Bcr-Abl
BCR-ABL1 is a Philadelphia chromosome-derived fusion oncogene that encodes a constitutively active tyrosine kinase and drives chronic myeloid leukemia (CML) pathophysiology[1]. Mechanistically, BCR-ABL1 coordinates malignant signaling with pathways linked to proliferation, apoptosis resistance, hematopoietic stem cell alteration, and leukemia stem cell persistence[2][3]. In disease models and clinical monitoring, CML is defined by BCR-ABL1 transcripts, most commonly e13a2 and e14a2, which encode p210 BCR-ABL1[4]. Compared with these common isoforms, rare transcripts such as e1a2, e19a2, e6a2, e8a2, e13a3, and e14a3 show structural divergence that can alter leukemogenic activity, diagnostic detection, and tyrosine kinase inhibitor response[5][6]. Transcript subtype also has practical research value, because e14a2 showed faster or deeper molecular responses than e13a2 in imatinib- or nilotinib-treated cohorts, while survival did not differ between transcripts[4]. For experimental applications, imatinib targets ABL kinase activity, whereas nilotinib and dasatinib show stronger BCR-ABL inhibition and retain activity against multiple imatinib-resistant mutants[1].
References:
- [1]. Kantarjian HM, et al. Important therapeutic targets in chronic myelogenous leukemia. Clin Cancer Res. 2007 Feb 15;13(4):1089-97. [Content Brief]
- [2]. Mencalha AL, et al. Role of calcium-dependent protein kinases in chronic myeloid leukemia: combined effects of PKC and BCR-ABL signaling on cellular alterations during leukemia development. Onco Targets Ther. 2014 Jul 8;7:1247-54. [Content Brief]
- [3]. Moradi F, et al. Signaling pathways involved in chronic myeloid leukemia pathogenesis: The importance of targeting Musashi2-Numb signaling to eradicate leukemia stem cells. Iran J Basic Med Sci. 2019 Jun;22(6):581-589. [Content Brief]
- [4]. Su YJ, et al. Comparison of molecular responses and outcomes between BCR::ABL1 e14a2 and e13a2 transcripts in chronic myeloid leukemia. Cancer Sci. 2022 Oct;113(10):3518-3527. [Content Brief]
- [5]. Zhou X, et al. The silent players: Atypical BCR‑ABL isoforms as biomarkers and therapeutic hurdles in CML pathogenesis (Review). Oncol Rep. 2025 Dec;54(6):162. [Content Brief]
- [6]. Massimino M, et al. Impact of the Breakpoint Region on the Leukemogenic Potential and the TKI Responsiveness of Atypical BCR-ABL1 Transcripts. Front Pharmacol. 2021 Jun 30;12:669469. [Content Brief]
All Product Categories
-
Bcr-Abl Related Products (197)
Related Products (197)
-
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.
-
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.
-
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.
-
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 .
-
DosatiLink-1
0 ImagesCat. No.: HY-155288CAS No.: 2941512-37-2DosatiLink-1 is an Abelson murine leukemia (ABL) enzyme inhibitor.
-
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).
-
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.
-
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.
-
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)).
-
ABL1 T315I Recombinant Human Active Protein Kinase
0 ImagesCat. No.: HY-E70640The 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 T315I Recombinant Human Active Protein Kinase is a recombinant ABL1 T315I protein that can be used to study ABL1 T315I-related functions.
-
ABL1 M351T Recombinant Human Active Protein Kinase
0 ImagesCat. No.: HY-E70638The 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 M351T Recombinant Human Active Protein Kinase is a recombinant ABL1 M351T protein that can be used to study ABL1 M351T-related functions.
-
PROTAC DDa-1
0 ImagesCat. No.: HY-156745CAS No.: 3036944-98-3PROTAC DDa-1 is a multi-targeted DCAF1-recruiting tyrosine kinase PROTAC degrader. PROTAC DDa-1 mediates the degradation of TNK2, CSK, LIMK2, TEC, and BTK, with a DC50 of 90 nM for BTK. PROTAC DDa-1 reduces the viability of BTK-dependent diffuse large B-cell lymphoma cells. PROTAC DDa-1 can be used for the research of diffuse large B-cell lymphoma.
-
WB-BC-15
0 ImagesCat. No.: HY-18814CAS No.: 309760-28-9Synonyms: WGB-BC-15WB-BC-15 (WGB-BC-15) is a c-Abl kinase inhibitor. WB-BC-15 can increase radiation-induced germ-cell apoptosis, with EC50 of 10.5 μM.
-
AK-HW-90
0 ImagesCat. No.: HY-157389AK-HW-90 (compound 2B) is a potent panBcr-Abl inhibitor with significant inhibitory activity against Imatinib (HY-15463)-resistant mutants. AK-HW-90 inhibits the resistance mutant Bcr-AblT315I with an IC50 of 0.65 nM. AK-HW-90 has potential anticancer activity and can be used in the study of chronic myelogenous leukemia (CML).
-
AP24163
0 ImagesCat. No.: HY-10364CAS No.: 926922-16-9
-
c-ABL-IN-3
0 ImagesCat. No.: HY-146528CAS No.: 2626934-64-1c-ABL-IN-3 is a potent inhibitor of c-Abl. Activation of c-Abl has been implicated in various diseases, notably cancer. c-ABL-IN-3 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 50).
-
PD173956
0 ImagesCat. No.: HY-119177CAS No.: 305820-76-2
