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Results for "

synthetic lethality

" in MedChemExpress (MCE) Product Catalog:

14

Inhibitors & Agonists

2

Peptides

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-N4115
    Syrosingopine
    4 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
    3 Publications Verification

    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-131493
    PF-06939999

    PRMT5-IN-3

    		 Histone Methyltransferase Cancer
    PF-06939999 (PRMT5-IN-3) is a PRMT5 inhibitor that exhibits synthetic lethality to tumor cells but produce few side effects combined with DNA damaging agents.
    PF-06939999
  • HY-112626
    CDK12-IN-2

    		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
    PP-C8

    		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-158116
    VVD-214

    RO7589831; VVD-133214

    		 DNA/RNA Synthesis Cancer
    VVD-214 is a synthetic lethal allosteric inhibitor of WRN helicase. 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-153361
    YD23

    		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-145268
    SLEC-11

    		Others Cancer
    SLEC-11 acts as a potential synthetic lethal lead for the research of gastric cancer. AL-GDa62 shows EC50 of 12.2 μM and 8.2 μM for isogenic mammary epithelial cells MCF10A-WT (wild-type) and MCF10A-CDH1 -/- .
    SLEC-11
  • HY-145269
    AL-GDa62

    		Others Cancer
    AL-GDa62 acts as a potential synthetic lethal lead for the research of gastric cancer. AL-GDa62 shows EC50 of 3.2 μM and 2 μM for isogenic mammary epithelial cells MCF10A-WT (wild-type) and MCF10A-CDH1 -/- .
    AL-GDa62
  • HY-149952
    ATR-IN-23

    		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-149887
    H3B-968

    		DNA/RNA Synthesis Cancer
    H3B-968 is a potent inhibitor of Werner syndrome protein (WRN) (IC50=~10 nM)，which acts function as helicase，ATPase，and exonuclease. WRN exhibits synthetic lethal activity in cancer research. However，H3B-968 inhibits WRN helicase activity，competitively with ATP .
    H3B-968
  • HY-161083
    PARP/EZH2-IN-2

    		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
    Bifenthrin (Standard)

    		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)

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