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Chemical Structure : KIN-8194
Catalog No.: PC-72484Not For Human Use, Lab Use Only.
KIN-8194 (KIN8194) is a highly potent dual HCK and BTK inhibitor with IC50 of <0.495 and 0.915 nM, respectively.
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KIN-8194 (KIN8194) is a highly potent dual HCK and BTK inhibitor with IC50 of <0.495 and 0.915 nM, respectively.
KIN-8194 demonstrated greater selectivity compared with A419259 with no KIT, RET, PDGFRA, EPHB6, or CDPK1 inhibition.
KIN-8194 binds to gatekeeper residue Thr333 of HCK, but not to Cys481 of BTK.
KIN-8194 shows robust inhibition of both HCK and BTK activity in MYD88-mutated cells, showed robust inhibition of HCK Tyr410 phosphorylation; inhibits the growth and survival of MYD88-mutated WM and ABC DLBCL cells.
KIN-8194 overcomes ibrutinib resistance relatedto BTK Cys481Ser-expressing MYD88-mutated B-cell lymphoma cells, synergizes with the BCL-2 inhibitor venetoclax.
KIN-8194 shows superior activity over ibrutinib in MYD88-mutated TMD-8 ABC DLBCL xenograft mouse model.
KIN-8194 is active against ibrutinib resistance in BTK Cys481Ser -expressing ABC DLBCL xenograft mouse model.
| M.Wt | 483.62 | |
| Formula | C28H33N7O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Guang Yang, et al. Blood. 2021 Nov 18;138(20):1966-1979.
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