btk

BTK-IN-16 is a potential inhibitor of wild-type BTK and C481S mutants.BTK-IN-16 can be used to study various autoimmune diseases and cancers caused by BTK.

Ibrutinib (PCI-32765) is an irreversible inhibitor of BTK (IC50: 0.5 nM) that selectively blocks B cell activation.

Remibrutinib inhibits BTK activity with an IC50 value of 0.023 μM in blood. Remibrutinib is an effective and orally active Bruton tyrosine kinase inhibitor (IC50: 1 nM). Remibrutinib has the potential for Chronic urticaria (CU) treatment.

Avitinib (AC0010), also known as AC0010 or AC0010MA, is an orally available, irreversible, epidermal growth factor receptor (EGFR) mutant-selective inhibitor, with potential antineoplastic activity. Upon oral administration, avitinib covalently binds to and inhibits the activity of mutant forms of EGFR, including the drug-resistant T790M EGFR mutant, which prevents signaling mediated by mutant forms of EGFR. This may both induce cell death and inhibit tumor growth in EGFR-mutated tumor cells. EGFR, a receptor tyrosine kinase that is mutated in a variety of Ys, plays a key role in tumor cell proliferation and tumor vascularization. As this agent is selective towards mutant forms of EGFR, its toxicity profile may be reduced when compared to non-selective EGFR inhibitors, which also inhibit wild-type EGFR.

BTK-IN-25 (compound 71) is a potent BTK inhibitor with an IC50 of 0.77 nM against BTK(C481S) and an IC50 of 1 nM in DOHH2 cells [1].

PROTAC BTK Degrader-6 (Compound 15), with a DC50 of 3.18 nM, exhibits anti-inflammatory properties by inhibiting NF-κB activation and suppressing the expression of pro-inflammatory cytokines such as IL-1β and IL-6 [1].

Spleen tyrosine kinase (Syk) is a non-receptor tyrosine kinase that, upon phosphorylation, binds to immunoreceptor tyrosine-based activation motifs of FcRγ chains and mediates downstream signaling related to platelet function and inflammation. Syk inhibit

BTK-IN-40 (compound 375) is an inhibitor of BTK.

Tirabrutinib hydrochloride is a potent, highly selective, and irreversible oral BTK inhibitor. Tirabrutinib hydrochloride irreversibly covalently binds to Bruton tyrosine kinase (BTK) in B cells and exhibits potent in vitro cytotoxicity against many types of B cell malignancies, as well as in vivo antitumor activity in mouse models [1].

PROTAC BTK Degrader-10 (Example 1P) is a PROTAC compound that targets BTK for degradation. It is applicable in the research of chronic lymphocytic leukemia (CLL). [Pink: ligand for target protein; Black: linker; Blue: ligand for E3 ligase Cereblon].

PROTAC BTK Degrader-12 (EXAMPLE 19) is a PROTAC-based BTK degrader, featuring a structure where the BTK ligand and linker are highlighted in pink and black, the linker in black, and the VHL ligand in blue.

BTK-IN-27 (example 8), a potent BTK inhibitor with an IC50 of 0.2 nM, demonstrates anti-proliferative effects in TMD8 cells with an IC50 of less than 5 nM. It is suitable for the research of various conditions including cancer, lymphoma, leukemia, and immunological diseases [1].

Olmutinib (HM61713, BI 1482694) is an orally available small molecule, a mutant-selective inhibitor of epidermal growth factor receptor (EGFR) with potential antineoplastic activity. Olmutinib binds to and inhibits mutant forms of EGFR, thereby leading to cell death of EGFR-expressing tumor cells. As this agent is selective towards mutant forms of EGFR, its toxicity profile may be reduced as compared to non-selective EGFR inhibitors which also inhibit the EGFR wild-type form.

Larotinib is an orally active, potent, and broad-spectrum tyrosine kinase inhibitor (TKI) with an IC50 of 0.6 nM for EGFR.

Rilzabrutinib (PRN1008) is a reversible covalent, selective, and orally active inhibitor of Bruton's Tyrosine Kinase (BTK) with an IC50 of 1.3 nM.

PROTAC BTK Degrader-13 (Compound 25) is a targeted BTK PROTAC degrader with a DC50 of 0.27 μM. It inhibits BTK activity with an IC50 of 0.44 μM and suppresses IL-2-induced T cell kinase (ITK) with an IC50 of 2.16 μM. This compound also inhibits the p38 MAPK signaling pathway, thereby blocking the activation of the BCR (B cell receptor) signaling pathway. [Pink: ligand for target protein BTK ligand 15; Black: linker; Blue: ligand for E3 ligase cereblon]

ARQ-531 is a potent and orally active BTK inhibitor with potential antineoplastic activity, with IC50s of 0.85 nM and 0.39 nM for WT-BTK and C481S-BTK, respectively.

Zanubrutinib (BGB-3111) is an inhibitor of Bruton tyrosine kinase (BTK).

PROTAC BTK Degraders-5 (Compound 3e) is a selective Bruton's tyrosine kinase (BTK) degrader with a DC50 of 7.0 nM in JeKo-1 cells, demonstrating specificity by not affecting CRBN neosubstrates. It also exhibits antiproliferative effects on various lymphoma cell lines, underscoring its potential application in chronic lymphoid malignancies research.

Sunvozertinib (DZD9008) is a potent ErbBs and BTK inhibitor, with inhibitory effects on EGFR, Her2, and mutant epidermal growth factor. Sunvozertinib (DZD9008) showed inhibitory effects on EGFR exon 20 NPH insertion, EGFR exon 20 ASV insertion, EGFR L858R and T790M mutations, as well as Her2 exon 20 YVMA and EGFR WT A431 with IC50 of 20.4, 20.4, 1.1, 7.5, and 80.4 nM.

Tirabrutinib (GS-4059) (ONO-4059) is an orally active Bruton's Tyrosine Kinase (Btk) inhibitor (can cross the blood-brain barrier (BBB)), with an IC50 of 6.8 nM. Tirabrutinib irreversibly and covalently binds to Btk and inhibits aberrant B cell receptor signaling. Tirabrutinib can be used in studies of autoimmune diseases and hematological malignancies.

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

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.

Edralbrutinib (TG-1701) is a potent BTK inhibitor with anticancer activity used in treating tumors, immune system disorders, and blood and lymphatic system disorders. Additionally, Edralbrutinib is studied for its efficacy in membranous glomerulonephritis and optic neuromyelitis optica.