HOXA Inhibitor
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MEISi-1
0 ImagesMEISi-1 is a small-molecule inhibitor targeting the homeodomain of the MEIS1 protein. MEISi-1 significantly inhibits the activity of luciferase reporter genes containing MEIS binding sites (TGACAG), and induces the self-renewal of a key type of mouse and human hematopoietic stem cells (HSC) both in vitro and in vivo. MEISi-1 promotes cardiomyocyte proliferation and cytokinesis, reduces cardiac fibroblast proliferation, and upregulates the expression of cardiomyocyte-specific genes. MEISi-1 can be used in research on hematological diseases, cardiac regeneration and cancer.
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MEIS-IN-1
0 ImagesMEIS-IN-1 is a potent myeloid ecotropic viral integration site (MEIS) inhibitor to induce murine and human hematopoietic stem-cell expansion.
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IKZF2-degrader 5
0 ImagesCat. No.: HY-182945IKZF2-degrader 5 is a highly efficient, highly selective, rapidly acting, and orally active IKZF2 molecular glue degrader. IKZF2-degrader 5 induces IKZF2 degradation via the Cullin-CRBN-dependent pathway. IKZF2-degrader 5 promotes the production of pro-inflammatory IL-2. IKZF2-degrader 5 attenuates the immunosuppressive function of regulatory T cells (Tregs). IKZF2-degrader 5 triggers rapid, significant, and sustained IKZF2 degradation in the spleen and thymus of mice. IKZF2-degrader 5 inhibits tumor growth. IKZF2-degrader 5 can be used for the research of B16F melanoma.
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HOXA1-IN-1
0 ImagesCat. No.: HY-181823CAS No.: 3118854-61-5HOXA1-IN-1 is a HOXA1 inhibitor. HOXA1-IN-1 downregulates HOXA1 protein levels, suppresses its transcriptional activity, and alters the expression of its downstream target genes. HOXA1-IN-1 induces DNA damage and apoptosis in cancer cells. HOXA1-IN-1 exhibits antitumor efficacy in xenograft models of colorectal cancer and triple-negative breast cancer. HOXA1-IN-1 shows synergistic activity in combination with Cisplatin (HY-17394). HOXA1-IN-1 can be used for the research of colorectal cancer and triple-negative breast cancer.
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AF9/ENL-DOT1L PPI-IN-1
0 ImagesCat. No.: HY-178172AF9/ENL-DOT1L/AF4 PPI-IN-1 is a potent AF9/ENL and histone methyltransferase DOT1L/AF4 protein-protein interactions (PPI) inhibitor. AF9/ENL-DOT1L/AF4 PPI-IN-1 can inhibit the AF9-DOT1L (IC50 = 1.5 μM), AF9-AF4 (IC50 = 1 μM), ENL-AF4 (IC50 = 1.2 μM) interactions. AF9/ENL-DOT1L/AF4 PPI-IN-1 can suppress the expression of Mixed lineage leukemia (MLL) target genes Myc and Meis1 and selectively block the proliferation of MLL-r and several other leukemia cells. AF9/ENL-DOT1L/AF4 PPI-IN-1 exhibits significant antitumor activities in a mouse model of MLL-r leukemia without overt toxicities. AF9/ENL-DOT1L/AF4 PPI-IN-1 can be used for the study of MLL-r leukemia.
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MEIS-IN-3
0 ImagesCat. No.: HY-132871CAS No.: 2761326-88-7MEIS-IN-3 is a potent myeloid ecotropic viral integration site (MEIS) inhibitor.
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HPK1-IN-65
0 ImagesCat. No.: HY-179338HPK1-IN-65 is a selective and orally active HPK1 inhibitor with an IC50 value of < 5 nM. HPK1-IN-65 inhibits HPK1 kinase activity and displays 1257-fold selectivity over the MAP4K kinase family member GLK. HPK1-IN-65 exhibits an IC50 of 92.3 nM for inhibiting pSLP76 phosphorylation. HPK1-IN-65 demonstrates an EC50 of 398 nM for stimulating IL-2 production. HPK1-IN-65 inhibits TCR-induced phosphorylation of SLP76 at Ser376 in a dose-dependent manner. HPK1-IN-65 can be further utilized for colorectal cancer research.
