Bcr-Abl

Cat. No.

A33609

CAS No.

688050-42-2

BCR-ABL-IN-7

BCR-ABL-IN-7 is a selective inhibitor of ABL kinases, including both wild-type and the T315I mutant forms. This compound demonstrates potent inhibitory activity against ABL kinases, making it a valuable tool in the study of chronic myeloid leukemia (CML). Researchers can utilize BCR-ABL-IN-7 to investigate mechanisms of resistance and explore therapeutic strategies in CML treatment.

Cat. No.

A33611

CAS No.

1808288-49-4

BCR-ABL-IN-8

BCR-ABL-IN-8 is a potent inhibitor of the BCR-ABL fusion protein. This compound features a trimethoxy group that enhances its activity against chronic myeloid leukemia (CML) cells. BCR-ABL-IN-8 can be utilized in research investigating the molecular mechanisms of CML and potential therapeutic strategies targeting BCR-ABL signaling pathways.

Cat. No.

A33614

CAS No.

2489876-34-6

PROTAC BCR-ABL1 ligand 1

PROTAC BCR-ABL1 ligand 1, also known as compound GMB-475, is designed to selectively target the BCR-ABL1 oncoprotein. It functions as an allosteric inhibitor by recruiting the E3 ligase Von Hippel-Lindau, leading to the ubiquitination and subsequent degradation of BCR-ABL1. This mechanism of action supports research applications in cancer biology, particularly in studying resistance mechanisms in chronic myeloid leukemia (CML) and therapeutic strategies to overcome BCR-ABL1-mediated signaling.

Cat. No.

A33616

CAS No.

2240191-12-0

BCR-ABL-IN-3

BCR-ABL-IN-3 is a potent and irreversible inhibitor of the Bcr-Abl tyrosine kinase, exhibiting an IC50 of ≤100 nM against Ba/F3Bcr-AblT3151 cells. This compound demonstrates significant anti-cancer activity, making it valuable for research applications focused on chronic myeloid leukemia and other malignancies driven by Bcr-Abl mutations. Its use can aid in elucidating the molecular mechanisms of resistance and the development of targeted therapies.

Cat. No.

A33617

CAS No.

2304918-82-7

c-ABL-IN-1

c-ABL-IN-1 is a selective inhibitor of c-Abl kinase, which plays a critical role in various cellular processes, including cell proliferation and survival. This compound demonstrates significant neuroprotective effects, making it a valuable tool in researching therapies for neurodegenerative diseases such as Parkinson's disease. Its ability to inhibit c-Abl specifically allows for targeted studies into the mechanisms underlying neurodegeneration and potential therapeutic interventions.

Cat. No.

A33619

CAS No.

2941512-37-2

DosatiLink-1

DosatiLink-1 is a selective inhibitor of the Abelson murine leukemia (ABL) enzyme. It exhibits potent inhibitory activity against ABL, making it a valuable tool for studying ABL-related signaling pathways and its role in oncogenesis. This compound is useful in research focused on cancer biology and can aid in the development of targeted therapies for ABL-driven malignancies.

Cat. No.

A33621

CAS No.

309760-28-9

WB-BC-15

Synonyms: WGB-BC-15

WB-BC-15 is a selective c-Abl kinase inhibitor that effectively enhances radiation-induced germ-cell apoptosis. With an EC50 value of 10.5 μM, it demonstrates potential for use in cancer research, focusing on mechanisms of radio-sensitivity and apoptosis in germ cells. This compound may serve as a valuable tool for elucidating the role of c-Abl in therapeutic contexts involving radiation exposure.

Cat. No.

A33622

CAS No.

926922-16-9

AP24163

AP24163 is a selective BCR-ABL kinase inhibitor that effectively targets both wild-type BCR-ABL and the resistant variant BCR-ABL-T315I, with IC50 values of 7 nM and 511 nM, respectively. This compound serves as a valuable tool in the study of chronic myeloid leukemia (CML), enabling researchers to investigate the mechanisms of resistance and develop potential therapeutic approaches.

Cat. No.

A33623

CAS No.

2626934-64-1

c-ABL-IN-3

c-ABL-IN-3 is a potent inhibitor of the c-Abl tyrosine kinase, a target implicated in multiple diseases, particularly cancer. This compound exhibits significant biological activity that may aid in the investigation of neurodegenerative disorders such as amyotrophic lateral sclerosis (ALS) and Parkinson’s disease (PD) as well as various cancer types. Its utilization in research may facilitate a better understanding of c-Abl's role in disease progression and therapeutic interventions.

Cat. No.

A33624

CAS No.

305820-76-2

PD173956

PD173956 is a pyridopyrimidine compound that selectively inhibits the Bcr-Abl kinase, particularly targeting the P-loop mutant form. This inhibitor demonstrates significant activity in blocking Bcr-Abl-mediated signaling pathways, making it valuable for research on chronic myeloid leukemia and other cancers driven by Bcr-Abl mutations. Its specificity and potency support investigations into therapeutic strategies aiming to overcome resistance encountered in kinase inhibitors.

Cat. No.

A33626

CAS No.

2489876-41-5

GMB-805

GMB-805 is a potent BCR-Abl PROTAC degrader, demonstrating a DC50 of 30 nM in K562 cells. It effectively induces antiproliferative activity, making it a valuable tool for studying chronic myeloid leukemia. Additionally, GMB-805 exhibits significant anti-tumor efficacy in vivo, coupled with a favorable safety profile, highlighting its potential for therapeutic development.

Cat. No.

A33628

CAS No.

1795736-60-5

BCR-ABL-IN-5

BCR-ABL-IN-5 is a potent Bcr-Abl kinase inhibitor that demonstrates significant inhibitory activity against both wild-type Bcr-Abl and the T315I mutant, with IC50 values of 0.014 μM and 0.45 μM, respectively. This compound exhibits anti-proliferative effects on leukemic cells, making it a valuable tool in research related to chronic myeloid leukemia and related conditions. BCR-ABL-IN-5 is suitable for studies aimed at understanding the mechanisms of Bcr-Abl-mediated oncogenesis and developing targeted therapies.

Cat. No.

A33629

CAS No.

3106065-83-9

Asciminib-NH2

Asciminib-NH2 is a ligand targeting BCR-ABL, specifically involved in the modulation of oncogenic signaling pathways. This compound is crucial for the synthesis of proteolysis-targeting chimeras (PROTACs), including P19As, facilitating the targeted degradation of BCR-ABL fusion proteins. Its utility in research supports investigations into targeted cancer therapies and the mechanistic study of BCR-ABL related malignancies.

Cat. No.

A33630

CAS No.

3037776-67-0

Arg-PEG1-Dasa

Arg-PEG1-Dasa is a mini-PROTAC designed to selectively degrade BCR-ABL, a key oncogenic driver in chronic myeloid leukemia. It demonstrates potent degradation efficacy with an EC50 of 0.85 nM, and exhibits significant antiproliferative activity in K562 cells, with an IC50 of 0.36 nM. This reagent is valuable for research applications focused on targeted therapies for BCR-ABL-driven malignancies.

Cat. No.

A33632

CAS No.

1808287-83-3

CHMFL-ABL-053

CHMFL-ABL-053 is a potent, selective inhibitor targeting BCR-ABL, SRC, and p38 kinases, exhibiting IC50 values of 70 nM, 90 nM, and 62 nM, respectively. This compound demonstrates significant antiproliferative activity, making it a valuable tool in cancer research, particularly in studies focusing on chronic myeloid leukemia and related malignancies. Its oral bioavailability enhances its utility in in vivo research applications.

Cat. No.

A33634

CAS No.

2941512-38-3

DosatiLink-2

DosatiLink-2 is an Abelson murine leukemia (ABL) enzyme inhibitor that functions by selectively inhibiting the kinase activity of the ABL protein. This compound demonstrates significant biological activity against ABL-driven malignancies, making it a valuable tool for research in cancer biology and therapeutic development. It is particularly useful in studies assessing the role of ABL in oncogenesis and resistance mechanisms in cancer treatment.

Cat. No.

A33635

CAS No.

2512843-74-0

P19P

P19P is a BCR-ABL PROTAC degrader that demonstrates a DC50 value of approximately 20 nM for wild-type BCR-ABL protein. It effectively degrades various drug-resistant mutants, including T315I, E255K, H396R, and V468F, and exhibits significant anti-proliferative activity in BaF3-BCR-ABL (T315I) cells, with an IC50 of 13.1 nM against ABL (T315I). P19P is suitable for research applications related to chronic myeloid leukemia and acute lymphoblastic leukemia while showing no inhibition of vascular lumen formation in HUVEC cells.

Cat. No.

A33636

CAS No.

3033463-06-5

SIAIS100

SIAIS100 is a potent BCR-ABL PROTAC degrader, exhibiting a DC50 value of 2.7 nM. This compound facilitates the targeted degradation of the BCR-ABL fusion protein, making it an important tool in the study of chronic myeloid leukemia (CML). Its ability to induce proteolytic degradation offers valuable insights for therapeutic development and understanding disease mechanisms associated with CML.

Cat. No.

A33640

CAS No.

2378581-37-2

SIAIS056

SIAIS056 is a BCR-ABL PROTAC degrader that effectively targets and degrades BCR-ABL fusion proteins, displaying a potent DC50 value of 0.18 nM. It inhibits the BCR-ABL signaling pathway in a time-dependent manner, leading to reduced phosphorylation of BCR-ABL as well as downstream effectors like STAT5 and CRKL in K562 cells. Additionally, SIAIS056 demonstrates the ability to degrade various BCR-ABL resistance mutations and exhibits significant anti-proliferative effects, resulting in marked tumor regression in K562 xenograft models. This compound is valuable for research in leukemia.

Cat. No.

A33641

CAS No.

2635386-51-3

P22D

P22D is a BCR-ABL PROTAC degrader designed for targeted protein degradation, exhibiting a DC50 value of approximately 10 nM for the wild-type BCR-ABL protein. This compound effectively inhibits the proliferation of K562 cells harboring the wild-type BCR-ABL, but does not exhibit activity against BaF3-BCR-ABL (T315I) cells. P22D is valuable for research on chronic myeloid leukemia and acute lymphocytic leukemia, offering insights into the mechanisms of resistance and targeted therapies.

Cat. No.

A33643

CAS No.

2574593-54-5

c-ABL-IN-2

c-ABL-IN-2 is a selective inhibitor of c-Abl, a tyrosine kinase implicated in various pathologies, particularly cancer. This compound demonstrates significant potential for investigating neurodegenerative diseases such as amyotrophic lateral sclerosis (ALS) and Parkinson's disease (PD). Additionally, c-ABL-IN-2 features an alkyne group, enabling it to function as a click chemistry reagent that can participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc), making it a valuable tool for chemical biology applications.

Cat. No.

A33644

CAS No.

2499499-26-0

BCR-ABL-IN-6

BCR-ABL-IN-6 is a selective Bcr-Abl kinase inhibitor targeting the Bcr-Abl fusion protein, with IC50 values of 4.6 nM for Bcr-AblWT and 227 nM for Bcr-AblT315I. It effectively inhibits Bcr-Abl kinase activity within cells, demonstrating an EC50 of 14.6 nM. As an imatinib derivative, BCR-ABL-IN-6 is applicable in research related to chronic myelogenous leukemia. Additionally, this compound features an alkyne group, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc) reactions, thus serving as a useful click chemistry reagent in various experimental contexts.

Cat. No.

A33645

CAS No.

2626934-68-5

c-ABL-IN-4

c-ABL-IN-4 is a potent inhibitor of the c-Abl tyrosine kinase, a critical target in the treatment of various malignancies and neurodegenerative disorders. Inhibition of c-Abl has been associated with potential therapeutic effects in conditions such as amyotrophic lateral sclerosis (ALS) and Parkinson’s disease (PD), as well as in cancer research. This compound facilitates the exploration of c-Abl’s role in disease pathology and therapeutic intervention strategies.

Cat. No.

A33646

CAS No.

2669790-59-2

BCR-ABL-IN-4

BCR-ABL-IN-4 is a potent inhibitor of the BCR-ABL oncogene, exhibiting significant anticancer activity. It effectively suppresses the proliferation of cancer cells, demonstrating IC50 values of 0.67 nM in K562 cells and 16 nM in BCR-ABL T315I transfected Ba/F3 cells. This compound is valuable for research applications focused on targeted cancer therapies and understanding resistance mechanisms in BCR-ABL positive malignancies.

Cat. No.

A33647

CAS No.

839708-29-1

GNF-6

GNF-6 is a potent inhibitor of the BCR-ABL-T315I mutation, acting primarily as an ATP-competitive inhibitor. It demonstrates inhibitory activity with IC50 values of 0.25 μM for c-ABL-T334I, 0.09 μM for BCR-ABL, and 0.590 μM for the BCR-ABL-T315I variant. By disrupting the assembly of the hydrophobic spine, GNF-6 stabilizes the kinase in an inactive 'DFG-out' conformation, making it a valuable tool for research on resistance mechanisms in chronic myeloid leukemia (CML) and targeted therapeutic strategies.