PAK Inhibitor
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AKT1-IN-13
0 ImagesCat. No.: HY-184145AKT1-IN-13 is an orally active AKT1 inhibitor with an IC50 of 5.17 μM. AKT1-IN-13 also exhibits high inhibitory activity against PAK1, PKA, MAP2K1 (MEK1 / MAPKK1) and MAPK1 (ERK2). AKT1-IN-13 induces cell apoptosis, activates the pro-apoptotic protein BAX, inhibits the anti-apoptotic protein Bcl-2, and activates caspase 3 simultaneously. As a cytotoxic agent, AKT1-IN-13 exerts a killing effect on orthotopically transplanted liver cancer in an AKT1-dependent manner. AKT1-IN-13 can be used in studies related to hepatocellular carcinoma.
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PF-3758309 hydrochloride
0 ImagesCat. No.: HY-13007ACAS No.: 1279034-84-2Synonyms: PF-03758309 hydrochloridePF-3758309 (PF-03758309) hydrochloride is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (Kd= 2.7 nM; Ki=18.7 nM). PF-3758309 hydrochloride has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation.
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GR2-128
0 ImagesCat. No.: HY-184396GR2-128 is a dual inhibitor targeting MLK3 and NAMPT with IC50 values of 84 nM and 14 nM, respectively. GR2-128 inhibits downstream JNK/c‑Jun signaling and reduces NAD+ levels. GR2-128 exhibits antiproliferative and pro-apoptotic activities in triple-negative breast cancer cells without significant toxicity to normal cells. GR2-128 suppresses tumor growth, reduces macrophage and neutrophil infiltration, and increases tumor T-cell markers in a syngeneic mouse model, and can be used for triple-negative breast cancer research.
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Rac/Cdc42-IN-1
0 ImagesCat. No.: HY-183246CAS No.: 2143950-05-2Rac/Cdc42-IN-1, the major phase I metabolite of the oral Rac/Cdc42 inhibitor MBQ-167 (HY-112842) in vivo, is a selective Rac inhibitor. Rac/Cdc42-IN-1 functions by blocking the GTP-binding activation of Rac1, targeting the autophosphorylation of Thr423/Thr402/Thr436 and Ser141/Ser144/Ser154 in downstream PAK1/2/3, with an inhibitory effect superior to that of MBQ-167. Rac/Cdc42-IN-1 significantly inhibits cell migration, and suppresses tumor growth and distant metastasis to the lung, liver and kidney in HER2+ breast cancer mouse models. Rac/Cdc42-IN-1 can be used for targeted research on metastatic breast cancer.
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RN193
0 ImagesCat. No.: HY-184447CAS No.: 3091508-49-2RN193 is a type II kinase inhibitor with a human PAK1 IC50 of 4.28 μM. RN193 functionally inhibits kinase activity of PAK1, PAK2, and PAK3, and engages with their kinase domains in live cells. RN193 induces thermal shifts in CLK1, GSK3B, ULK1, MELK, MAPK13, BRAF, and STK10, indicating binding and stabilization of these proteins. RN193 induces formation of PAK3:PAK2 heterodimers and displaces PAK2 homodimers in live cells. RN193 acts as a tool compound for studying group I PAK conformational states.
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PAK4-IN-5
0 ImagesCat. No.: HY-159897PAK4-IN-5 (Compound 12i) is a PAK4 inhibitor (IC50: 7.68 nM for PAK4, 1872.01 nM for PAK1). PAK4-IN-5 binds to PAK4 stably via multiple interactions. PAK4-IN-5 inhibits the proliferation and the migratory potential of MDA-MB-231 cells by inhibiting the phosphorylation of PAK4 and LIMK1. PAK4-IN-5 arrests cell cycle in the G0/G1 phase, induces apoptosis and ROS production. LD50: >500 mg/kg for mice (p.o.).
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PF-3758309 dihydrochloride
0 ImagesCat. No.: HY-13007BSynonyms: PF-03758309 dihydrochloridePF-3758309 (PF-03758309) dihydrochloride is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (Kd= 2.7 nM; Ki=18.7 nM). PF-3758309 dihydrochloride has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation.
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G-9791
0 ImagesCat. No.: HY-116917CAS No.: 1926204-95-6G-9791, a poyridone side chain analogue, is a potent PAK inhibitor with Ki values of 0.95 nM and 2.0 nM for PAK1 and PAK2, respectively.
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PI3Kα-IN-27
0 ImagesCat. No.: HY-178812CAS No.: 2098649-83-1PI3Kα-IN-27 (Compound 50b) is an orally active PI3K-α inhibitor, with an IC50 of 40 nM. PI3Kα-IN-27 effectively inhibits PAK3, p110α, phospho-mTOR and phospho-ERK1/2. PI3Kα-IN-27 induces early Apoptosis. PI3Kα-IN-27 shows anticancer activity against pancreatic cancer, lung cancer, breast cancer.
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CZh226 hydrochloride
0 ImagesCat. No.: HY-111103ACAS No.: 2231440-94-9CZh226 hydrochloride is a potent and selective PAK4 inhibitor with an IC50 of 18 nM, and its selectivity for PAK1 is 346 times. The oral bioavailability of CZh226 hydrochloride is poor, and it requires the use of the prodrug PAK4-IN-1 (HY-130628) to improve absorption and metabolic stability. CZh226 hydrochloride can be used for research on colorectal cancer and melanoma.
