产品
编 号：F747737
分子式：C16H11Cl2FN4O2
分子量：381.19
分子式：C16H11Cl2FN4O2
分子量：381.19
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CAS No: 1888305-17-6
产品详情
生物活性：
ERK5-IN-4 (compound 34b) is a potent and selective inhibitor of extracellular signal-related kinase 5 (ERK5). ERK5-IN-4 inhibits ERK5 (full-length) and truncated ERK5 (ERK5 ΔTAD) kinase activity in HEK293 cells with an IC50 of 77 nM and 300 nM, respectively.
体内研究：
ERK5-IN-4 (compound 34b) (p.o.; 10 mg/kg) has low clearance and an oral bioavailability of 42% in the mouse.Animal Model:Pharmacokinetic Parameters for ERK5-IN-4
Dosage:
Administration:
Result:RouteDose (mg/kg)Cl (mL/min/kg)Vd (L/kg)t1/2 (min)BA (%)
i.v. or p.o.10140.68042
体外研究：
ERK5-IN-4 (compound 34b) is selective against MAP3K, p38 (IC50>30 μM) and BRD4 (IC50>20 μM), in contrast to many reported ERK5 inhibitors.ERK5-IN-4 (0-100 μM; 72 h) suppresses ERK5 kinase activity in HEK293 cells and (0-1 μM; 72 h) induces paradoxical activation of ERK5 transcriptional activity, thus resulting in C-terminal transcriptional activation domain (TAD) separated from the nuclear localization sequence (NLS) and results ERK5 nuclear translocation.ERK5-IN-4 inhibits cancer cells with GI50 of 19.6 μM (HEK293), 22.3 μM (A498), 25 μM (SJSA-1), 26.6 μM (MDA-MB-231) following a 72 h incubation.ERK5-IN-4 exhibits kinome selectivity Kd of 1.2 μM, 0.29 μM, 0.046 μM, 0.061 μM, 0.18 μM, 0.38 μM, 1.3 μM, 0.42 μM, 0.22 μM, 2.8 μM against ABL1-nonphosphorylated, AURKA, CSF1R, DCAMKL1 (DCLK1), ERK5 (MAPK7), FGFR1, JAK3 (JH1domain-catalytic), KIT, LRRK2, MEK5 (MAP2K5).
ERK5-IN-4 (compound 34b) is a potent and selective inhibitor of extracellular signal-related kinase 5 (ERK5). ERK5-IN-4 inhibits ERK5 (full-length) and truncated ERK5 (ERK5 ΔTAD) kinase activity in HEK293 cells with an IC50 of 77 nM and 300 nM, respectively.
体内研究：
ERK5-IN-4 (compound 34b) (p.o.; 10 mg/kg) has low clearance and an oral bioavailability of 42% in the mouse.Animal Model:Pharmacokinetic Parameters for ERK5-IN-4
Dosage:
Administration:
Result:RouteDose (mg/kg)Cl (mL/min/kg)Vd (L/kg)t1/2 (min)BA (%)
i.v. or p.o.10140.68042
体外研究：
ERK5-IN-4 (compound 34b) is selective against MAP3K, p38 (IC50>30 μM) and BRD4 (IC50>20 μM), in contrast to many reported ERK5 inhibitors.ERK5-IN-4 (0-100 μM; 72 h) suppresses ERK5 kinase activity in HEK293 cells and (0-1 μM; 72 h) induces paradoxical activation of ERK5 transcriptional activity, thus resulting in C-terminal transcriptional activation domain (TAD) separated from the nuclear localization sequence (NLS) and results ERK5 nuclear translocation.ERK5-IN-4 inhibits cancer cells with GI50 of 19.6 μM (HEK293), 22.3 μM (A498), 25 μM (SJSA-1), 26.6 μM (MDA-MB-231) following a 72 h incubation.ERK5-IN-4 exhibits kinome selectivity Kd of 1.2 μM, 0.29 μM, 0.046 μM, 0.061 μM, 0.18 μM, 0.38 μM, 1.3 μM, 0.42 μM, 0.22 μM, 2.8 μM against ABL1-nonphosphorylated, AURKA, CSF1R, DCAMKL1 (DCLK1), ERK5 (MAPK7), FGFR1, JAK3 (JH1domain-catalytic), KIT, LRRK2, MEK5 (MAP2K5).
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