Bcr-Abl

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  1. p210bcr/abl Inhibitor

    Adaphostin, a potent inhibitor of the p210bcr/abl fusion protein (IC50 = 14 μM), exhibits significant anti-leukemic activity. It induces apoptosis in T-lymphoblastic leukemia cell lines, with IC50 values ranging from 17 to 216 nM. This compound demonstrates selective efficacy against both chronic and acute myeloid leukemia cells and increases reactive oxygen species (ROS) levels in chronic lymphocytic leukemia (CLL) B cells, making it valuable for research in leukemia therapeutics and cellular pathways related to oxidative stress.
  2. Bcr-Abl Inhibitor

    HG-7-85-01 is a type II ATP competitive inhibitor that targets Bcr-Abl, including its T315I mutant, as well as PDGFRα, Kit, and Src kinases. It demonstrates potent inhibition with IC50 values of 3 nM for T315I Bcr-Abl, 20 nM for KDR, and 30 nM for RET, while showing minimal activity against other kinases (IC50 > 2 μM). HG-7-85-01 effectively inhibits cell proliferation through the induction of apoptosis and the suppression of cell-cycle progression, making it a valuable tool for research in cancer biology.
  3. Multi-kinase Inhibitor

    Debio 0617B is a multi-kinase inhibitor that targets key kinases involved in the regulation of STAT3/STAT5 signaling, including JAK, SRC, ABL, and class III/V receptor tyrosine kinases. This compound effectively reduces the maintenance and self-renewal of primary human acute myeloid leukemia (AML) CD34+ stem/progenitor cells. Additionally, Debio 0617B has demonstrated efficacy in preclinical models of STAT3-driven solid tumors, making it a valuable tool for cancer research and therapeutic development.
  4. Abl Kinase Inhibitor

    AFG210 is a potent Abl kinase inhibitor with an IC50 of 330 nM, demonstrating significant inhibitory effects on additional kinases including B-Raf, C-Raf, FGFR-1, RET, and VEGF receptors. Its unique multi-target profile positions AFG210 as a valuable tool for investigating chronic myeloid leukemia and other disorders associated with aberrant Abl kinase activation. This compound facilitates research exploring targeted therapies and signaling pathways linked to these diseases.
  5. Bcr/Abl Kinase Inhibitor

    PD166326 is a potent Bcr/Abl kinase inhibitor with an IC50 of 8 nM for Abl tyrosine kinase and 6 nM for Src tyrosine kinase. This compound effectively blocks Bcr/Abl kinase activity, leading to the inhibition of Bcr/Abl-dependent cell proliferation and cell cycle progression. In preclinical studies, PD166326 has demonstrated the ability to reduce peripheral blood granulocytosis, alleviate splenomegaly, and prolong survival in mouse models of chronic myeloid leukemia. It serves as a valuable tool for research focused on chronic myeloid leukemia and related signaling pathways.
  6. BCR-ABL1 Inhibitor

    Asciminib hydrochloride is a potent and selective allosteric inhibitor targeting BCR-ABL1. This compound demonstrates significant biological activity by inhibiting Ba/F3 cells with an IC50 of 0.25 nM. Asciminib is primarily utilized in research applications focusing on chronic myeloid leukemia and other BCR-ABL1 driven malignancies, providing valuable insight into the mechanisms of resistance and therapeutic strategies.
  7. Bcr-Abl Inhibitor

    Nilotinib-d6 is a deuterated form of Nilotinib, a selective inhibitor of the Bcr-Abl tyrosine kinase. This compound exhibits antineoplastic activity, making it valuable in the study of chronic myeloid leukemia and other malignancies characterized by Bcr-Abl expression. Nilotinib-d6 is particularly useful in pharmacokinetic studies and metabolic profiling due to its unique isotopic labeling.
  8. Bcr-Abl Inhibitor

    AKE-72 is a potent Bcr-Abl inhibitor that selectively targets various BCR-ABL variants, including BCR-ABLWT, BCR-ABLT315, BCR-ABLE255K, BCR-ABLF3171, BCR-ABLH396P, and BCR-ABLQ252H, exhibiting IC50 values of less than 0.5 nM to 9 nM. This compound demonstrates significant anti-leukemic activity in the K-562 cell line, making it a valuable tool for research in hematological malignancies and targeted cancer therapies. AKE-72 holds potential for further studies investigating BCR-ABL-mediated signaling pathways and resistance mechanisms.
  9. ABL Inhibitor

    BCR-ABL1-IN-1 is a selective ABL1 inhibitor with an IC50 of 8.7 nM. This compound is primarily utilized in research investigating diseases of the central nervous system (CNS). Its potent inhibitory action on ABL1 makes it an invaluable tool for studying ABL-related signaling pathways and their implications in various neurological disorders.
  10. Abl Inhibitor

    PPY-A is an effective inhibitor of both wild-type and T315I mutant Abl kinases, exhibiting IC50 values of 9 nM and 20 nM, respectively. This compound also demonstrates inhibitory activity in Ba/F3 cells transformed with wild-type Abl and the T315I mutant, with IC50s of 390 nM and 180 nM, respectively. PPY-A is particularly relevant for research in chronic myeloid leukemia (CML), offering a valuable tool for investigating therapeutic strategies against this malignancy.
  11. ABL Kinase Inhibitor

    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.
  12. Bcr-Abl Inhibitor

    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.
  13. Bcr-Abl Inhibitor

    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.
  14. Bcr-Abl Inhibitor

    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.
  15. c-ABL Inhibitor

    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.
  16. ABL Inhibitor

    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.
  17. c-Abl Inhibitor

    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.
  18. BCR-ABL Kinase Inhibitor

    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.
  19. c-Abl Inhibitor

    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.
  20. Bcr-Abl Inhibitor

    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.
  21. Bcr-Abl Kinase Inhibitor

    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.
  22. BCR-ABL/SRC/p38 Inhibitor

    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.
  23. ABL Inhibitor

    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.
  24. c-Abl Inhibitor

    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.
  25. Bcr-Abl Inhibitor

    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.
  26. c-Abl Inhibitor

    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.
  27. BCR-ABL Inhibitor

    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.
  28. BCR-ABL-T315I Mutation Inhibitor

    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.
  29. ABL Inhibitor

    PonatiLink-1-24 is an inhibitor of the Abelson murine leukemia virus (ABL) enzyme. This compound demonstrates significant biological activity by selectively inhibiting ABL kinase activity, which is vital in various malignancies. It is particularly useful in studying cancer cell signaling pathways and the development of targeted therapies for ABL-related disorders.
  30. Scr/ABL Inhibitor

    AP-24226 is a selective inhibitor of the non-receptor tyrosine kinases Src and ABL. It exhibits significant activity in hindering cell proliferation and survival in various cancer cell lines, making it a valuable tool for cancer research. Its specificity for Src/ABL pathways allows for detailed investigations into their roles in oncogenic processes and therapeutic responses.
  31. c-Abl Inhibitor

    Tyrosine kinase-IN-9 is a potent inhibitor of the c-Abl tyrosine kinase. This compound demonstrates significant biological activity in modulating signaling pathways associated with neurodegenerative diseases such as Alzheimer’s and Parkinson’s disease. It serves as a valuable research tool for investigating the roles of c-Abl in cellular processes related to these conditions.
  32. BCR-ABL Inhibitor

    BCR-ABL kinase-IN-3 is a potent inhibitor of the BCR-ABL fusion protein, a critical driver in the pathology of acute myeloid leukemia (AML). This compound exhibits significant biological activity in inhibiting the kinase activity, making it a valuable tool for research into therapeutic strategies targeting BCR-ABL-related malignancies. Its application spans the investigation of molecular mechanisms underlying leukemia and the development of innovative treatments for improved patient outcomes.
  33. BCR-ABL Inhibitor

    BCR-ABL-IN-11 is a selective BCR-ABL inhibitor that exhibits significant anticancer activity in chronic myelogenous leukemia (CML) models. With an IC50 value of 129.61 μM in K562 cells, BCR-ABL-IN-11 is a useful tool for studying the molecular mechanisms underlying CML and for evaluating potential therapeutic strategies targeting this oncogenic fusion protein. Its efficacy makes it suitable for research applications focused on leukemia treatment and drug resistance mechanisms.
  34. JAK2/Bcr-Abl/FLT3 Inhibitor

    LS-104 is a non-ATP-competitive inhibitor targeting JAK2, Bcr-Abl, and FLT3. It effectively induces apoptosis in JAK2V617F-positive cells while inhibiting JAK2 autophosphorylation and downstream signaling pathways. Additionally, LS-104 demonstrates significant cytotoxic effects and inhibits the proliferation of FLT3-expressing leukemic cells. This hydroxystyryl-acrylonitrile compound holds potential for research into myeloproliferative disorders and refractory or relapsed hematologic malignancies.
  35. Bcr-Abl1 Inhibitor

    Radotinib dihydrochloride is a selective Bcr-Abl1 tyrosine kinase inhibitor with an IC50 of 34 nM, demonstrating oral bioavailability and the ability to penetrate the blood-brain barrier. This compound exhibits significant anti-tumor activity by inhibiting cell proliferation, inducing cell cycle arrest, and promoting apoptosis in tumor cells. Radotinib dihydrochloride is utilized in research related to chronic myeloid leukemia, multiple myeloma, and neurodegenerative disorders, particularly those involving prion diseases.
  36. BCR-ABL Inhibitor

    CHMFL-48 is a potent BCR-ABL kinase inhibitor that effectively targets both wild-type and imatinib-resistant mutants. With IC50 values of 1 nM for ABL wild-type and 0.8 nM for the ABL T315I mutant, CHMFL-48 inhibits autophosphorylation of BCR-ABL, disrupting downstream signaling pathways involving STAT5 and CRKL. This mechanism results in cell cycle arrest and the induction of apoptosis, making CHMFL-48 a valuable tool for research focused on chronic myeloid leukemia (CML).
  37. BCR-ABL Inhibitor

    HS-438 is a potent and selective inhibitor of BCR-ABL, a fusion protein associated with chronic myeloid leukemia (CML). This compound exhibits significant antiproliferative effects, leading to reduced phosphorylation of BCR-ABL at Tyr177, and promotes apoptosis alongside G0/G1 cell cycle arrest. HS-438 demonstrates substantial antitumor activity, making it a valuable tool for investigations into CML and related therapeutic strategies.

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