Bcr-Abl

<p>SNIPER(ABL)-020, a Dasatinib-Bestatin conjugate via linker, inhibits ABL and targets IAP, reducing BCR-ABL protein.</p>

<p>SNIPER(ABL)-019, a compound that links Dasatinib (ABL inhibitor) to MV-1 (IAP ligand) via a linker, effectively reduces BCR-ABL protein levels, exhibiting a</p>

<p>cSRC/BCR-ABL1-IN-1 (compound 16a) is a dual-target inhibitor of the cSRC/BCR-ABL1 kinases.</p>

<p>cSRC/BCR-ABL-IN-1 (compound 21b) is a potent inhibitor of Bcr-Abl and C-Src, with IC50 values of 56.2 nM and 101 nM, respectively. It exhibits cytotoxicity.</p>

<p>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.</p>

<p>SNIPER(ABL)-013, a compound that links GNF5 (ABL inhibitor) with Bestatin (IAP ligand) via a linker, effectively reduces BCR-ABL protein levels with a DC50 of</p>

<p>A unique collection of 1016 tyrosine kinase inhibitors for high throughput screening and high content screening for drug discovery in tyrosine kinase related</p>

<p>SNIPER(ABL)-050 is a chemical compound that combines Imatinib, an ABL inhibitor, with MV-1, an IAP ligand, using a linker.</p>

<p>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.</p>

<p>SIAIS178 is a potent and selective degrader of BCR-ABL based on PROTAC technology (IC50 of 24 nM).</p>

<p>SNIPER(ABL)-033, a compound that conjugates HG-7-85-01 (ABL inhibitor) to a LCL161 derivative (IAP ligand) via a linker, effectively reduces BCR-ABL protein</p>

<p>A unique collection of 2720 kinase inhibitors/regulators for high throughput screening and high content screening for drug discovery in kinase related diseases;</p>

<p>SNIPER(ABL)-044, a compound that links HG-7-85-01 (ABL inhibitor) to Bestatin (IAP ligand) via a linker, effectively reduces BCR-ABL protein levels, achieving a</p>

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

<p>Tyrosine kinase-IN-8 (compound 4e) is a BCR‐ABL1 tyrosine kinase inhibitor (TKI) exhibiting antiproliferative activity against the chronic myeloid leukemia (CML) cell line K562, with a CC50 of 0.8 µM. Tyrosine kinase-IN-8 is applicable for research in chronic leukemia.</p>

<p>SNIPER(ABL)-049, a compound that conjugates Imatinib (ABL inhibitor) with Bestatin (IAP ligand) through a linker, effectively reduces BCR-ABL protein levels,</p>

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

<p>SNIPER(ABL)-024, a compound that conjugates GNF5 (ABL inhibitor) to an LCL161 derivative (IAP ligand) via a linker, effectively reduces BCR-ABL protein levels,</p>

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

<p>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).</p>