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DFG-out inactive conformation

" in MedChemExpress (MCE) Product Catalog:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-107779
    BI-882370

    		Raf Cancer
    BI-882370 is a potent and selective RAF kinase inhibitor that binds to the ATP binding site of the kinase positioned in the DFG-out (inactive) conformation of the BRAF kinase. BI-882370 (BI 882370) inhibits the oncogenic BRAF V600E-mutant, the WT BRAF and CRAF kinases with IC50s of 0.4, 0.8, and 0.6 nM, respectively. BI-882370 also inhibits SRC family kinases .
    BI-882370
  • HY-160478
    GNF-6

    		Bcr-Abl Cancer
    GNF-6 (Compound 14) inhibits the gatekeeper threonine residue mutation of BCR-ABL-T315I with IC50s of 0.25 μM, 0.09 μM and 0.590 μM for c-ABL-T334I, BCR-ABL and BCR-ABL-T315I variants, respectively. GNF-6, an ATP competitive inhibitor, disrupts the assembly of the hydrophobic spine (a network of hydrophobic interactions), thereby locking the kinase in an inactive ‘DFG-out’ conformation .
    GNF-6
  • HY-125444
    TH251

    		LIM Kinase (LIMK) Neurological Disease Cancer
    TH251 is a LIMK1 and LIMK2 inhibitor with IC50s of 52 nM and 47 nM against LIMK1 and LIMK2, respectively. TH251 binds to inactive αC-out and DFG-out LIMK1 conformations, inhibits unphosphorylated LIMK1 and LIMK2 enzymatic activity, and exhibits unchanged potency despite PAK-mediated phosphorylation of either kinase. TH251 can be used for the research of cancers, glaucoma, and CNS diseases .
    TH251
  • HY-107779R
    BI-882370 (Standard)

    		Reference Standards Raf Cancer
    BI-882370 (Standard) is the analytical standard of BI-882370 (HY-107779). This product is intended for research and analytical applications. BI-882370 is a potent and selective RAF Kinase inhibitor that binds to the ATP binding site of the Kinase positioned in the DFG-out (inactive) conformation of the BRAF Kinase. BI-882370 (BI 882370) inhibits the oncogenic BRAFV600E-mutant, the WT BRAF and CRAF Kinases with IC50s of 0.4, 0.8, and 0.6 nM, respectively. BI-882370 also inhibits SRC family Kinases .
    BI-882370 (Standard)
  • HY-18909
    Multi-kinase-IN-11

    		Src Bcr-Abl Pyk2 p38 MAPK c-Kit Others
    Multi-kinase-IN-11 (Compound 1a) is a DFG-out conformation-targeted multi-kinase inhibitor, including SRC, LCK, ABL, PYK2, CSK, HCK, P38 and C-KIT. Multi-kinase-IN-11 serves as a scaffold for the preparation of fluorescently labeled binding probes and affinity matrices .
    Multi-kinase-IN-11

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