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Results for "

rs4-11-cell

" in MedChemExpress (MCE) Product Catalog:

11

Inhibitors & Agonists

1

Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-114312
    MD-224
    5+ Cited Publications

    		 PROTACs MDM-2/p53 E1/E2/E3 Enzyme Cancer
    MD-224 is a first-in-class and highly potent small-molecule human murine double minute 2 (MDM2) degrader based on the proteolysistargeting chimera (PROTAC) concept. MD-224 consists of ligands for Cereblon and MDM2. MD-224 induces rapid degradation of MDM2 at concentrations <1 nM in human leukemia cells, and achieves an IC50 value of 1.5 nM in inhibition of growth of RS4;11 cells. MD-224 has the potential to be a new class of anticancer agent . MD-224 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    MD-224
  • HY-148369
    U7D-1

    		PROTACs Deubiquitinase Apoptosis MDM-2/p53 Cancer
    U7D-1 is a first-in-class potent and selective USP7 (ubiquitin-specific protease 7) PROTAC degrader, with a DC50 of 33 nM in RS4;11 cells. U7D-1 shows anticancer activity. U7D-1 induces apoptosis in Jeko-1 cells .
    U7D-1
  • HY-130122
    MG-277
    1 Publications Verification

    		 Molecular Glues PROTACs Apoptosis Cancer
    MG-277, a molecular glue degrader, effectively induces degradation of a translation termination factor based on Cereblon E3 ligand, GSPT1, with a DC50 of 1.3 nM. MG-277 potently inhibits tumor cell growth in a p53-independent manner, with IC50s of 3.5 nM for RS4;11 cells and 3.4 nM for p53 mutant RS4;11/IRMI-2 cells, respectively. Anticancer activity .
    MG-277
  • HY-149428
    AD4
    1 Publications Verification

    		 PROTACs Cancer
    AD4 is an artemisinin derivative that is a proteolytic targeting chimera (PROTAC) targeting PCLAF. AD4 can effectively degrade PCLAF in RS4;11 cells (IC50: 0.6 nM), thereby activating the p21/Rb axis and exerting anti-tumor activity. AD4 also prolonged survival of RS4;11-transplanted NOD/SCID mice, with in vivo efficacy .
    AD4
  • HY-146887
    USP7-IN-9

    		Deubiquitinase Apoptosis Cancer
    USP7-IN-9 is a highly potent ubiquitin-specific protease 7 (USP7) inhibitor with an IC50 value of 40.8 nM. USP7-IN-9 can induce apoptosis and arrest cell progression at G0/G1 and S phases in RS4; 11 cells. USP7-IN-9 reduces the protein levels of oncoproteins MDM2 and DNMT1 and increases the protein levels of tumor suppressors p53 and p21 .
    USP7-IN-9
  • HY-159175
    XM-U-14

    		PROTACs Deubiquitinase Apoptosis MDM-2/p53 Cancer
    XM-U-14 is a selective PROTAC USP7 Degrader (DC50: 0.74 nM in inducing USP7 degradation in RS4;11 cell line). XM-U-14 upregulates the levels of p53 and p21. XM-U-14 also significantly inhibits acute lymphoblastic leukemia (ALL) cell growth (IC50: 0.5 nM and 8.3 nM for RS4;11 cells and Reh cells respectively). XM-U-14 induces apoptosis and cycle arrest. XM-U-14 inhibits tumor growth. (Blue: VHL ligand (HY-159465), Black: linker (HY-W539783); Pink: USP7 inhibitor (HY-159464)) .
    XM-U-14
  • HY-177102
    Mesutoclax

    ICP-248

    		 Bcl-2 Family Cancer
    Mesutoclax (ICP-248) (Compound 5) is a selective BCL-2 inhibitor with an IC50 of 1.54 nM. Mesutoclax has weak activity against BCL-XL (IC50: ＞1000 nM). Mesutoclax can inhibit the activity of RS4;11 cells with an IC50 of 2.75 nM. Mesutoclax can be used in the study of cancer .
    Mesutoclax
  • HY-174458
    MD-4251

    		PROTACs MDM-2/p53 IKZF Family Casein Kinase Cancer
    MD-4251 is an orally active MDM2 PROTAC degrader. MD-4251 potently degrades MDM2 in RS4;11 cells (DC50: 0.2 nM) and actives p53. MD-4251 shows strong antiproliferative activity against acute leukemia cells (wild-type p53) with minimal efficacy in mutant type. MD-4251 induces complete tumor regression in RS4;11 xenograft mice model . Pink: MDM2 ligand (HY-130684); Blue: CRBN ligase ligand (HY-W883326); Black: linker
    MD-4251
  • HY-114228
    PROTAC BET degrader-2
    2 Publications Verification

    		 PROTACs Epigenetic Reader Domain Cancer
    PROTAC BET degrader-2 is a PROTAC connected by ligands for Cereblon and BET with an IC50 value of 9.6 nM in cell growth inhibition in the RS4;11 cells and capable of achieving tumor regression.
    PROTAC BET degrader-2
  • HY-143872
    Bcl-2-IN-4

    		Bcl-2 Family Cancer
    Bcl-2-IN-4 is a potent, orally active and selective Bcl-2 inhibitor with an IC50 of 1.5 nM. Bcl-2-IN-4 displays >200-fold selectivity over Bcl-xL (IC50 of 411 nM). Bcl-2-IN-4 inhibits RS4; 11 cell proliferation with an IC50 of 2.7 nM (WO2021180040A1; compound 2) .
    Bcl-2-IN-4
  • HY-143873
    Bcl-2-IN-5

    		Bcl-2 Family Cancer
    Bcl-2-IN-5 is a BCL-2 inhibitor with IC50s of 0.12 nM, 0.14 nM and 0.22 nM for Bcl-2 wild type, Bcl-2 D103Y and Bcl-2 G101V, respectively. Bcl-2-IN-5 inhibits the cell growth with IC50 values of 0.2 nM and 0.44 nM for Bcl 2-G101V knock-in RS4; 11 and RS4; 11 cells, respectively (WO2021208963A1; Example 155) .
    Bcl-2-IN-5

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