BTK

<p>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.</p>

<p>BMS-935177 is a reversible BTK inhibitor with IC50 value of 3 nM.</p>

<p>WS-11 is a non-covalent reversible inhibitor of BTK, with IC50 values of 3.9 nM for the wild-type and 2.2 nM for the C481S mutant BTK. In addition to strong hydrogen bonding, WS-11 also forms robust π-π interactions with PHE540, and p-π interactions with LYS430 within the active pocket.</p>

<p>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.</p>

<p>JAK3/BTK-IN-4, a dual inhibitor for JAK3/BTK, shows synergy in autoimmune disease treatment. (Patent WO2021147953A1, compound 003)</p>

<p>GNE-431: potent, selective noncovalent Btk inhibitor, IC50=3.2 nM; effective against C481R, T474I, T474M mutants, may counter ibrutinib resistance.</p>

<p>BIIB129 is a selective and brain-penetrant BTK covalent inhibitor used to study B-cell proliferation-related diseases.</p>

<p>BTK-IN-15: Oral BTK inhibitor, IC50 0.7 nM, induces cancer cell apoptosis, selective with anti-tumor effects.</p>

<p>RET-IN-14 inhibits RET (IC50: &lt;0.51-9.3 nM) &amp; BTK (C481S) (IC50: 9.2-15 nM), promising for tumor research.</p>

<p>BMS-986143: oral BTK inhibitor, IC50=0.26 nM, potential for autoimmune research, also targets TEC, BLK, BMX, TXK, YES1, ITK.</p>

<p>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.</p>

<p>BTK inhibitor 18 is a selective, potent, covalent, orally active Btk inhibitor (IC50: 142 nM) that exhibits anti-inflammatory effects.</p>

<p>G-744 is a selective and orally active inhibitor of Btk (IC50: 2 nM).</p>

<p>JAK3/BTK-IN-3: strong dual JAK3/BTK suppressor, promising for autoimmune disease research.</p>

<p>BTK-IN-10 is a potent inhibitor of BTK, acting on wild-type BTK (IC50&lt;5 nM) or mutant BTK (C481S) (IC50&lt;5 nM).</p>

<p>HDHD4-IN-1 (compound 3) is an inhibitor of N-acetylneuraminate-9-phosphate phosphatase (HDHD4) with an IC50 value of 11 μM. It is utilized in the research of neurological disorders.</p>

<p>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].</p>

<p>Brefeldin A 4-O-nicotinate (CHNQD-01228) is a dual inhibitor of Arf1 and BMX proteins with an IC50 value of 0.22 μM for T24 cell proliferation. It also suppresses T24 cell migration and colony formation in a dose-dependent manner, induces G1 phase arrest, and triggers apoptosis. By targeting BMX proteins, it inhibits the AKT/p-AKT and STAT3/p-STAT3 signaling pathways, while also inhibiting Arf1 proteins to eliminate bladder cancer stem cells and activate antitumor immunity, thus exhibiting anticancer activity. Brefeldin A 4-O-nicotinate is applicable in research related to bladder cancer.</p>

<p>BTK-IN-8: potent, selective covalent BTK inhibitor; IC50=0.22 nM, Kd=0.91 nM; effective in blood CD69 cells (IC50=0.029 μM).</p>

<p>BTK-IN-6, a potent BTK inhibitor, may treat immune, cardiac, cancer, viral, inflammatory, metabolic, and neurological disorders.</p>