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KMS11

" in MedChemExpress (MCE) Product Catalog:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-101291
    Iberdomide
    Maximum Cited Publications
    11 Publications Verification

    CC-220

    		 Ligands for E3 Ligase Apoptosis Molecular Glues Inflammation/Immunology Cancer
    Iberdomide (CC-220) is an orally active and potent cereblon (CRBN) E3 ligase modulator (CELMoD) with an IC50 of ~150 nM for cereblon-binding affinity. Iberdomide, a derivative of Thalidomide (HY-14658), has antitumor and immunostimulatory activities .
    Iberdomide
  • HY-50905
    Dovitinib
    Maximum Cited Publications
    11 Publications Verification

    CHIR-258; TKI258

    		 FLT3 c-Kit FGFR VEGFR PDGFR c-Fms Cancer
    Dovitinib (CHIR-258) is an orally active, potent multi-targeted tyrosine kinase (RTK) inhibitor with IC50s of 1, 2, 36, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, CSF-1R, FGFR1/FGFR3, VEGFR1/VEGFR2/VEGFR3 and PDGFRα/PDGFRβ, respectively. Dovitinib has potent antitumor activity .
    Dovitinib
  • HY-154812
    Gintemetostat

    KTX-1001

    		 Histone Methyltransferase CD44 Cancer
    Gintemetostat (KTX-1001) is an orally active, highly specific NSD2/MMSET histone methyltransferase inhibitor with human NSD2 IC50 values ranging 0.460-2.17 nM and NSD2 SET domain IC50 of 2.32 nM and Kd values ranging 6.3-70.4 nM .Gintemetostat reduces H3K36me2 levels, impairs multiple myeloma cell adhesion and colony formation, enhances cytotoxicity, boosts T-cell activation, and sensitizes resistant multiple myeloma cells to other agents .Gintemetostat can be used for the research of multiple myeloma and relapsed and refractory multiple myeloma .
    Gintemetostat
  • HY-145103
    UNC6934

    		Histone Methyltransferase Cancer
    UNC6934 is a selective NSD2-PWWP1 antagonist with IC50 values of 78 nM and 104 nM, and a Ka of 91 nM against human targets. UNC6934 binds to the canonical methyl-lysine binding pocket of NSD2-PWWP1 and directly competes with H3K36me2 for binding. UNC6934 induces the aggregation of NSD2 within the nucleolus, without altering ribosomal RNA transcription, global H3K36me2 levels or the proliferation of KMS-11 cells. UNC6934 can be used in studies related to multiple myeloma and diffuse intrinsic pontine glioma.
    UNC6934
  • HY-139626
    EPZ-719
    4 Publications Verification

    		 Histone Methyltransferase Cancer
    EPZ-719 is a selective, orally effective SETD2 inhibitor with an IC50 value of 0.005 μM. EPZ-719 has anticancer activity .
    EPZ-719
  • HY-147914
    NSD2-IN-1

    		Apoptosis Cancer
    NSD2-IN-1 (compound 38) is a potent and high selective NSD2-PWWP1 (nuclear receptor-binding SET domain 2-PWWP1) inhibitor, with an IC50 of 0.11 μM. NSD2-IN-1 can bind to NSD2-PWWP1 and then affect the expression of genes regulated by NSD2. NSD2-IN-1 induces apoptosis and cell cycle arrest .
    NSD2-IN-1
  • HY-101291R
    Iberdomide (Standard)

    CC-220 (Standard)

    		 Reference Standards Ligands for E3 Ligase Apoptosis Molecular Glues Inflammation/Immunology Cancer
    Iberdomide (Standard) is the analytical standard of Iberdomide. This product is intended for research and analytical applications. Iberdomide (CC-220) is an orally active and potent cereblon (CRBN) E3 ligase modulator (CELMoD) with an IC50 of ~150 nM for cereblon-binding affinity. Iberdomide, a derivative of Thalidomide (HY-14658), has antitumor and immunostimulatory activities .
    Iberdomide (Standard)
  • HY-174981
    LC-MF-4

    		PROTACs FGFR ATP Synthase Cancer
    LC-MF-4 is a selective FGFR3 PROTAC degrader with a DC50 of 30.89 nM in KMS-11 cells. LC-MF-4 inhibits the metabolic function of FGFR3-TACC3 fusion positive cancers with reduction of ATP synthesis and inhibition of mitochondrial biogenesis genes. LC-MF-4 has potent antitumor activity in the Ba/F3-FGFR3-TACC3 xenograft mice model. LC-MF-4 can be used for FGFR3-altered cancers like bladder cancer and urothelial carcinoma (UC) research . Pink: FGFR3 ligand (HY-175414); Blue: VHL ligase ligand (HY-125905); Black: linker (HY-Y1224)
    LC-MF-4
  • HY-171119
    NSD2-PWWP1-IN-1

    		Histone Methyltransferase Cancer
    NSD2-PWWP1-IN-1 (compound 31) is a potent NSD2-PWWP1 inhibitor with an IC50 value of 0.64 µM. NSD2-PWWP1-IN-1 has the potential for the research of cancer .
    NSD2-PWWP1-IN-1
  • HY-171120
    NSD2-PWWP1-IN-2

    		Histone Methyltransferase Cancer
    NSD2-PWWP1-IN-2 (compound 33) is a potent NSD2-PWWP1 inhibitor with an IC50 value of 1.49 µM. NSD2-PWWP1-IN-2 has the potential for the research of cancer .
    NSD2-PWWP1-IN-2
  • HY-50905R
    Dovitinib (Standard)

    CHIR-258 (Standard); TKI258 (Standard)

    		 FLT3 c-Kit FGFR VEGFR PDGFR c-Fms Reference Standards Cancer
    Dovitinib (Standard) is the analytical standard of Dovitinib. This product is intended for research and analytical applications. Dovitinib (CHIR-258) is an orally active, potent multi-targeted tyrosine kinase (RTK) inhibitor with IC50s of 1, 2, 36, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, CSF-1R, FGFR1/FGFR3, VEGFR1/VEGFR2/VEGFR3 and PDGFRα/PDGFRβ, respectively. Dovitinib has potent antitumor activity .
    Dovitinib (Standard)
  • HY-177400
    NSD-IN-5

    		Histone Methyltransferase Cancer
    NSD-IN-5 (Example 47) is a nuclear receptor-binding SET domain (NSD) inhibitor with IC5050 values ​​of 6 and < 1 nM for NSD1 and NSD2, respectively. NSD-IN-5 also exhibits inhibitory activity against Avg KMS11 cells with an IC5050 of 6 nM. NSD-IN-5 may be used in research on multiple myeloma .
    NSD-IN-5
  • HY-171121
    NSD2-PWWP1-IN-3

    		Histone Methyltransferase Cancer
    NSD2-PWWP1-IN-3 (compound 36) is a potent NSD2-PWWP1 inhibitor with an IC50 value of 8.05 µM. NSD2-PWWP1-IN-3 has the potential for the research of cancer .
    NSD2-PWWP1-IN-3

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