PAK

亜型選択性的な製品

PAK1 PAK3 PAK2 PAK4 PAK5 PAK6

シグナル伝達経路

PAK製品

All (11)
PAK阻害剤 (11)
新製品

製品コード	製品名称	製品説明	文献中Selleckの製品使用例
S8032	PRT062607 (P505-15) HCl	PRT062607 (P505-15, BIIB057, PRT-2607) 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 PAK1 inhibitor.	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) 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 PAK1 inhibitor.	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.

PAK阻害剤の選択性比較