BTK

GNE-431: potent, selective noncovalent Btk inhibitor, IC50=3.2 nM; effective against C481R, T474I, T474M mutants, may counter ibrutinib resistance.

BTK-IN-6, a potent BTK inhibitor, may treat immune, cardiac, cancer, viral, inflammatory, metabolic, and neurological disorders.

BTK-IN-8: potent, selective covalent BTK inhibitor; IC50=0.22 nM, Kd=0.91 nM; effective in blood CD69 cells (IC50=0.029 μM).

JAK3/BTK-IN-7 (XL-12), characterized as a JAK3/BTK inhibitor, exhibits IC 50 values of 2 nM and 14 nM for JAK3 and BTK respectively. This compound demonstrates anti-inflammatory properties and is applicable in research related to rheumatoid arthritis [1].

Brefeldin A 4-O-nicotinate (CHNQD-01228) is a dual inhibitor of Arf1 and BMX proteins with an IC50 value of 0.22 μM for T24 cell proliferation. It also suppresses T24 cell migration and colony formation in a dose-dependent manner, induces G1 phase arrest, and triggers apoptosis. By targeting BMX proteins, it inhibits the AKT/p-AKT and STAT3/p-STAT3 signaling pathways, while also inhibiting Arf1 proteins to eliminate bladder cancer stem cells and activate antitumor immunity, thus exhibiting anticancer activity. Brefeldin A 4-O-nicotinate is applicable in research related to bladder cancer.

WS-11 is a non-covalent reversible inhibitor of BTK, with IC50 values of 3.9 nM for the wild-type and 2.2 nM for the C481S mutant BTK. In addition to strong hydrogen bonding, WS-11 also forms robust π-π interactions with PHE540, and p-π interactions with LYS430 within the active pocket.

BTK-IN-38 (Example 125) is an efficacious inhibitor of BTK. It effectively suppresses the proliferation of DOHH2 and BT474 cells, with IC50 values of 114 nM and 340 nM, respectively.

BTK-IN-15: Oral BTK inhibitor, IC50 0.7 nM, induces cancer cell apoptosis, selective with anti-tumor effects.

UBX-382 is an orally administered proteolysis-targeting chimera (PROTAC) designed to target BTK and disrupt B-cell receptor signaling. It demonstrates enhanced degradation of both wild-type and mutant BTK proteins, exhibiting anti-cancer effects in murine xenograft models using TMD-8 cells [1].

RET-IN-14 inhibits RET (IC50: <0.51-9.3 nM) & BTK (C481S) (IC50: 9.2-15 nM), promising for tumor research.

BIIB129 is a selective and brain-penetrant BTK covalent inhibitor used to study B-cell proliferation-related diseases.

Vecabrutinib (SNS-062) is a potent and noncovalent BTK and ITK inhibitor (Kd: 0.3 nM and 2.2 nM, respectively). Vecabrutinib displays an IC50 of 24 nM for ITK.

Ibrutinib is a selective, irreversible Btk inhibitor (IC50: 0.5 nM). Ibrutinib Racemate is the racemate of Ibrutinib.

PCI 45227 is an active metabolite of the Bruton's tyrosine kinase inhibitor ibrutinib .1PCI 45227 is formed from ibrutinib by the cytochrome P450 (CYP) isoform CYP3A. 1.Veeraraghavan, S., Viswanadha, S., Thappali, S., et al.Simultaneous quantification of lenalidomide, ibrutinib and its active metabolite PCI-45227 in rat plasma by LC-MS/MS: Application to a pharmacokinetic studyJ. Pharm. Biomed. Anal.107151-158(2015)