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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Bcr-Abl Antagonist
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Bcr-Abl Activator
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Bcr-Abl Degraders
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ABL1 Proteins
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Bcr-Abl Related Products (257)
Related Products (257)
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Recombinant Proteins (8)
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Antibodies (6)
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Bcr-Abl Isoform Comparison
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Relcobatinib
0 ImagesCat. No.: HY-184100SCAS No.: 2767305-95-1Synonyms: RelcobatinibumRelcobatinib (Relcobatinibum) is a ABL1 kinase inhibitor with an IC50 of 12.7 nM against wild-type ABL1 and an IC50 of 43.5 nM against the ABL1T315I mutant. Relcobatinib inhibits the phosphorylation of CRKL. Relcobatinib exhibits anticancer activity against chronic myeloid leukemia. Relcobatinib can be used in studies related to chronic myeloid leukemia.
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SNIPER(ABL)-058
0 ImagesCat. No.: HY-111859CAS No.: 2222354-61-0SNIPER(ABL)-058, conjugating Imatinib (ABL inhibitor) to LCL161 derivative (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 10 μM.
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c-ABL-IN-1
0 ImagesCat. No.: HY-139730CAS No.: 2304918-82-7c-ABL-IN-1 is a novel selective c-Abl inhibitor that prevents neurodegeneration in parkinson’s disease.
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ABL1 Q252H Recombinant Human Active Protein Kinase
0 ImagesCat. No.: HY-E70639The 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 Q252H Recombinant Human Active Protein Kinase is a recombinant ABL1 Q252H protein that can be used to study ABL1 Q252H-related functions.
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EphB4-IN-1
0 ImagesCat. No.: HY-185227CAS No.: 1394837-94-5EphB4-IN-1 is a selective EphB4 tyrosine kinase inhibitor with IC50 values of 0.16-0.30 μM. EphB4-IN-1 binds to the ATP binding site of EphB4 in a DFG-in conformation, forming four stable intermolecular hydrogen bonds. EphB4-IN-1 also inhibits Src, Abl1, Lck, and EGFR kinases. EphB4-IN-1 inhibits EphB4 autophosphorylation. EphB4-IN-1 can be used for the research of cancer, such as non small cell lung cancer.
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EAPB0503
0 ImagesCat. No.: HY-171184CAS No.: 1140627-77-5EAPB0503 is a quinoline compound with anti-tumor activity, showing strong cytotoxicity against melanoma cells in vitro (IC50=200 nM). EAPB0503 can induce specific cell cycle arrest in mitosis of CML cells and directly activate apoptosis, leading to an increase in the G0 cell population, disruption of mitochondrial membrane potential, PARP cleavage, and DNA fragmentation. EAPB0503 also reduces the levels of BCR-ABL protein .
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AP 24149
0 ImagesCat. No.: HY-10363CAS No.: 926922-29-4
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IM-12 (GMP)
0 ImagesCat. No.: HY-12292GCAS No.: 1129669-05-1IM-12 GMP is IM-12 (HY-12292) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. IM-12 is an orally active anti-inflammatory agent that targets and inhibits the NF-κB and STAT3 signaling pathways. IM-12 activates the Wnt signaling pathway and promotes the nuclear translocation of β-catenin by inhibiting GSK3β, while also blocking the tyrosine kinase activity of p210BCR/ABL. IM-12 reduces the levels of IL-6, IL-17, NO, prostaglandin E2, iNOS and COX-2, and induces ER stress, Ca2+ release, autophagy and apoptosis. IM-12 is heat-sensitive and does not induce autophagy in IM-resistant p210BCR/ABLT315I mutant cells. IM-12 is also a component of the 5iLA medium used for naive pluripotent stem cell research. IM-12 has been applied in studies related to carrageenan (HY-125474)-induced hind paw edema, TNBS-induced colitis, and acute and chronic myeloid leukemia.
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DosatiLink-1
0 ImagesCat. No.: HY-155288CAS No.: 2941512-37-2DosatiLink-1 is an Abelson murine leukemia (ABL) enzyme inhibitor.
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Leu-PEG1-Dasa
0 ImagesCat. No.: HY-180925CAS No.: 3037776-72-7Leu-PEG1-Dasa is a potent BCR-ABL PROTAC degrader with a DC50 of 0.48 nM. Leu-PEG1-Dasa uses a single amino acid as the E3 ligand and belongs to a mini-PROTAC, functioning through the N-terminal canonical pathway. Leu-PEG1-Dasa exhibits potent anti-proliferative activity against K562 cells. Leu-PEG1-Dasa can be used for the study of chronic myeloid leukemia (CML).
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Antiproliferative agent-30
0 ImagesCat. No.: HY-155112CAS No.: 2713553-88-7Antiproliferative agent-30 (Compound 8g) inhibits tubulin assembly and inhibits FLT3 and Abl1. Antiproliferative agent-30 has vascular-disrupting activity. Antiproliferative agent-30 has broad antiproliferative activities against cancer cell lines (IC50s: 0.054 nM, 0.008 nM, 0.144 nM for HCT-116, K562, MV-4-11 cells respectively). Antiproliferative agent-30 also has anticancer effect against AML with FLT3-ITD-TKD mutation.
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Dasatinib (GMP Like)
0 ImagesCat. No.: HY-10181GLCAS No.: 302962-49-8Synonyms: BMS-354825 (GMP Like)Dasatinib (GMP Like) (BMS-354825 (GMP Like)) is Dasatinib (HY-10181) produced by using GMP like guidelines. GMP Like small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Dasatinib (BMS-354825) 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 inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively. Dasatinib also induces apoptosis and autophagy.
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Multi-kinase-IN-15
0 ImagesCat. No.: HY-131571CAS No.: 1613168-52-7Multi-kinase-IN-15 is an orally active multi-kinase inhibitor. Multi-kinase-IN-15 inhibits the kinase activity of MNK1, MNK2, ABL1, ABL1 T315I, FLT3, VEGFR2, RET, cKIT, FGFR2, PDGFRα, and PDGFRβ. Multi-kinase-IN-15 dose-dependently reduces phosphorylation of eIF4E and phosphorylated Crkl in tumor cells, and decreases phosphorylation of eIF4E in tumor tissues. Multi-kinase-IN-15 inhibits tumor growth. Multi-kinase-IN-15 can be used for research on chronic myeloid leukemia.
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DS-PPE-GW
0 ImagesCat. No.: HY-180218DS-PPE-GW is a BCR-ABL ATTEC degrader. DS-PPE-GW connects BCR-ABL and LC3B, thereby tethering BCR-ABL to the autophagosome membrane. DS-PPE-GW shows potent BCR-ABL degradation. DS-PPE-GW has anticancer activity against chronic myeloid leukemia (Pink: LC3B ligand (HY-10542); Blue: BCR-ABL ligand (HY-107447); Black: Linker (HY-W001860)).
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BCR-ABL degrader 1
0 ImagesCat. No.: HY-180798BCR-ABL degrader 1 is a hydrophobic tag degrader with GNF‑2 (HY-11007) as the ligand and Boc2His (HY-185595) as the hydrophobic tag. BCR-ABL degrader 1 mediates the degradation of BCR‑ABL with a DC50 of 19.9 μM. BCR-ABL degrader 1 induces the degradation of BCR-ABL fusion protein via the ubiquitin-proteasome pathway, a process involving Hsp70 and Hsp90. BCR-ABL degrader 1 downregulates p‑STAT5 and p‑SHP2, the downstream signaling molecules of BCR‑ABL. BCR-ABL degrader 1 can be used in the research of chronic myeloid leukemia.
