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Results for "

synthetic lethality

" in MedChemExpress (MCE) Product Catalog:

18

Inhibitors & Agonists

1

Fluorescent Dye

1

Biochemical Assay Reagents

2

Peptides

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-N4115
    Syrosingopine
    5 Publications Verification

    Su 3118

    Monocarboxylate Transporter Cardiovascular Disease Cancer
    Syrosingopine (Su 3118) is an orally active lactate transporters (MCT1/MCT4) dual inhibitor, which can reduce glycolysis and induce synthetic lethality in cancer cells when combine with metformin. Syrosingopine shows anti-hypertensive activity by depleting peripheral stores of norepinephrine .
    Syrosingopine
  • HY-132167
    Saruparib
    5+ Cited Publications

    AZD5305

    PARP Cancer
    Saruparib (AZD5305) is a potent, orally active and selective PARP inhibitor and trapper with IC50 values of 3 nM and 1400 nM for PARP1 and PARP2, respectively. Saruparib has anti-proliferative activity and inhibits growth in cells with deficiencies in DNA repair .
    Saruparib
  • HY-141520
    ART558
    Maximum Cited Publications
    23 Publications Verification

    DNA/RNA Synthesis Cancer
    ART558 is a potent, selective and allosteric DNA polymerase theta (Polθ) inhibitor (IC50=7.9 nM). ART558 elicits BRCA-gene synthetic lethality and DNA damage. ART558 can be used for the research of cancer, such as breast cancer .
    ART558
  • HY-P3912A

    Interleukin Related Infection
    Endotoxin inhibitor TFA is a synthetic peptide that binds lipid A with high affinity, thereby detoxifying LPS (HY-D1056) and preventing LPS-induced cytokine release in vivo. Endotoxin inhibitor TFA inhibits the febrile response to LPS with very low toxicity and lethality .
    Endotoxin inhibitor TFA
  • HY-112626

    CDK Cancer
    CDK12-IN-2 is a potent, selective and nanomolar CDK12 inhibitor (IC50=52 nM) with good physicochemical properties. CDK12-IN-2 is also a strong CDK13 inhibitor due to CDK13 is the closest homologue of CDK12. CDK12-IN-2 shows excellent kinase selectivity for CDK12 over CDK2, 9, 8, and 7. CDK12-IN-2 inhibits the phosphorylation of Ser2 in the C-terminal domain of RNA polymerase II. CDK12-IN-2 can be used an excellent chemical probe for functional studies of CDK12 .
    CDK12-IN-2
  • HY-144691

    PROTACs CDK Cancer
    PP-C8 is a potent and selective PROTAC CDK12-Cyclin K degrader. PP-C8 induces CDK12-Cyclin K degradation with DC50s of 416 and 412 nM for CDK12 and Cyclin K, respectively. PP-C8 demonstrates profound synergistic antiproliferative effects with PARP inhibitor in triple-negative breast cancer (TNBC) .
    PP-C8
  • HY-145268

    Cadherin Cancer
    SLEC-11 is a CDH1/E-cadherin modulator that potently inhibits cell death in E-cadherin-deficient cells (EC50=8.2 μM). SLEC-11 can be used to study potential synthetic lethal therapies for gastric cancer .
    SLEC-11
  • HY-P3912

    COX Interleukin Related Infection
    Endotoxin inhibitor a synthetic peptide that binds lipid A with high affinity, thereby detoxifying LPS (HY-D1056) and preventing LPS-induced cytokine release in vivo. Endotoxin inhibitor inhibits the febrile response to LPS with very low toxicity and lethality .
    Endotoxin inhibitor
  • HY-149952

    ATM/ATR Cancer
    ATR-IN-23 (Compound 34) is a potent and selective ATR inhibitor with an IC50 of 1.5 nM. ATR-IN-23 has potent antiproliferative effects on LoVo cells and synthetic lethality on HT-29 cells, and can be used in the study of DNA damage response (DDR)-deficient cancers .
    ATR-IN-23
  • HY-172737

    Polo-like Kinase (PLK) Cancer
    RP-1664 is a selective and orally active PLK4 inhibitor. RP-1664 drives potent synthetic lethality in TRIM37-high tumor models in vitro and in vivo. RP-1664 induces both centriole loss and amplification contribute to hypersensitivity of neuroblastoma cells .
    RP-1664
  • HY-153361

    PROTACs Cancer
    YD23 is a SMARCA2 PROTAC. YD23 induces degradation of SMARCA2, which is synthetic lethal to SMARCA4. Moreover, YD23 decreases chromatin accessibility at enhancers of a number of genes including cell cycle and cell growth regulatory genes. YD23 reduces chromatin accessibility only in SMARCA4 deficient cells mechanistically .
    YD23
  • HY-145269

    Cadherin Cancer
    AL-GDa62 is a derivative of the CDH1/E-cadherin modulator SLEC-11 (HY-145268) and induces apoptosis in CDH1 -/- cells. AL-GDa62 has an EC50 of 3.2 μM and 2 μM for isogenic mammary epithelial cells MCF10A-WT (wild type) and mutant MCF10A-CDH1 -/-, respectively. AL-GDa62 specifically inhibits TCOF1, ARPC5, and UBC9, and suppresses SUMOylation at low micromolar concentrations .
    AL-GDa62
  • HY-158116

    RO7589831; VVD-133214

    DNA/RNA Synthesis Cancer
    VVD-214 is a synthetic lethal allosteric inhibitor of WRN helicase with an IC50 of 0.1316 µM. VVD-214 covalently binds to cysteine 727 of WRN and inhibits ATP hydrolysis and helicase activity. VVD-214 is potent in causing double-stranded DNA breaks, nuclear swelling, and cell death in high microsatellite instability (MSI) cancers .
    VVD-214
  • HY-141520G

    DNA/RNA Synthesis Cancer
    ART558 (GMP) is ART558 (HY-141520) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. ART558 is a potent, selective and allosteric DNA polymerase theta (Polθ) inhibitor (IC50=7.9 nM). ART558 elicits BRCA-gene synthetic lethality and DNA damage. ART558 can be used for the research of cancer, such as breast cancer .
    ART558
  • HY-161083

    PARP Histone Methyltransferase Cancer
    PARP/EZH2-IN-2 (compound 12e) is a dual target PARP1 and EZH2 inhibitor, with IC50 values of 6.89 and 27.34 nM, respectively. PARP/EZH2-IN-2 shows anticancer activity, with no toxicity to normal cells. PARP/EZH2-IN-2 achieves synthetic lethality indirectly by inhibiting EZH2 to increase the sensitivity to PARP1, and induces cell death by regulating excessive autophagy .
    PARP/EZH2-IN-2
  • HY-B0824
    Bifenthrin
    1 Publications Verification

    Sodium Channel Neurological Disease
    Bifenthrin is a synthetic pyrethroid insecticide. Bifenthrin prolongs the opening time of Nav1.8 sodium channels, leading to membrane depolarization and conductance block in the insect nervous system, thereby disrupting neural function. Bifenthrin was effective in inhibiting A. gambiae (LD50=0.15 ng/mg) and C. quinquefasciatus (LD50=0.16 ng/mg). Bifenthrin has good lethality against susceptible and resistant mosquitoes and is very effective in inhibiting blood sucking and can be developed as a mosquito-removal netting material .
    Bifenthrin
  • HY-B0824R

    Sodium Channel Neurological Disease
    Bifenthrin (Standard) is the analytical standard of Bifenthrin. This product is intended for research and analytical applications. Bifenthrin is a synthetic pyrethroid insecticide. Bifenthrin prolongs the opening time of Nav1.8 sodium channels, leading to membrane depolarization and conductance block in the insect nervous system, thereby disrupting neural function. Bifenthrin was effective in inhibiting A. gambiae (LD50=0.15 ng/mg) and C. quinquefasciatus (LD50=0.16 ng/mg). Bifenthrin has good lethality against susceptible and resistant mosquitoes and is very effective in inhibiting blood sucking and can be developed as a mosquito-removal netting material .
    Bifenthrin (Standard)
  • HY-170824

    PROTACs Epigenetic Reader Domain Cancer
    SMD-3236 is a SMARCA2-targeted PRAOTAC degrader designed based on SMARCA ligands and VHL-1 ligands, with long-lasting antitumor activity in vivo. SMARCA2 is a synthetic lethal target in SMARCA4-deficient cancer cells, and SMD-3236 has a 2000-fold selectivity for degradation of SMARCA2 over SMARCA4, with a DC50< 1 nM and a Dmax>95%. SMD-3236 can induce SMARCA2 loss in tumor tissues while retaining SMARCA4 protein, and inhibit tumor growth in the H838 smarca4-deficient human cancer xenograft model. SMD-3236 is composed of target protein ligand (red part) SMI-1074 (HY-170817), PROTAC linker (black part) (trans-4-Ethynylcyclohexyl)methyl methanesulfonate (HY-170825), and E3 ligase ligand (blue part) SMARCA2 ligand-14 (HY-170826), of which the E3 ligase ligand and linker form a conjugate E3 Ligase Ligand-linker Conjugate 159 (HY-170827) .
    SMD-3236

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