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BRCA2-deficient

" in MedChemExpress (MCE) Product Catalog:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-124691
    D-I03
    3 Publications Verification

    		 DNA/RNA Synthesis Cancer
    D-I03 is a selective RAD52 inhibitor with a Kd of 25.8 μM. D-I03 specifically inhibits RAD52-dependent single-strand annealing (SSA) and D-loop formation with IC50s of 5 μM and 8 μM, respectively. D-I03 suppresses growth of BRCA1- and BRCA2-deficient cells and inhibits formation of damage-induced RAD52 foci, but does not effect on RAD51 foci induced by Cisplatin [2].
    D-I03
  • HY-177512
    MSC778

    		FLAP Cancer
    MSC778 is an effective and orally active flap endonuclease 1 (FEN1) inhibitor with an IC50 of 3 nM and a KD of 2.9 nM. MSC778 exhibits 145-fold, 516-fold, and 65-fold selectivity over EXO1, GEN1, and XPG, respectively. MSC778 selectively kills BRCA2-deficient cells and potentiates the activity of Niraparib (HY-10619) to induce tumor stasis in a BRCA2 KO DLD-1 mouse xenograft. MSC778 can be used in the research of colorectal cancer .
    MSC778
  • HY-170844
    MU147

    		Endonuclease Cancer
    MU147 is an MRE11 nuclease inhibitor and chemical probe with anticancer activity, which is lethal to Ehrlich ascites tumor cells both in vitro and in vivo. MU147 also eliminates the double-strand break repair mechanism dependent on the MRE11 nuclease activity without impairing the activation of ATM. MU147 also impairs the degradation of nascent strands of stalled replication FOX and selectively affects brca2-deficient cells .
    MU147
  • HY-158346
    RP-2119

    		DNA/RNA Synthesis Cancer
    RP-2119 is an orally bioactive Polymerase Theta (Polθ) inhibitor, with an IC50 of 0.7 nM against human Polθ ATPase. RP-2119 reduces Polθ activity and exerts antiproliferative effects in BRCA2-deficient cancer cells. RP-2119 exhibits antitumor activity in BRCA2-deficient cancer cell xenograft mouse models . RP-2119 can be used for the research of cancer and homologous recombination-deficient cancers, including brca1/brca2-mutant cancers and shld2-mutant cancers [2].
    RP-2119
  • HY-170845
    MU1409

    		Endonuclease Cancer
    MU1409 is an inhibitor of MRE11 nuclease with an IC50 of 12.1 μM. Additionally, MU1409 also inhibits FEN1 and EXO1, with IC50 values of 24.2 and 176.4 μM, respectively. MU1409 affects DNA repair in cells, preventing the degradation of stalled replication forks in BRCA2-deficient cells, making it a promising candidate for research on BRCA2 mutation-induced cancers .
    MU1409
  • HY-122583
    D-G23

    		RAD51 Cancer
    D-G23 is a selective RAD52 inhibitor. D-G23 disrupts RAD52-mediated DNA repair pathways and suppresses the growth of BRCA1- and BRCA2-deficient cancer cells. D-G23 is promising for research of homologous recombination-related cancers, such as hereditary breast cancer and ovarian cancer caused by BRCA1/2 mutations .
    D-G23
  • HY-181557
    SY-589

    		DNA Alkylator/Crosslinker DNA/RNA Synthesis Apoptosis Cancer
    SY-589 is an orally active DNA polymerase Polθ helicase domain inhibitor (IC50=2.29 nM) and DNA damage inducer. SY-589 inhibits the ATPase activity of the Polθ helicase domain and blocks the Polθ-mediated microhomology-mediated end joining (MMEJ) DNA repair pathway (IC50=0.85 nM). SY-589 also induces the accumulation of DNA double-strand breaks by increasing γ-H2AX levels. SY-589 exerts antiproliferative effects on BRCA2-deficient cells and is used in the research of HR-deficient tumors .
    SY-589
  • HY-182322
    POLQ-IN-1

    		DNA/RNA Synthesis Cancer
    POLQ-IN-1 is a DNA polymerase θ (POLQ) inhibitor with a pIC50 of 8.2. POLQ-IN-1 inhibits the proliferation of homologous recombination-deficient cells. POLQ-IN-1 is used for the research of homologous recombination-deficient tumors .
    POLQ-IN-1

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