Btk inhibitor-2

Btk Inhibitor 2 (BGB-3111 analog) is a BTK inhibitor.

BTK inhibitor 1 (Compound 27) is a BTK inhibitor (IC50: 0.11 nM) with an inhibitory effect on B-cell activation in hWB with an IC50 of 2 nM.

QL-X-138 is a potent and selective BTK and MNK dual kinase inhibitor that binds covalently to BTK and non-covalently to MNK. The IC50 values of QL-X-138 are 9.4 nM for BTK, 107.4 nM for MNK1, 26 nM for MNK2, and 3.5 μM against Dengue 2. QL-X-138 is used in the study of B-cell malignancies and B-cell malignant tumors.

QL-X-138 HCl is a novel selective and highly potent BTK MNK dual-kinase inhibitor with anticancer activity that binds covalently to BTK and noncovalently to MNK. QL-X-138 HCl inhibited BTK, MNK1, and MNK2 kinases. QL-X-138 HCl has anti-dengue virus 2 activity and shows anti-proliferative activity in acute myeloid leukemia cells. QL-X-138 HCl can be used to study lymphoma and leukemia.

JAK3 BTk-in-2 is a potent JAK3 BTK inhibitor. JAK3 BTk-in-2 inhibits both BTK and JAK3, which are two important targets IN autoimmune diseases. JAK3 BTk-in-2 simultaneously inhibits the BTK JAK3 signaling pathway, showing a synergistic effect. JAK3 BTk-in-2 has the potential to treat diseases associated with abnormal JAK3 and BTK activity.

G-744 is a selective and orally active inhibitor of Btk (IC50: 2 nM). G-744 is well-tolerated, metabolically stable. It also has an efficacious to treat arthritis.

Lck inhibitor 2 is a bis-anilinopyrimidine inhibitor of tyrosine kinases including LCK, BTK, LYN, SYK, and TXK [IC50s: 13nM, 9nM, 3nM, 26nM, and 2nM for Lck, Btk, Lyn, Btk, and Txk respectively].

Luxeptinib (CG-806) is a novel pan-FLT3 pan-BTK inhibitor that is administered orally. It exhibits potent and reversible inhibition of these enzymes, acting through a non-covalent mechanism. Luxeptinib effectively induces cell cycle arrest, apoptosis, or autophagy in acute myeloid leukemia cells [1][2][3][4].

BAY 61-3606 (Syk inhibitor IV) is a potent, ATP-competitive, reversible, and highly selective inhibitor of Syk tyrosine kinase activity (Ki= 7.5 nM), exhibiting no inhibitory effect against Btk, Fyn, Itk, Lyn, and Src.

ITK inhibitor 6 is a selective and potent ITK inhibitor that acts on ITK (IC50: 4 nM), BTK (IC50: 133 nM), JAK3 (IC50: 320 nM), EGFR (IC50: 2360 nM), LCK (IC50: 155 nM). ITK inhibitor 6 inhibited the phosphorylation of PLCγ1 and ERK1 2 and showed anti-proliferative effect.

BTK-IN-17 is a selective, orally active inhibitor of Bruton's Tyrosine Kinase (BTK) with an inhibition concentration (IC50) value of 13.7 nM. It effectively reduces the expression of phosphorylated BTK at Tyrosine 223 (p-BTK Y223) and phosphorylated Phospholipase C Gamma 2 at Tyrosine 1217 (p-PLCγ2 Y1217), demonstrating anti-inflammatory properties.

BLK-IN-2 is a potent, selective, and irreversible inhibitor of B-Lymphoid tyrosine kinase (BLK), demonstrating significant efficacy with an IC50 of 5.9 nM. Additionally, it exhibits an inhibitory effect on BTK (Bruton's tyrosine kinase) with an IC50 of 202.0 nM. This compound has shown strong antiproliferative activities against various lymphoma cells.

NX-2127 (ETX2514 Triethylamine) is an orally active BTK inhibitor that induces degradation of mutant BTKC481S in cells.NX-2127 has potent antiproliferative activity and inhibits the proliferation of BTKC481S mutant TMD8 cells.NX-2127 potently catalyzes the degradation of Ikaros (IKZF1) and Aiolos (IKZF3) at 25 nM and 54 nM, respectively. NX-2127 is associated with the immune system, stimulating T cell activation and increasing IL-2 production in primary human T cells.

(Rac)-IBT6A hydrochloride is a racemic mixture of IBT6A hydrochloride, an impurity of Ibrutinib, involved in the synthesis of IBT6A Ibrutinib dimer and IBT6A adduct [1]. IBT6A is related to Ibrutinib, a selective and irreversible Bruton's tyrosine kinase (Btk) inhibitor with an IC50 of 0.5 nM [2].

CYY292 is a chemical compound acting as an inhibitor of PDGFRα, PDGFRβ, FGFR1, -2, and -3, with respective IC50 values of 5.35, 4.6, 28, 28, and 78 nM. It exhibits selectivity over FGFR4 (IC50 > 1,000 nM) while also targeting c-Kit, VEGFR2, VEGFR1, and IGF-1R (IC50 values of 67, 33, 36, and 75 nM, respectively). Additionally, CYY292 inhibits EGFR, BTK, Cdk4/cyclin D3, and MET with IC50 values of 128, 198, 214, and 396 nM, respectively. This compound demonstrates efficacy in arresting the proliferation of various osteosarcoma cell lines—MG-63, U2OS, MNNG/HOS, and Saos-2—with IC50s ranging from 0.72 to 1.36 µM. Moreover, CYY292 at 0.3 and 0.5 µM concentrations inhibits migration and invasion in glioblastoma cells (U87MG and LN-229) and, at a dose of 30 mg/kg, decreases tumor volume and enhances survival in a U87MG orthotopic mouse xenograft model.

BTK-IN-31 (Compound 2), a selective and non-covalently reversible Btk inhibitor, is permeable to the blood-brain barrier (BBB). This compound shows research potential for treating a variety of conditions, including immune disorders, cancer, cardiovascular disease, viral infections, inflammation, metabolic endocrine dysfunction, and neurological disorders [1].

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].

KIN-8194 is a dual inhibitor of HCK and BTK, effective when administered orally, displaying IC 50 values of 0.915 nM for HCK and <0.495 nM for BTK. It inhibits growth and disrupts integrin-mediated adhesion in BTKi-resistant mantle cell lymphoma (MCL). Additionally, KIN-8194 has shown efficacy in overcoming ibrutinib resistance, enhancing survival in TMD-8 ABC DLBCL xenografted mice [1] [2].

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

(S)-Sunvozertinib (DZD9008) is a rationally designed selective, irreversible EGFR HER2 inhibitor.