Bcr-Abl
Bcr-Abl tyrosine-kinase inhibitors (TKI) are the first-line therapy for most patients with chronic myelogenous leukemia (CML). More than 90% of CML cases are caused by a chromosomal abnormality that results in the formation of a so-called Philadelphia chromosome. This abnormality is a consequence of fusion between the Abelson (Abl) tyrosine kinase gene at chromosome 9 and the break point cluster (Bcr) gene at chromosome 22, resulting in a chimeric oncogene (Bcr-Abl) and a constitutively active Bcr-Abl tyrosine kinase that has been implicated in the pathogenesis of CML. Compounds have been developed to selectively inhibit the tyrosine kinase.
Bcr-Abl Isoform Specific Products
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Bcr-Abl Inhibitors
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ABL1 Proteins
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Bcr-Abl Related Products (249)
Related Products (249)
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Recombinant Proteins (7)
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Antibodies (6)
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Bcr-Abl Isoform Comparison
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c-ABL-IN-4
0 ImagesCat. No.: HY-146530CAS No.: 2626934-68-5c-ABL-IN-4 is a potent inhibitor of c-Abl. Activation of c-Abl has been implicated in various diseases, notably cancer. c-ABL-IN-4 has the potential for the research of neurodegenerative diseases (amyotrophic lateral sclerosis (ALS) and Parkinson’s disease (PD) and cancer (extracted from patent WO2021048567A1, compound 54).
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BCR-ABL-IN-4
0 ImagesCat. No.: HY-142922CAS No.: 2669790-59-2BCR-ABL-IN-4 is a BCR-ABL inhibitor with anticancer effects. BCR-ABL-IN-4 inhibits the cancer cell growth with IC50 values of 0.67 nM and 16 nM for K562 cells and BCR-ABL T315I transfected Ba/F3 cells, respectively (WO2021143927A1; compound 11).
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BRAFV600E/ABL2-IN-1
0 ImagesCat. No.: HY-178382BRAFV600E/ABL2-IN-1 is a BRAFV600E (IC50 = 0.088 μM)/ABL2 (IC50 = 0.3 μM) dual inhibitor. BRAFV600E/ABL2-IN-1 can diminish P-glycoprotein expression. BRAFV600E/ABL2-IN-1 effectively inhibits p-CrkL (Abl2 signaling) and p-ERK1/2 (BRAFV600E pathway) in A375-R melanoma cells. BRAFV600E/ABL2-IN-1 causes cell cycle arrest. BRAFV600E/ABL2-IN-1 significantly increases the percentage of late apoptotic cells. BRAFV600E/ABL2-IN-1 can be used for the study of melanoma.
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GNF-6
0 ImagesCat. No.: HY-160478CAS No.: 839708-29-1GNF-6 (Compound 14) inhibits the gatekeeper threonine residue mutation of BCR-ABL-T315I with IC50s of 0.25 μM, 0.09 μM and 0.590 μM for c-ABL-T334I, BCR-ABL and BCR-ABL-T315I variants, respectively. GNF-6, an ATP competitive inhibitor, disrupts the assembly of the hydrophobic spine (a network of hydrophobic interactions), thereby locking the kinase in an inactive ‘DFG-out’ conformation.
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Azo-PROTAC-4C-trans
0 ImagesCat. No.: HY-180983Azo-PROTAC-4C-trans is a BCR-ABL PROTAC degrader that can efficiently degrade the BCR-ABL fusion protein and ABL protein. Azo-PROTAC-4C-trans exhibits potent selective anti-proliferative activity against K562 cells. Azo-PROTAC-4C-trans allows real-time, reversible regulation of its activity via UV (to inactivate it) /visible light (to activate it) irradiation. Azo-PROTAC-4C-trans can be used for the study of myeloid leukemia.
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c-ABL-IN-5
0 ImagesCat. No.: HY-156102CAS No.: 3056613-20-5c-ABL-IN-5 is a selective c-Abl inhibitor with neuroprotective effects. c-ABL-IN-5 has blood-brain barrier penetrability, metabolic stability and good pharmacokinetic properties. When c-ABL-IN-5 is labeled with [18F] (compound [18F]3), it can be used as a tracer to evaluate disease-modifying efficacy by complementary positron emission tomography (PET). c-ABL-IN-5 can be used in the study of neurodegenerative diseases such as Parkinson's disease (PD).
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Nilotinib-13C,d3
0 ImagesCat. No.: HY-10159S1CAS No.: 1261398-62-2Synonyms: AMN107-13C,d3Nilotinib-13C,d3 is a deuterated labeled Nilotinib. Nilotinib is an orally available Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity.
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MRLB-223
0 ImagesCat. No.: HY-124792CAS No.: 937727-03-2MRLB-223 is a preferential HDAC1 and HDAC2 inhibitor with activity against tumor cells.MRLB-223 induces histone hyperacetylation, intrinsic apoptotic pathway activation, tumor cell apoptosis, Hsp90 hyperacetylation, and caspase-dependent Bcr-Abl degradation.MRLB-223 mediates p53-independent tumor cell death, with activity suppressed by Bcl-2 overexpression, and kills Bcr-Abl-expressing myeloid cells.MRLB-223 exerts effects in mice bearing Eμ-myc lymphomas.MRLB-223 can be used for the research of Eμ-myc lymphoma.
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Dasatinib monohydrate (Standard)
0 ImagesCat. No.: HY-10181BRCAS No.: 863127-77-9Synonyms: BMS-354825 monohydrate (Standard)Dasatinib (monohydrate) (Standard) is the analytical standard of Dasatinib (monohydrate). This product is intended for research and analytical applications. Dasatinib (BMS-354825) monohydrate is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib monohydrate inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively. Dasatinib monohydrate also induces apoptosis and autophagy.
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c-ABL-IN-6
0 ImagesCat. No.: HY-163189c-ABL-IN-6 (compound A6) is a c-ABL inhibitor with IC50 value of 16.6 nM. c-ABL-IN-6 displays higher neuroprotective effects against SH-SY5Y cell death induced by MPP+ (HY-W008719). c-ABL-IN-6 can be used for the research of neurodegenerative disorder.
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ML 2-23
0 ImagesCat. No.: HY-153582ML 2-23 is a PROTAC degrader that recruits RNF114 to target BCR-ABL/c-ABL for degradation. ML 2-23 promotes proteasome-dependent degradation of the target protein and inhibits phosphorylation of downstream CRKL. At concentrations used for BCR-ABL degradation, ML 2-23 only causes slight impairment to the viability of cancer cells. ML 2-23 can be used in the research of chronic myeloid leukemia.
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Phe-PEG1-Dasa
0 ImagesCat. No.: HY-180962CAS No.: 3037776-73-8Phe-PEG1-Dasa is a BCR-ABL PROTAC degrader, with its DC50 being 1.56 nM. Phe-PEG1-Dasa uses a single amino acid (Phe) as the E3 ligand and employs the N-end rule pathway to induce the degradation of the target protein, significantly reducing the molecular size, thus being called a mini-PROTAC. Phe-PEG1-Dasa significantly inhibits the proliferation of K562 cells. Phe-PEG1-Dasa can be used for the study of leukemia.
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IHMT-TRK-284
0 ImagesCat. No.: HY-146697CAS No.: 2416844-79-4
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SNIPER(ABL)-039
0 ImagesCat. No.: HY-111874CAS No.: 2222354-29-0SNIPER(ABL)-039, conjugating Dasatinib (ABL inhibitor) to LCL161 derivative (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 10 nM. IC50s are 0.54 nM, 10 nM, 12 nM, and 50 nM for ABL, cIAP1, cIAP2, XIAP, respectively.
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PonatiLink-1-24
0 ImagesCat. No.: HY-155290CAS No.: 2941512-45-2PonatiLink-1-24 is an Abelson murine leukemia (ABL) enzyme inhibitor.
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ABL1 E255K Recombinant Human Active Protein Kinase
0 ImagesCat. No.: HY-E70634The emergence of mutations in the BCR::ABL1 kinase domain (KD) impairs Imatinib Mesylate (HY-50946) binding capacity, thus contributing to Imatinib Mesylate resistance. Identification of these mutations is important for treatment decisions and precision medicine in chronic myeloid leukaemia (CML). ABL1 E255K Recombinant Human Active Protein Kinase is a recombinant ABL1 E255K protein that can be used to study ABL1 E255K-related functions.
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Radotinib dihydrochloride
0 ImagesCat. No.: HY-179460CAS No.: 926037-85-6Synonyms: IY-5511 dihydrochlorideRadotinib (IY-5511) dihydrochloride is an orally active and BBB-permeable selective tyrosine kinase Bcr-Abl1 inhibitor with an IC50 of 34 nM. Radotinib dihydrochloride has anti-prion and anti-tumor activities. Radotinib dihydrochloride can inhibit the proliferation, induce cell cycle arrest and apoptosis of tumor cells . Radotinib dihydrochloride can be used in the research of cancer such as chronic myeloid leukemia and multiple myeloma, as well as neurodegenerative diseases such as prion diseases.
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Multi-kinase-IN-14
0 ImagesCat. No.: HY-181046CAS No.: 2201083-51-2Multi-kinase-IN-14 is an orally active and blood-brain barrier-permeable multi-kinase inhibitor. Multi-kinase-IN-14 reduces the excessive phosphorylation of α-synuclein by inhibiting four kinases (ABL1, DYRK1A, GSK3β, and LRRK2) and stabilizing microtubules. Multi-kinase-IN-14 is applicable for research on neurodegenerative diseases such as Parkinson’s disease and Alzheimer’s disease.
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AP-24226
0 ImagesCat. No.: HY-14142CAS No.: 926922-22-7AP-24226 is a potent inhibitor of Scr/ABL.
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Tyrosine kinase-IN-9
0 ImagesCat. No.: HY-W839261CAS No.: 370854-75-4Tyrosine kinase-IN-9 (Compound B) is the inhibitor for c-Abl. Tyrosine kinase-IN-9 can be used in research of neurodegenerative diseases including Alzheimer’s and Parkinson’s disease.
