Bcr-Abl

Abl Cytosolic Substrate is a substrate for Abelson tyrosine kinase (Abl ).

FGFRs-IN-1 (Compound A16) is an orally active inhibitor targeting FGFR1/2/3/4, with IC₅₀ values of 2.3, 7, 11, and 163 nM respectively. It also inhibits VEGFR1/2/3, Abl, and Flt3, with IC₅₀ values of 61, 176, 112, 26, and 353 nM. The compound shows weak inhibition of CYP enzymes. FGFRs-IN-1 reduces the expression of α-SMA and collagen I, and it inhibits epithelial-mesenchymal transition (EMT) in A549 cells stimulated by TGF-β1. Additionally, FGFRs-IN-1 demonstrates anti-inflammatory activity in mouse models of lung fibrosis induced by Bleomycin and liver fibrosis induced by CCl4.

A unique collection of xnum HIF-1 related small chemicals can be used for drug discovery in ischemic disease and cancer and related mechanism studies;

Phe-PEG1-Dasa is a BCR-ABL PROTAC degrader with a DC50 of 1.56 nM. It employs a single amino acid (Phe) as an E3 ligase ligand, leveraging the N-end rule pathway to induce target protein degradation, thereby significantly reducing its molecular size, earning the name mini-PROTAC. Phe-PEG1-Dasa markedly inhibits the proliferation of K562 cells and is applicable in leukemia research.

BCR-ABL-IN-9 (Compound B1) is an inhibitor of BCR-ABL that achieves sustained suppression through the formation of stable covalent bonds with the ABL kinase. It effectively inhibits the activity of ABL kinase (IC₅₀ = 1.2 nM) and possesses anticancer activity.

SIAIS100, a potent BCR-ABL PROTAC degrader, demonstrates a DC50 value of 2.7 nM, highlighting its efficacy.

BCR-ABL-IN-10 (compound B4) is a covalent BCR-ABL inhibitor featuring an arylvinylsulfonate (AVS) moiety, demonstrating an IC₅₀ of 43.1 nM against ABL kinase. It forms a covalent and stable adduct with ABL kinase, enabling the sustained inhibition of intrinsic BCR-ABL activity. This compound is utilized in the study of chronic myeloid leukemia (CML).

Ponatinib, also known as PonatiLink-1-24, is a selective inhibitor of the Abelson murine leukemia (ABL) enzyme [1].

C-ABL-IN-5, a selective c-Abl inhibitor, exhibits neuroprotective properties and has favorable characteristics including blood-brain barrier permeability,

TG-100435 is a novel multi-target oral protein tyrosine kinase inhibitor. The metabolic flux of TG100435 is entirely inhibited by methimazole and ketoconazole. In human liver microsomes or recombinant P450, the formation of TG100435 increases with the activity of cytochrome P450 reductase, suggesting that cytochrome P450 reductase may be involved.

GMB-475 is a PROTAC ligand targeting BCR-ABL1 for degradation via E3 ligase recruitment.

AD57 is a potent inhibitor of both c-Src and Abl with IC50 of 0.025 μM and 0.041 μM, respectively.

Asciminib hydrochloride is a STAMP inhibitor targeting the ABL myristoyl pocket, applied in Ph+ CML research for selective oncogenic signaling modulation.

Imatinib-D4 is a deuterated compound of Imatinib (T6230). Imatinib is an orally active multi-target receptor tyrosine kinase inhibitor.

AT9283 (J-504568) is an effective multi-targeted inhibitor of JAK2(IC50=1.2 nM) and JAK3(IC50=1.1 nM), Aurora A, Aurora B and Abl(T315I).

Flumatinib (HHGV678) is an orally bioavailable tyrosine kinase inhibitor flumatinib, with potential antineoplastic activity.

GNF-2 is a highly selective non-ATP competitive inhibitor of Bcr-Abl.

NVP-BHG712 is a specific EphB4 inhibitor with ED50 of 25 nM that discriminates between VEGFR and EphB4 inhibition; also shows activity against c-Raf, c-Src and

Agerafenib (CEP32496) is a highly potent inhibitor of BRAF.

AG1024 (Tyrphostin) suppresses IGF-1R autophosphorylation(IC50=7 μM), and is less potent for IR(IC50=57 μM).