JWG-071 is the first reported kinase-selective chemical probe for ERK5, inhibits ERK5 and LRRK2 with IC50 of 88 and 109 nM, respectively. JWG-071 improves ERK5 activity and BRD4 selectivity.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
|Related ERK Products|
2',5'-Dihydroxyacetophenone (DHAP, 2-Acetylhydroquinone, Quinacetophenone) is a mixture of dihydroxyacetophenone isomers used in food flavoring. 2',5'-Dihydroxyacetophenone significantly inhibits the production of NO by inhibiting the expression of iNOS. 2',5'-Dihydroxyacetophenone significantly reduces the expression levels of the pro-inflammatory cytokines TNF-α and IL-6 by blocking the ERK1/2 and NF-κB signaling pathways.
Tenuifoliside A is isolated from Yuanzhi and has anti-apoptotic and antidepressant effects. In C6 cells, Tenuifoliside A exhibits its neurotrophic effects and promotes cell proliferation through the ERK/CREB/BDNF signaling pathway.
Tauroursodeoxycholate (Tauroursodeoxycholic acid; TDUCA) dihydrate is an endoplasmic reticulum stress inhibitor. Tauroursodeoxycholate significantly reduces the expression of apoptotic molecules such as caspase-3 and caspase-12. Tauroursodeoxycholate also suppresses ERK.
DMU-212 is a resveratrol methylated derivative with anti-division, antiproliferative, antioxidant and apoptosis-promoting activities. DMU-212 causes mitosis to stop by inducing apoptosis and activating the ERK1/2 protein.
(rel)-AR234960 is the relatively active configuration of AR234960. AR234960 is a non-peptide MAS (a G protein coupling receptor) agonist that upregulates CTGF mRNA and protein levels through the ERK1/2 signaling pathway in HEK293-MAS cells and adult myocardial fibroblasts.
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