydrastine ((-)-β-Hydrastine; (1R,9S)-β-Hydrastine), a natural alkaloid present in Hydrastis canadensis, is an inhibitor of PAK4.
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.	Sci Rep, 2024, 14(1):7739 J Exp Med, 2023, 220(9)e20230054 J Exp Med, 2023, 220(9)e20230054
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).	Nat Commun, 2024, 15(1):2989 Biomolecules, 2024, 14(2)237 Cell Death Dis, 2023, 14(7):463
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.	J Cell Physiol, 2024, 10.1002/jcp.31291 Sci Rep, 2024, 14(1):4060 Nat Commun, 2023, 14(1):700
S7094	PF-3758309	PF-03758309 (PF-03758309) is a potent, ATP-competitive, pyrrolopyrazole inhibitor of PAK4 with Kd of 2.7 nM. PF-3758309 is antiproliferative and induces apoptosis in a HCT116 tumor model.	Oncogene, 2023, 42(39):2878-2891 Oncogene, 2023, 10.1038/s41388-023-02809-0 Biomolecules, 2023, 13(1)100
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.	iScience, 2023, 26(8):107333 Biochim Biophys Acta Mol Cell Res, 2022, 1869(8):119264 Mol Cell, 2020, 80(6):1104-1122.e9
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.	Cell Rep Med, 2024, 5(2):101416 Sci Rep, 2023, 13(1):3334 Sci Adv, 2023, 9(15):eadf8522
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
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.	Endocrinology, 2023, 164(6)bqad073
E2484	Hydrastine	Hydrastine ((-)-β-Hydrastine; (1R,9S)-β-Hydrastine), a natural alkaloid present in Hydrastis canadensis, is an inhibitor of PAK4.
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.

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