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KIN-8194

  Cat. No.:  DC70541  
Chemical Structure
330786-01-1
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More than 5000 active chemicals with high quality for research!
Field of application
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.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 330786-01-1
Chemical Name: KIN-8194
Synonyms: KIN8194
Formula: C28H33N7O
M.Wt: 483.62
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
Cat. No. Product name Field of application
DC48043 BIIB091 BIIB091 is a novel reversible, selective, potent BTK inhibitor with Kd of 0.07 nM.
DC47717 TAK-020 TAK-020 is a covalent Btk inhibitor, which becomes the clinical candidate.
DC42420 Tolebrutinib Tolebrutinib (SAR442168) is a potent, selective, orally active and brain-penetrant of Bruton tyrosine kinase (BTK), with IC50s of 0.4 and 0.7 nM in Ramos B cells and in HMC microglia cells, respectively. Tolebrutinib can be used for the research of multiple sclerosis (MS).
DC40447 N-piperidine Ibrutinib hydrochloride N-piperidine Ibrutinib hydrochloride (Compound 1) is a reversible Ibrutinib derivative. N-piperidine Ibrutinib hydrochloride is a potent BTK inhibitor with IC50s of 51.0 and 30.7 nM for WT BTK and C481S BTK, respectively. N-piperidine Ibrutinib hydrochloride can be used as a BTK ligand in the synthesis of a series of PROTACs, such as SJF620. SJF620 is a potent PROTAC BTK degrader with a DC50 of 7.9 nM.
DC39103 Remibrutinib (LOU064) Remibrutinib (LOU064) is a potent, highly selective covalent inhibitor of bruton tyrosine kinase (BTK) with IC50 of 1.3 nM, 2.5 nM and 18 nM for BTK, FcγR-induced IL8 and anti-IgM/IL4-induced CD69, respectively. Remibrutinib (LOU064) exhibits an exquisite kinase selectivity due to binding to an inactive conformation of BTK and has the potential for the treatment of autoimmune diseases.
DC28073 CNX-500 CNX-500 is a probe consisting of a covalent Btk inhibitor (CC-292) chemically linked to biotin. CNX-500 retains inhibitory activity against Btk (IC50 of 0.5 nM) and the ability to form a covalent bond with Btk. CNX-500 has low inhibitory effects on kinase epidermal growth factor receptor, and upstream Src-family kinases including Syk and Lyn.
DC11914 Poseltinib Poseltinib (HM-71224, LY-3337641) is a potent and selective, covalent inhibitor of Btk with IC50 of 1.95 nM.
DC8358 ONO-4059(Tirabrutinib) ONO-4059 is a novel Small Molecule Dual Inhibitor Of Bruton’s Tyrosine Kinase (Btk) and Tec Kinase.
DC9942 GDC-0853(RG7845) GDC-0853 is orally available inhibitor of Bruton's tyrosine kinase (BTK) with potential antineoplastic activity.
DC77159 Rilzabrutinib Rilzabrutinib (PRN1008) is an orally active Bruton's tyrosine kinase (BTK) inhibitor with anti-inflammatory and immunomodulatory activities. Rilzabrutinib can be used in the research of various inflammatory and immune-related diseases such as acute respiratory distress syndrome and sepsis.
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