bcr-abl-in-1

BCR-ABL-IN-1 is a BCR-ABL tyrosine kinase inhibitor (pIC50: 6.46) and may be used in the research of chronic myelogenous leukemia.

cSRC BCR-ABL-IN-1 (compound 21b) is a potent inhibitor of Bcr-Abl and C-Src, with IC50 values of 56.2 nM and 101 nM, respectively. It exhibits cytotoxicity.

BCR-ABL-IN-10 (compound B4) is a covalent BCR-ABL inhibitor featuring an arylvinylsulfonate (AVS) moiety, demonstrating an IC50 of 43.1 nM against ABL kinase. It forms a covalent and stable adduct with ABL kinase, enabling the sustained inhibition of intrinsic BCR-ABL activity. This compound is utilized in the study of chronic myeloid leukemia (CML).

BCR-ABL-IN-11 (Compound 2) is an inhibitor of BCR-ABL, exhibiting anticancer activity against chronic myelogenous leukemia (CML) with an IC50 value of 129.61 μM in K562 cells.

1. trans-Cinnamaldehyde (Phenylacrolein) exhibits excellent anti-inflammatory activities and antidepressant-like effects in stressed mid-aged rats as a COX-2 inhibitor. 2. Cinnamic aldehyde induces apoptosis of CML cells in vitro, down-regulation of the expression and function of BCR-ABL may be one of its most important anti-leukemia mechanisms. 3. Cinnamic aldehyde and cinnamic acid are cardioprotective in a rat model of ischemic myocardial injury, the mechanism is related to anti-oxidative and anti-inflammatory properties.

Lyn-IN-1 (Bafetinib analog) is a selective, potent dual inhibitor of Bcr-Abl and Lyn.

Mcl1-IN-9 is a potent myeloid cell leukemia-1 (Mcl-1) inhibitor, exhibiting an IC50 of 446 nM in reengineered BCR-ABL+ B-ALL cells and a Ki of 0.03 nM.

SNIPER(ABL)-050 is a chemical compound that combines Imatinib, an ABL inhibitor, with MV-1, an IAP ligand, using a linker. This conjugation results in the reduction of BCR-ABL protein[1].

Tyrphostin AG957, a tyrosine kinase inhibitor with anti-BCR ABL tyrosine kinase activity restores beta1 integrin-mediated adhesion and inhibitory signaling in chronic myelogenous leukemia hematopoietic progenitors[1].

BCR-ABL1-IN-1 is a highly potent, orally bioavailable inhibitor with remarkable specificity towards ABL kinase, showing significant promise for elucidating the precise role of ABL kinases in the central nervous system, particularly in preclinical investigations [1].

AKI603 is a novel small molecule inhibitor of Aurora kinase A (AurA)(IC50 = 12.3 nM). AKI603 is developed to overcome resistance mediated by BCR-ABL-T315I mutation. AKI603 exhibits strong anti-proliferative activity in leukemic cells[1][2].

BVB-808 is a selective Jak2 type 1 inhibitor. Janus kinases are critical components of signaling pathways that regulate hematopoiesis. Mutations of the non-receptor tyrosine kinase JAK2 are found in many BCR-ABL-negative myeloproliferative neoplasms. Preclinical results support that JAK2 inhibitors could show efficacy in treating chronic myeloproliferative neoplasms. JAK2 has also been postulated to play a role in BCR-ABL signal transduction. Therefore, inhibitors of JAK2 kinases are turning into therapeutic strategies for treatment of chronic myelogenous leukemia (CML).

Imatinib Impurity E is a specific impurity found in Imatinib, an orally available inhibitor of multiple tyrosine kinases, including BCR ABL, v-Abl, PDGFR, and c-kit. Imatinib (STI571) operates by semi-competitively inhibiting enzyme activity; it binds adjacent to the ATP binding site, inducing a closed or self-inhibited conformation [1] [2] [3] [4]. Additionally, Imatinib acts as an inhibitor against SARS-CoV and MERS-CoV [5].

SIAIS100, a potent BCR-ABL PROTAC degrader, demonstrates a DC50 value of 2.7 nM, highlighting its efficacy. It is primarily utilized in the investigation of chronic myeloid leukemia (CML) [1].

SIAIS100 TFA is a potent BCR-ABL PROTAC degrader with a DC50 of 2.7 nM, used in chronic myeloid leukemia (CML) research [1].

PROTAC BCR-ABL Degrader-1 (compound PROTAC 1), featuring a 2-oxoethyl linker, induces Bcr-Abl degradation via the ubiquitin-proteasome pathway and exhibits antiproliferative effects on K562 cells, indicating its potential in cancer research [1].

ML 2-23 is a potent BCR-ABL degrader functioning as a PROTAC, demonstrating selective proteasome-dependent degradation of BCR-ABL in leukemia cells [1].

BCR-ABL-IN-8 (compound 26f) is a BCR-ABL inhibitor characterized by a trimethoxy group [1].

BCR-ABL kinase-IN-3 (example 1), a potent BCR-ABL inhibitor, is significant in the study of acute myeloid leukemia (AML) [1].

GNF-6 (Compound 14), an ATP competitive inhibitor, inhibits the gatekeeper threonine residue mutation of BCR-ABL-T315I with IC50 values of 0.25 μM for c-ABL-T334I, 0.09 μM for BCR-ABL, and 0.590 μM for BCR-ABL-T315I variants. It disrupts the assembly of the hydrophobic spine (a network of hydrophobic interactions), locking the kinase in an inactive 'DFG-out' conformation [1].