Zanubrutinib is a selective Bruton tyrosine kinase (BTK) inhibitor.
BTK-IN-10 is a potent BTK inhibitor with IC50s of <5 nM for wild-type BTK or mutated BTK (C481S), respectively (WO2022012509A1; example 111)[1].
VA5 is a BTK kinaseinhibitor. VA5 has the potential to be used to study diseases associated with BTK kinase activity.
AS-1763 is a potent, selective, noncovalent, and orally available inhibitor of Bruton’s tyrosine kinase (IC50 = 0.85 nM).
BGB-8035 is an orally active, highly selective bruton's tyrosine kinase (BTK) inhibitor with IC50s of 1.1 nM, 99 nM, 621 nM for BTK, TEC, EGFR, respectively. BGB-8035 has antitumor and anti-arthritis activity. BGB-8035 has the potential for B-cell malignancies and autoimmune diseases research[1].
Terreic acid, a quinone epoxide antibiotic, acts as an effective Btk inhibitor. Terreic acid blocks the interaction between PKC and the pleckstrin homology domain of Btk. Terreic acid inhibits the binding of GST-BtkPH to PKC in lysates of HMC-1 human mast cells with an IC50 of approximately 100 μM[1].
Ibrutinib (PCI-32765) is a selective, irreversible Btk inhibitor with an IC50 of 0.5 nM.
(±)-Zanubrutinib is a potent, selective and orally available Bruton's tyrosine kinase (Btk) inhibitor.
Evobrutinib is an inhibitor of Bruton's tyrosin kinase (Btk) inhibitor extracted from patent US20140162983 example 0174.
BTK-IN-25 (compound 71) is a potent inhibitor of BTK, and inhibits BTK(C481S) with an IC50 value of 0.77 nM. BTK-IN-25 inhibits BTK in DOHH2 cells with an IC50 value of 1 nM[1].
G-744 is a highly potent, selective Btk inhibitor with an IC50 of 2 nM.
HZ-A-005 is a potent, selective, and covalent Bruton’s tyrosine kinase (BTK) inhibitor. HZ-A-005 markedly decreases tumor growth in xenograft mouse models[1].
PCI-33380 is an irreversible Bruton's Tyrosine Kinase (BTK) inhibitor (fluorescent probe).
Ibrutinib-biotin is a probe that consists of Ibrutinib linked to biotin via a long chain linker, extracted from patent WO2014059368A1 Compound 1-5, has an IC50 of 0.755-1.02 nM for BTK.
Btk inhibitor 1 R enantiomer is a pyrazolo[3,4-d]pyrimidine derivative as a Btk kinase inhibitor.IC50 value:Target: BtkFrom PCT Int. Appl. (2012), WO 2012158843 A2 20121122.
PROTAC BTK Degrader-2 is a potent BTK PROTAC degrader. PROTAC BTK Degrader-2 effectively reduces BTK protein levels[1].
Edralbrutinib is a potent BTK inhibitor[1].
Btk inhibitor 1 is a pyrazolo[3,4-d]pyrimidine derivative as a Btk kinase inhibitor.IC50 value:Target: BtkFrom PCT Int. Appl. (2012), WO 2012158843 A2 20121122.
Acalabrutinib is a novel, potent, and highly selective BTK inhibitor, with an IC50 of 3 nM and EC50 of 8 nM in in vitro assay.
JDB175 is a highly selective BTK inhibitor with oral activity and excellent blood-brain barrier penetration. JDB175 shows good activity in the mouse model of central nervous system lymphoma without obvious signs of toxicity, effectively inhibits the proliferation of BTK signaling pathway of human lymphoma cells, induces cell cycle arrest, and promotes cell apoptosis [1].
BTK-IN-26 (compound 18) is a potent inhibitor of Bruton's tyrosine kinase (BTK) and its C481 mutant, with IC50 values of 0.7 and 0.8 nM for BTK and BTK C481S, respectively. BTK-IN-26 can be used for cancer and autoimmune diseases research[1].
Vecabrutinib is a potent, noncovalent BTK and ITK inhibitor, with Kd of 0.3 nM and 2.2 nM, respectively; Vecabrutinib shows an IC50 of 24 nM for ITK.
(S)-Sunvozertinib ((S)-DZD9008), the S-enantiomer of Sunvozertinib, shows inhibitory activity against EGFR exon 20 NPH and ASV insertions, EGFR L858R/T790M mutation and Her2 exon20 YVMA insertion (IC50=51.2 nM, 51.9 nM, 1 nM, and 21.2 nM, respectively). (S)-Sunvozertinib also inhibits BTK[1].
Ibrutinib D5 (PCI-32765 D5) is a deuterium labeled Ibrutinib. Ibrutinib is a selective, irreversible Btk inhibitor[1].