Catalog No.
Product Name
Application
Product Information
Citations
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PROTAC BCR-ABL Degrader
SIAIS178 is a potent and selective PROTAC BCR-ABL degrader that operates through the recruitment of Von Hippel-Lindau (VHL) E3 ubiquitin ligase, achieving an IC50 of 24 nM. This compound effectively induces degradation of the BCR-ABL protein, demonstrating significant anticancer activity. SIAIS178 is suitable for research applications focused on targeted protein degradation in cancer models. -
Kinases PROTAC
DB1113 is a bifunctional compound designed for targeted protein degradation of various kinases. It effectively induces degradation of ABL1, ABL2, BLK, CDK4, CDK11B, EPHA3, MAPK7, RIPK1, and others, facilitating the investigation of kinase-related signaling pathways. DB1113 is suitable for research focusing on diseases or disorders associated with dysregulated kinase activity, providing a valuable tool for exploring therapeutic interventions in cancer and other conditions. -
BCR-ABL Inhibitor
VS1150 is a BCR-ABL inhibitor that induces inhibitory phosphorylation at the Y253 site, effectively disrupting oncogenic BCR-ABL signaling with an EC50 of 69 nM. This compound not only targets the BCR-ABL fusion protein but also demonstrates inhibitory effects on other oncogenic ABL fusions and drug-resistant mutants, such as T315I. VS1150 is suitable for research applications related to chronic myeloid leukemia (CML) and other cancers driven by ABL fusions. -
T315I Mutant Bcr-Abl Inhibitor
DB07107 is a potent inhibitor of the T315I mutant Bcr-Abl tyrosine kinase, demonstrating resistance against this specific mutation associated with chronic myeloid leukemia. Additionally, DB07107 effectively inhibits Akt1 with an IC50 value of 360 nM, highlighting its dual-targeting capability. This compound is suitable for research applications related to cancer signaling pathways and the development of targeted therapies for resistant forms of leukemia. -
Bcr-Abl Inhibitor
Nilotinib hydrochloride is a potent Bcr-Abl tyrosine kinase inhibitor that exhibits significant antineoplastic activity. It is primarily utilized in research related to chronic myelogenous leukemia (CML), providing valuable insights into the molecular mechanisms of this disease and potential therapeutic strategies. Its oral bioavailability makes it a convenient choice for in vitro and in vivo studies focused on targeting the Bcr-Abl fusion protein. -
PDGFRα/β/Bcr-Abl Inhibitor
GZD856 formic is a selective inhibitor of PDGFRα/β, displaying IC50 values of 68.6 nM and 136.6 nM, respectively, along with potent inhibition of Bcr-Abl, including the T315I mutant with IC50s of 19.9 nM and 15.4 nM. This compound exhibits notable antitumor activity, making it a valuable tool for cancer research. Additionally, GZD856 formic serves as a click chemistry reagent due to its alkyne group, enabling copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules, facilitating bioconjugation studies and compound labeling. -
BCR-ABL Inhibitor
S116836 is a potent BCR-ABL tyrosine kinase inhibitor that effectively targets both wild-type and T315I BCR-ABL variants. It induces apoptosis and arrests the cell cycle in the G0/G1 phase, promoting increased reactive oxygen species (ROS) and reduced glutathione (GSH) levels in BaF3/WT and BaF3/T315I cells. Additionally, S116836 inhibits SRC, LYN, HCK, LCK, BLK, as well as receptor tyrosine kinases including FLT3, TIE2, KIT, and PDGFR-β, demonstrating significant antitumor activity. This compound also features an alkyne group, making it suitable for click chemistry applications, particularly the copper-catalyzed azide-alkyne cycloaddition (CuAAc). -
p210Bcr-Abl Kinase Inhibitor
PD180970 is a potent ATP-competitive inhibitor of the p210Bcr-Abl kinase, exhibiting an IC50 of 5 nM for the inhibition of its autophosphorylation. Additionally, it inhibits Src and KIT kinases with IC50 values of 0.8 nM and 50 nM, respectively. PD180970 effectively induces apoptosis in K562 leukemic cells, making it a valuable reagent for research on chronic myelogenous leukemia. -
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. -
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. -
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. -
BCR-ABL PROTAC Degrader
Leu-PEG1-Dasa is an efficient BCR-ABL PROTAC degrader that operates through the N-terminal canonical pathway, demonstrating a DC50 of 0.48 nM. This compound utilizes a single amino acid as the E3 ligase ligand and exhibits significant anti-proliferative effects on K562 cells. Leu-PEG1-Dasa is applicable in the research of chronic myeloid leukemia (CML) and provides insights into targeted degradation mechanisms in cancer therapy. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
BCR-Abl PROTAC Degrader
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. -
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. -
BCR-ABL Ligand
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. -
mini-PROTAC BCR-ABL Degrader
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. -
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. -
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. -
BCR-ABL PROTAC Degrader
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. -
BCR-ABL PROTAC Degrader
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. -
BCR-ABL PROTAC Degrader
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. -
BCR-ABL PROTAC Degrader
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. -
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. -
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. -
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. -
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. -
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. -
BCR-ABL PROTAC Degrader
Phe-PEG1-Dasa is a BCR-ABL PROTAC degrader, demonstrating a DC50 value of 1.56 nM. This compound utilizes phenylalanine as the E3 ligase ligand and triggers the N-end rule pathway to facilitate the degradation of target proteins. Phe-PEG1-Dasa effectively suppresses the proliferation of K562 leukemia cells, making it a valuable tool for research into leukemia treatment strategies. -
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. -
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. -
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. -
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. -
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. -
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.
