Btk Inhibitor

CHMFL-BTK-01 (compound 9) is a highly selective irreversible BTK inhibitor, with an IC₅₀ of 7 nM. CHMFL-BTK-01 (compound 9) potently inhibited BTK Y223 auto-phosphorylation.

PF-06250112 is a potent, highly selective, orally bioavailable BTK inhibitor with an IC₅₀ of 0.5 nM, shows inhibitory effect toward BMX nonreceptor tyrosine kinase and TEC with IC₅₀s of 0.9 nM and 1.2 nM, respectively.

BTK-IN-14 is a potent inhibitor of BTK. BTK plays an important role in signaling mediated by B cell antigen receptor (BCR) and Fcγreceptor (FcγR) in B cells and myeloid cells, respectively. BTK-IN-14 has the potential for the research of related diseases, especially autoimmune diseases, inflammatory diseases or cancer (extracted from patent WO2022057894A1, compound 1).

BTK-IN-20 (compound 283) is a BTK tyrosine kinase inhibitor and a 1H-pyrazolo[3,4-d]pyrimidine derivative. BTK-IN-20 can be used for the research of cancer and inflammation.

BTK-IN-27 (example 8) is a BTK inhibitor (IC₅₀: 0.2 nM). BTK-IN-27 shows anti-proliferative activity in TMD8 cells (IC₅₀: < 5 nM). BTK-IN-27 can be used for research of cancer, lymphoma, leukemia and immunological diseases.

Midobrutinib (Example 13) is a BTK inhibitor (IC₅₀: 0.813 nM). Midobrutinib can be used for research of diseases involving BTK, particularly cancer.

BTK-IN-11 is a potent inhibitor of BTK. BTK plays an important role in signaling mediated by B cell antigen receptor (BCR) and Fcγreceptor (FcγR) in B cells and myeloid cells, respectively. BTK-IN-11 has the potential for the research of related diseases, especially autoimmune diseases, inflammatory diseases or cancer (extracted from patent WO2022063101A1, compound Z2).

JAK3/BTK-IN-3 is a potent inhibitor of JAK3/BTK. BTK and JAK3 are two important targets for autoimmune diseases. Simultaneous inhibition of the BTK/JAK3 signalling pathway exhibits synergistic effects. JAK3/BTK-IN-3 has the potential for the research of JAK3 kinase and/or BTK-related diseases (extracted from patent WO2021147952A1, compound 009)

CA/PRAK-IN-1 is a dual inhibitor of carbonic anhydrase (Carbonic Anhydrase) and PRAK, with a K_i of 20.1 nM against hCA IX and 16.4 nM against hCA XII. CA/PRAK-IN-1 exhibits inhibitory activity against YES1 kinase, BTK, and MAP4K3. CA/PRAK-IN-1 induces G0/G1 phase arrest of the cancer cell cycle, inhibits DNA synthesis, disrupts hypoxia-driven survival pathways, promotes cell death, and shows broad-spectrum cytotoxicity against tumor cells. CA/PRAK-IN-1 can be used in research on various cancers including leukemia, colon cancer, melanoma, and renal cancer.

GSTO1-IN-2 (Compound B-9) is a dual covalent inhibitor of GSTO1/BTK with IC₅₀ values of 441 nM and 6.2 nM respectively.

BTK-IN-22 is a BTK inhibitor (IC₅₀: 0.9 nM). BTK-IN-22 also inhibits BLX and BMX with IC₅₀s of 1.4 and 1.2 nM respectively. BTK-IN-22 shows improved kinase selectivity compared to Ibrutinib (HY-10997)

JAK3/BTK-IN-7 (XL-12) is a JAK3/BTK inhibitor with IC₅₀ values of 2 nM and 14 nM, respectively. JAK3/BTK-IN-7 has anti-inflammatory activity and can be used in the study of rheumatoid arthritis.

BTK-IN-18 is a potent, reversible BTK inhibitor with an IC₅₀ of 0.002 µM. BTK-IN-18 inhibits both CD69 and CD86 in vivo.

BTK-IN-41 (Compound 47) is the inhibitor for BTK with an IC₅₀ of 5.4 nM. BTK-IN-41 inhibits the diffuse large B cell lymphoma cell TDM-8 with IC₅₀ of 13.8 nM.

BTK-IN-47 (Compound 9e) is a covalent, selective BTK inhibitor with an IC₅₀ of 5.15 nM against BTK. BTK-IN-47 inhibits the BTK signaling pathway, induces cell cycle arrest, and activates the canonical Caspase-dependent Apoptotic pathway (promoting the cleavage of Caspase-3, Caspase-7 and PARP), without inducing necroptosis, pyroptosis or ferroptosis. BTK-IN-47 exerts dose-dependent antiproliferative activity against hematologic tumor cell lines. BTK-IN-47 exhibits dose-dependent in vivo antitumor activity in a Ramos cell xenograft model in BALB/c nude mice. BTK-IN-47 can be used for the research of hematologic malignancies.

GFH647 (BTK-IN-33) is a Btk inhibitor with anticancer effects (WO2023174300A1; compound I).

PF-303 is a potent, oral inhibitor of Bruton's tyrosine kinase (BTK) (IC₅₀=0.64 nM). The melamine portion of PF-303 forms a covalent bond with BTK's Cys481, which is reversible and exhibits a high selectivity compared to irreversible covalent BTK inhibitors. PF-303 can be used to model and study the effects of BTK inhibition on the mature immune system, including effects on B-cell subsets, antibody responses, and T-cell-mediated activation.

BTK-IN-40 (compound 375) is a BTK inhibitor.

WS-11 is a non-covalent reversible BTK inhibitor with IC₅₀s of 3.9 nM and 2.2 nM for wild type, C481S mutation BTK, respectively. WS-11 can form strong π-π interaction with PHE540 and form p-π interaction with LYS430 within the active pocket, besides the strong hydrogen bonds.

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.