bmx kinase

BMX-IN-1 (BMX kinase inhibitor) is a selective inhibitor of bone marrow tyrosine kinase on chromosome X (BMX, IC50 = 8 nM) and the related Bruton's tyrosine kinase (BTK, IC50 = 10.4 nM), but BMX-IN-1 is more than 47-656 fold less potent against Blk, JAK3, EGFR, Itk, or Tec activity.

CHMFL-BMX-078 is a highly potent and selective type II irreversible inhibitor of BMX kinase, with an IC50 of 11 nM.

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

CHMFL-EGFR-202 is a potent, irreversible inhibitor of EGFR mutant kinase with IC50 values of 5.3 nM for drug-resistant mutant EGFR T790M and 8.3 nM for WT EGFR kinases.

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].

Rilzabrutinib (PRN1008) is a small-molecule inhibitor and a reversible covalent inhibitor of Bruton's tyrosine kinase (BTK) (IC50 = 1.3 nM), featuring high selectivity, oral activity, and favorable cell permeability, exhibiting anti-inflammatory and immunomodulatory activities.

(Rac)-PF-06250112 is a racemic form of PF-06250112, a potent and highly selective BTK inhibitor that is orally bioavailable; it also inhibits BMX non-receptor tyrosine kinase and TEC [1].

PF-06250112 is an effective and highly selective BTK inhibitor (IC50: 0.5 nM. PF-06250112 displays an inhibitory effect toward BMX nonreceptor tyrosine kinase and TEC (IC50s: 0.9 nM and 1.2 nM, respectively).

PRN694 shows extended target residence time on ITK and RLK, enabling durable attenuation of effector cells in vitro and in vivo. PRN694 is an irreversible, highly selective, and effective covalent interleukin-2-inducible T-cell kinase (ITK) and resting ly

Ibrutinib-biotin, a probe consisting of Ibrutinib linked to biotin via a long-chain linker, has an IC50 of 0.755-1.02 nM for BTK.

IHMT-15130 is a potent and irreversible BMX kinase inhibitor (IC50=1.47 nM). It suppresses the secretion of inflammatory cytokines, obstructs inflammatory signaling pathways, and alleviates angiotensin II-induced myocardial hypertrophy in mice. IHMT-15130 shows potential for research in myocardial hypertrophy.

Poseltinib is an orally active, selective, and irreversible inhibitor of Bruton's tyrosine kinase (BTK), with an IC50 value of 1.95 nM. Poseltinib demonstrates 0.3-, 2.3-, and 2.4-fold higher selectivity for BTK over BMX, TEC, and TXK, respectively. Poseltinib covalently binds to cysteine 481 in BTK’s active site, thereby inhibiting BCR-, FcR-, and TLR-mediated signaling pathways.

BMS-986142 is a potent and highly selective reversible BTK inhibitor (IC50: 0.5 nM).

Aurora kinase inhibitor-3 (Aurora Kinase Inhibitor III) is a potent inhibitor of Aurora A kinase (IC50 = 42 nM).1 It is selective for Aurora A over BMX, BTK, IGF-1R, c-Src, TRKB, SYK, and EGFR.

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.

TAS0728 is a HER2 inhibitor, with antitumor activity

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.