Btk Inhibitor

BTK-IN-50 is a covalent BTK inhibitor with an IC₅₀ of 6 nM. BTK-IN-50 blocks collagen-induced platelet aggregation by inhibiting the GPVI-mediated BTK-PLCγ2-PKC signaling cascade, and attenuates CRP-XL-induced phosphorylation of BTK, PLCγ2 and PKC substrates in platelets. BTK-IN-50 can be used for research related to thrombosis.

BTK-IN-31 (Compound 2) is a selective, non-covalently reversible, and blood-brain barrier (BBB) permeable Btk inhibitor. BTK-IN-31 has research potential in immune disorders, cancer, cardiovascular disease, viral infections, inflammation, metabolic/endocrine dysfunction, and neurological disorders.

I-As-1 is a potent inhibitor of Bruton’s tyrosine kinase (BTK), with the IC₅₀ of 2.35 nM. I-As-1 shows antiproliferative activities among Ramos cells and OCI-LY10 cells with IC₅₀s of 0.52 μM and 0.11 μM, respectively.

BTK-IN-34 (compound 9h) is a selective BTK inhibitor. BTK-IN-34 shows antiproliferative activity in RAMOS cells through selective inhibition of pBTK (Tyr223) without affecting Lyn and Syk, upstream proteins in the BCR signaling pathway.

Birelentinib (DZD8586) is an orally effective, selective, non-covalent inhibitor targeting LYN tyrosine kinase and BTK tyrosine kinase, capable of penetrating the blood-brain barrier. Birelentinib exhibits concentration-dependent antiproliferative effects in RI-1 cells and diffuse large B-cell lymphoma (DLBCL) cell lines carrying BTK resistance mutations (such as C481X, V416L, etc.). Birelentinib blocks both BTK-dependent and independent signaling of the B-cell receptor (BCR), thereby inhibiting tumor cell proliferation and inducing cell death. Birelentinib can be used in research to overcome resistance to existing covalent and non-covalent BTK inhibitors in B-cell non-Hodgkin lymphoma (B-NHL).

BTK-IN-17 (compound 36R) is a selective and orally activeBTK inhibitor with an IC₅₀ value of 13.7 nM. BTK-IN-17 decreases the expression of p-BTK^Y223 and p-PLCγ2^Y1217. BTK-IN-17 shows anti-inflammatory effects.

BLK-IN-1 (compound 1) is a selective and covalent inhibitor of B-Lymphoid tyrosine kinase (BLK) and BTK, with IC₅₀s of 18.8 nM and 20.5 nM, respectively. BLK-IN-1 can be used for the research of cancer.

Ibt-DOX is a BTK inhibitor with an IC₅₀ of 2.89 nM. Ibt-DOX is also a targeted covalent activated chemotherapeutic agent composed of the targeting ligand Ibrutinib (HY-10997), Doxorubicin (DOX) (HY-15142A), α-MAA (HY-W017180), and a linker (HY-Y0892). Ibt-DOX specifically binds to BTK and releases DOX, synergistically achieving BTK inhibition and chemotherapeutic killing, significantly enhancing toxicity against B-cell lymphoma cells and greatly reducing the toxic side effects of DOX on BTK-negative cells. Ibt-DOX can be used in lymphoma-related research.

HBC-12551 is an orally active BTK inhibitor (IC₅₀ in HEK293 cells: 1.31 nM for BTK; 2.18 nM for BTK^C481S). HBC-12551 has antitumor activity against diffuse large B-cell lymphoma.

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).

JAK3/BTK-IN-2 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-2 has the potential for the research of JAK3 kinase and/or BTK-related diseases (extracted from patent WO2021147952A1, compound 004)

GNE-431 is a potent, selective and noncovalent “pan-BTK” inhibitor against C481R, T474I and T474Ms mutants. GNE-431 shows potency against wild-type BTK (IC₅₀= 3.2 nM) and potency against C481S mutant (IC₅₀= 2.5 nM). GNE-431 is proming for rasearch of haematological disorders and autoimmune diseases.

BTK-IN-21 (Compound 12) is a BTK inhibitor with an IC₅₀ of 33 nM. BTK-IN-21 can be used for research in cancer and autoimmunity therapies.

PDD-87 is an orally active, blood-brain barrier permeable kinase inhibitor, with IC₅₀ values ranging from 0.07 nM to 0.72 nM against ABL, SRC family, BTK kinases and their key mutants. PDD-87 induces antiproliferative effects in leukemia and lymphoma cells, and inhibits tumor growth in mouse xenograft models. PDD-87 can be used for the research of leukemia and lymphoma.

BTK-IN-42 (Compound 11a) is a Btk inhibitor. BTK-IN-42 can effectively inhibit the growth and migration of tumor cells TMD8, with IC₅₀ values of 2.61 and 5.34 μM for TMD8 and T9 cells respectively. It shows promise for research in the field of anti-cancer.

BTK inhibitor 19 is a highly selective, covalent BTK inhibitor (IC₅₀ = 2.7 nM).

BTK-IN-28 (compound PID-4) is a potent BTK inhibitor with anticancer activity. BTK-IN-28 has inhibitory effects on BTK and downstream signaling cascades and selectively inhibits Burkitt lymphoma RAMOS proliferation. BTK-IN-28 has no significant cytotoxicity towards non-tumor cells.

RN941 is a BTK inhibitor. RN941 is applicable to research related to rheumatoid arthritis and B-cell malignancies.

AMX5160 (36) is an orally active BTK inhibitor, with an IC₅₀ of 0.98 nM against mutant BTK^C481S. AMX5160 (36) can be used in the research for leukemia, lymphoma, multiple sclerosis, and other autoimmune diseases.

BTK-IN-7 is a potent and selective inhibitor of BTK (IC₅₀=4.0 nM). BTK-IN-7 has high selectivity in both enzymatic (ITK >250-fold, EGFR >2500-fold) and cellular levels (ITK >227-fold, EGFR 27-fold). BTK-IN-7 also has potent antitumor activity.