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.

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.

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.

JAK3/ BTk-in-1 is a dual JAK3/BTK inhibitor that specifically targets and inhibits Janus kinase 3 (JAK3) and Bruton's tyrosine kinase (BTK), two important targets in autoimmune diseases. JAK3/ BTk-in-1 simultaneously inhibited the BTK/JAK3 signaling pathway, showing a synergistic effect. JAK3/ BTK-in-1 is a potential compound for the treatment of immune-related diseases, such as autoimmune diseases, certain types of cancer (including lymphoma and leukemia), and other diseases that may be characterized by an unbalanced immune response.

BTK inhibitor 17 is a potent irreversible Bruton’s tyrosine kinase (BTK) inhibitor with an IC50 value of 2.1 nM, suitable for use in rheumatoid arthritis studies.

BTK IN-1 [SNS062 analog] is an effective BTK inhibitor with an IC50 of less than 100 nM.

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

JAK3 BTK-IN-5 is a potent inhibitor of JAK3 BTK, crucial targets in autoimmune diseases. Inhibiting the BTK JAK3 signaling pathway simultaneously has a synergistic effect, enhancing its potential research value for JAK3 kinase and or BTK-related diseases.

JAK3 BTK-IN-3 is a potent inhibitor of JAK3 BTK and targets two important pathways in autoimmune diseases. The simultaneous inhibition of the BTK JAK3 signaling pathway exhibits a synergistic effect, highlighting JAK3 BTK-IN-3's potential for investigating JAK3 kinases and or BTK-related diseases.

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].

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].

BTK inhibitor 19 is a highly selective, covalent BTK inhibitor (IC 50 = 2.7 nM).

JAK3 BTK-IN-4 is a potent inhibitor of JAK3 BTK, targeting critical pathways in autoimmune diseases. The simultaneous inhibition of the BTK JAK3 signaling pathway exerts a synergistic effect, making JAK3 BTK-IN-4 a promising therapeutic candidate for JAK3 kinase and or BTK-related diseases.

BTK-IN-8 is a potent, selective, peripheral covalent BTK inhibitor with an IC50 value of 0.22 nM and a Kd value of 0.91 nM. BTK-IN-8 exhibits good potency in whole blood CD69 cells with an IC50 value of 0.029 μM.

BTK inhibitor 10 is a potent and orally active compound with potential applications in rheumatoid arthritis treatment.

BTK-IN-10 is a potent inhibitor of BTK, effective against both wild-type BTK (IC50<5 nM) and mutant BTK (C481S) (IC50<5 nM).

BTK-IN-15 is a novel, orally active Bruton's tyrosine kinase (BTK) inhibitor that inhibits BTK (IC50: 0.7 nM). BTK-IN-15 induces apoptosis in cancer cells and has good kinase selectivity and anti-tumour activity.

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].

BTK-IN-6 is a potent inhibitor of Bruton's tyrosine kinase (BTK) with research potential in immune diseases, cardiovascular diseases, cancer, viral infections, inflammation, metabolic endocrine dysfunction, and neurological disorders (for more information).

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.

BTK-IN-18 is a potent, reversible inhibitor of Bruton's tyrosine kinase (BTK) with an IC50 of 0.002 µM, and it effectively suppresses CD69 and CD86 expression in vivo.

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

Btk inhibitor 1 Hcl is a pyrazolo[3,4-d]pyrimidine derivative as a Btk kinase inhibitor.IC50 value:Target: BtkFrom PCT Int. Appl. (2012), WO 2012158843 A2 20121122. [1]. PCT Int. Appl. (2012), WO 2012158843 A2 20121122.

CHMFL-BTK-01 is an irreversible inhibitor of BTK (IC50: 7 nM) and also potently inhibits BTK Y223 auto-phosphorylation.

BTK-IN-11 is a potent BTK inhibitor with potential applications in research on autoimmune diseases, inflammatory diseases, and cancer.

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.

PROTAC BTK Degrader-3 is a potent degrader of Bruton's tyrosine kinase (BTK), with a DC50 (median degradation concentration) of 10.9 nM in Mino cells, and shows promise for research into B-cell malignancies, such as chronic lymphoid malignancies [1].

BTK-IN-22, a BTK inhibitor (IC 50: 0.9 nM), also exhibits inhibition against BLX and BMX with IC 50 values of 1.4 and 1.2 nM, respectively. Demonstrating enhanced kinase selectivity, BTK-IN-22 outperforms Ibrutinib in this regard [1].

BTK-IN-23 is a BTK inhibitor with an IC50 value of 12.8 nM, demonstrating kinase selectivity superior to Ibrutinib [1]. It effectively inhibits BLX and BMX, with IC50 values of 35.6 nM and 5.7 nM, respectively.

PROTAC BTK Degrader-1, a powerful, selective, and orally bioavailable degrader of PROTAC BTK, demonstrates effective reduction in BTK protein levels and tumor suppression. It exhibits IC50 values of 34.51 nM for BTK WT and 64.56 nM for BTK-481S, highlighting its potency and efficacy in targeting and diminishing BTK protein abundance [1].

BTK-IN-7 is a selective and potent BTK inhibitor with an IC50 value of 4.0 nM. BTK-IN-7 exhibits high selectivity at both the enzymatic (ITK>250-fold, EGFR>2500-fold) and cellular levels (ITK>227-fold, EGFR27-fold). BTK-IN-7 exhibits high high antitumor effect.

BTK inhibitor 20 is a potent BTK inhibitor with an IC [50 ] of 8 nM.

PROTAC BTK Degrader-2, a potent degrader of BTK through the PROTAC mechanism, effectively diminishes BTK protein levels [1].

BTK-IN-24 (compound 195) is a potent BTK inhibitor via a ubiquitin proteolytic pathway [1] .

BTK-IN-5, a covalent inhibitor of Bruton's tyrosine kinase (BTK), is designed for treating cardiovascular diseases, respiratory diseases, inflammation, and diabetes.

JAK3/BTK-IN-6 is a potent dual inhibitor of BTK (IC50: 0.6 nM) and JAK3 (IC50: 0.4 nM).JAK3/BTK-IN-6 exhibits good metabolic stability in human liver microsomes.JAK3/BTK-IN-6 can be used to study blood and immune diseases.

BTK-IN-9 is a reversible inhibitor of BTK that exhibits potent anti-proliferative effects in condyloma cells. It specifically disrupts mitochondrial membrane potential, elevates reactive oxygen species levels in Z138 cells, and induces apoptosis in Z138 cells.

BTK-IN-19 is a reversible BTK inhibitor with an IC 50 of <0.001 μM .

BTK inhibitor 13 (compound 8) is a potent and selective BTK inhibitor with an IC50 of 1.2 nM.

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

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

1,2-Bis(2-iodoethoxy)ethane is a PEG-based PROTAC linker used in the synthesis of MT802 and SJF620, which are potent PROTAC BTK degraders with DC50s of 1 nM and 7.9 nM, respectively [1].