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Results for "

synthetic lethality

" in MedChemExpress (MCE) Product Catalog:

31

Inhibitors & Agonists

1

Fluorescent Dyes

1

Biochemical Assay Reagents

2

Peptides

1

GMP Molecules

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-132167
    Saruparib
    15+ 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
    49 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-N4115
    Syrosingopine
    10+ Cited Publications

    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-158116
    VVD-214

    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-159607
    PRT3789

    		PROTACs SWI/SNF Complex Cancer
    PRT3789 is a selective SMARCA2 PROTAC degrader (DC50 in HeLa cell: 0.72 nM for SMARCA2, 14 nM for SMARCA4). PRT3789 forms a stable ternary complex with Von Hippel-Lindau (VHL) E3 ligase, induces polyubiquitination at SMARCA2-specific lysine residues, and drives proteasome-dependent SMARCA2 degradation. PRT3789 disrupts SWI/SNF chromatin remodeling complex integrity, induces dissociation of specific subunits, suppresses oncogenic gene expression, reduces chromatin accessibility, and upregulates antigen processing/presentation-related gene expression. PRT3789 induces synthetic lethality, inhibits proliferation and colony formation, and drives tumor growth inhibition and regression in SMARCA4-deficient contexts. PRT3789 can be used for the research of SMARCA4-mutated solid tumors, non-small cell lung cancer, endometrial cancer, colorectal cancer, bladder cancer, esophageal cancer, ovarian cancer, and gastric cancer .
    PRT3789
  • HY-B0824
    Bifenthrin
    1 Publications Verification

    		 Environmental Pollutants 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-153361
    YD23

    		PROTACs Epigenetic Reader Domain Inflammation/Immunology Cancer
    YD23 is a selective SMARCA2 PROTAC degrader with DC50 values of 64 nM and 297 nM in H1792 cells and H1975 cells. YD23 induces degradation of SMARCA2, which is synthetic lethal to SMARCA4. YD23 reduces chromatin accessibility only in SMARCA4 deficient cells, including cell cycle and cell growth regulatory genes. YD23 selectively inhibits growth of SMARCA4 mutant lung cancer cells. YD23 has potent tumor growth inhibitory activity in SMARCA4-mutant xenografts. YD23 can be used for the study of non-small cell lung cancer (NSCLC) .
    YD23
  • HY-112626
    CDK12-IN-2
    1 Publications Verification

    		 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-162386
    UM4118

    		Cuproptosis Mitochondrial Metabolism Cancer
    UM4118 is a potent copper-selective non-genotoxic copper ionophore that induces cuproptosis in acute myeloid leukemia cells. UM4118 exhibits stronger activity against SF3B1G12C mutant acute myeloid leukemia cells. UM4118 transports extracellular copper into cells, elevates intracellular and mitochondrial copper levels, and triggers lipoylated DLAT aggregation, proteotoxic stress, iron-sulfur cluster protein depletion, reduced lipoylated protein levels, and maximal mitochondrial respiratory damage. UM4118 cytotoxicity can be enhanced by supplementation with extracellular copper, abolished by copper chelation, and shows synthetic lethal effects in the absence of iron-sulfur cluster biosynthesis/transport genes. UM4118 can be used for the study of acute myeloid leukemia .
    UM4118
  • 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-153338
    C791-0064

    		DNA/RNA Synthesis Apoptosis Cancer
    C791-0064 is a RAD52 inhibitor. C791-0064 specifically binds to RAD52 and disrupts its single-strand annealing activity. C791-0064 specifically inhibits the proliferation of cancer cells with BRCA2 deficiency, inducing DNA damage and apoptosis (apoptosis). C791-0064 can be used for the study of BRCA mutation-related cancers (such as breast cancer and ovarian cancer) .
    C791-0064
  • HY-P3912A
    Endotoxin inhibitor TFA

    		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-N4115R
    Syrosingopine (Standard)

    Su 3118 (Standard)

    		 Reference Standards 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 (Standard)
  • HY-145268
    SLEC-11

    		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
    Endotoxin inhibitor

    		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
    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-178511
    KIF18A-IN-17

    		Kinesin Cancer
    KIF18A-IN-17 (Example 37A) is a KIF18A inhibitor with racemic form with an IC50 of 48 nM. KIF18A-IN-17 exhibits anti-proliferative activity against HT29 cells. KIF18A-IN-17 can be used for the study of cancers such as breast cancer and ovarian cancer .
    KIF18A-IN-17
  • HY-174217
    WRN-IN-19

    		DNA/RNA Synthesis Cancer
    WRN-IN-19 (Compound (S)-27) is a covalent WRN helicase inhibitor, with pIC50 (0 h/4 h) = 5.4/7.5 in the DNA-unwinding 5 endpoint assays. WRN-IN-19 shows synthetic lethality in MSI-H (high microsatellite instability) cancer cells .
    WRN-IN-19
  • HY-153141
    MP-1

    		RNA MTase Cancer
    MP-1 is a potent Fumarate hydratase-dependent hit. MP-1 engages an array of functional cysteines, including one lying in the Zn-finger domain of the tRNA methyltransferase enzyme TRMT1. MP-1 causes fumarate hydratase-dependent synthetic lethality in a metastatic hereditary leiomyomatosis and renal cell carcinoma cell line .
    MP-1
  • HY-141520G
    ART558

    		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/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-145269
    AL-GDa62

    		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-B0824R
    Bifenthrin (Standard)

    		Reference Standards 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-182313
    WRN-IN-25

    		DNA/RNA Synthesis Cancer
    WRN-IN-25 is an allosteric Werner syndrome helicase (WRN) inhibitor with an IC50 of 15 nM and a Kd of 54 nM. WRN-IN-25 induces DNA damage, reduces cell viability, and exhibits synthetic lethality in WRN-driven high microsatellite instability cancer cells. WRN-IN-25 can be used in research related to microsatellite instability cancers .
    WRN-IN-25
  • HY-181561
    BRCA2-RAD51-IN-3

    		RAD51 Cancer
    BRCA2-RAD51-IN-3 is a RAD51-BRCA2 protein-protein interaction inhibitor with an EC50 of 29.35 μM and a Kd of 75.14 μM. BRCA2-RAD51-IN-3 blocks RAD51-BRCA2 binding, impairs homologous recombination in cancer cells, and induces synthetic lethality. BRCA2-RAD51-IN-3 acts in human pancreatic cancer cells and shows no activity in normal pancreatic cells. BRCA2-RAD51-IN-3 can be used for the research of pancreatic cancer .
    BRCA2-RAD51-IN-3
  • HY-185459
    PCIP-1

    		PARP Epigenetic Reader Domain Cancer
    PCIP-1 is a PARP2 inhibitor. PCIP-1 recruits BET proteins to PARP2 to inhibit DNA repair, acts via event-driven pharmacology, and does not inhibit PARP-catalyzed PARylation. PCIP-1 inhibits DNA repair, thereby inducing synthetic lethality in homologous recombination-deficient cancer cells and increasing the sensitivity of PARP1-knockout cells. PCIP-1 can be used in the research of homologous recombination-deficient cancers, T-cell acute lymphoblastic leukemia, and BRCA-mutant cancers .
    PCIP-1
  • HY-181440
    TDG-IN-1

    		DNA Glycosylase DNA/RNA Synthesis Cancer
    TDG-IN-1 is an orally active, selective small-molecule inhibitor of thymine DNA glycosylase (TDG) with a Ka of 1.46 nM. TDG-IN-1 impairs the DNA-binding ability of TDG, induces downregulated expression of DHX9, accumulation of double-stranded RNA, and activation of the RIG-I/MDA5-MAVS pathway, while acting as a tumor suppressor, innate immune activator and immunostimulant. TDG-IN-1 inhibits the growth of p53-deficient tumor cells and xenograft tumors, and exerts a synthetic lethal effect with p53. TDG-IN-1 is applicable to the research of p53-deficient cancers .
    TDG-IN-1
  • HY-180484
    PKMYT1-IN-12

    		Wee1 CDK Ligands for Target Protein for PROTAC Cancer
    PKMYT1-IN-12 (Compound 4) is a selective inhibitor of PKMYT1, with an IC₅₀ of 2.6 nM. PKMYT1-IN-12 can effectively inhibit the phosphorylation of CDK1, with an IC₅₀ of 44 nM. PKMYT1-IN-12 is a target protein ligand that can be used for the synthesis of PROTAC D16-M1P2 (HY-180485) .
    PKMYT1-IN-12
  • HY-180485
    PROTAC D16-M1P2

    		PROTACs Wee1 CDK Cancer
    PROTAC D16-M1P2 is an orally active PKMYT1 PROTAC degrader with a DC50 of 0.7 nM. PROTAC D16-M1P2 also inhibits the activity of PKMYT1 with an IC50 of 7.6 nM. PROTAC D16-M1P2 inhibits pCDK1 with an IC50 of 9 nM. PROTAC D16-M1P2 has demonstrated significant anti-tumor efficacy in mouse models and can be used for research on breast cancer .
    PROTAC D16-M1P2
  • HY-185075
    FHD-909

    LY4050784

    		 SWI/SNF Complex Cancer
    FHD-909 (LY4050784) is an orally active and selective SMARCA2 (BRM) ATPase inhibitor. FHD-909 potently inhibits purified BRM ATPase with an IC50 of 0.0025 μM and exhibits 35.69-fold selectivity for BRM over purified SMARCA4 (BRG1) ATPase. FHD-909 induces synthetic lethality, suppresses cell proliferation, modulates target gene expression, and achieves remarkable tumor growth inhibition and regression in SMARCA4-mutant cancer cells and xenograft models. FHD-909 can be used for the research of SMARCA4/BRG1-mutant cancers, advanced solid tumors, and BAF complex-related disorders .
    FHD-909
  • HY-183118
    CID-078

    		CDK Apoptosis Neurological Disease Cancer
    CID-078 is an orally active macrocyclic cyclin A and cyclin B inhibitor. CID-078 binds cyclin hydrophobic patches, disrupting interactions of cyclin A-Cdk2 with E2F1 and cyclin B-Cdk1 with Myt1, and selectively targets RxL binding motifs to block complex-substrate interactions. CID-078 induces DNA damage, G2/M cell cycle arrest, apoptosis, mitotic catastrophe, spindle assembly checkpoint activation, and neomorphic cyclin B-CDK2 complex formation, driving synthetic lethality in E2F-driven cancer cells. CID-078 can be used for the research of small cell lung cancer, non-small cell lung cancer, triple negative breast cancer, advanced solid tumors, luminal HR +/HER 2- breast cancer, RB1-altered solid tumors, and neuroblastoma .
    CID-078

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