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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
19 Results for "
HR repair
" in MedChemExpress (MCE) Product Catalog:
Products (19)
19 Results for "HR repair" in MCE Product Catalog:
6
6 Publications Verification
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PFM01, N-alkylated Mirin derivative, is a MRE11 endonuclease inhibitor. PFM01 can regulate double-strand break repair (DSBR) by nonhomologous end-joining (NHEJ) versus homologous recombination (HR) .
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5 Cited Publications
Synonyms: SHR3162; Fuzuloparib
Fluzoparib (SHR3162) is a potent and orally active PARP1 inhibitor (IC50=1.46±0.72 nM, a cell-free enzymatic assay) with superior antitumor activity. Fluzoparib selectively inhibits the proliferation of homologous recombination repair (HR)-deficient cells, and sensitizes both HR-deficient and HR-proficient cells to cytotoxic agents. Fluzoparib exhibits good pharmacokinetic properties in vivo and can be used for BRCA1/2-mutant relapsed ovarian cancer research .
Simmiparib is a highly potent and orally active PARP1 and PARP2 inhibitor with IC50 values of 1.75 nM and 0.22 nM, respectively. Simmiparib has more potent PARP1/2 inhibition than its parent Olaparib (HY-10162). Simmiparib induces DNA double-strand breaks (DSB) accumulation and G2/M arrest in homologous recombination repair (HR)-deficient cells, thereby inducing apoptosis. Simmiparib exhibits remarkable anticancer activities in cells and nude mice bearing xenografts .
Cat. No.: HY-162384
CAS No.: 3034959-68-4
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EPIC-0628 is an inhibitor of the HOTAIR-EZH2 interaction and promotes ATF3 expression. The long noncoding RNA HOTAIR has been found to regulate glioblastoma (GBM) progression and mediate DNA damage repair (DDR) by interacting with the catalytic subunit EZH2 of PRC2. EPIC-0628 also inhibits the ATF3-p38-E2F1 DDR pathway to inhibit the HR pathway and upregulates CDKN1A (p21) expression, causing cell cycle arrest. EPIC-0628 also synergizes with Temozolomide (TMZ) (HY-17364) to enhance its in vivo potency .
Cat. No.: HY-175812
CAS No.: 1208829-24-6
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MU876 (Compound 32) is a MUS81 inhibitor with an IC50 of 0.5 μM. MU876 effectively inhibits MUS81-dependent homologous recombination (HR) and break-induced replication (BIR) pathways. MU876 sensitizes cancer cells to DNA-damaging agents, such as Cisplatin (HY-17394), through impairing their ability to repair DNA lesions. MU876 can be used for cancers chemotherapy research .
Cat. No.: HY-144338
CAS No.: 2758117-74-5
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PARP1/BRD4-IN-1 is a potent and high selective PARP1/BRD4 inhibitor (IC50s of 49 and 202 nM in PARP1 and BRD4, respectively). PARP1/BRD4-IN-1 represses the expression and activity of PARP1 and BRD4 to synergistically inhibit the malignant growth of pancreatic cancer cells .
Cat. No.: HY-175466
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BER-IN-1 is a base excision repair (BER) inhibtor, targeting DNA abasic sites. BER-IN-1 cleaves abasic sites via β- and β,δ-elimination mechanisms, disrupts the base excision repair (BER) pathway and leads to DNA double-strand breaks (DSBs). BER-IN-1 can enhance the effectiveness of the PARP inhibitor Olaparib (HY-10162) in homologous recombination (HR)-proficient cancer cells (MDA-MB-231, HeLa, and SKOV3). BER-IN-1 induces an S-phase arrest and apoptosis companied with Olaparib (HY-10162). BER-IN-1 can be used for the research of cancer, such as breast, cervical and ovarian cancer .
Cat. No.: HY-126972
CAS No.: 1902146-75-1
RI(dl)-2 blocks RAD51’s D-loop activity in biochemical systems with an IC50 value of 11.1 µM and inhibits homologous recombination (HR) activity with an IC50 value of 3.0 µM. RI(dl)-2 inhibits HR-mediated repair of DNA double strand breaks and sensitizes different cancer cell lines .
Cat. No.: HY-146194
CAS No.: 2974448-39-8
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NHEJ inhibitor-1 (Compound C2) is a trifunctional Pt(II) complex, alleviates the non-homologous end connection (NHEJ)/homologous recombination (HR)-related double strand breaks (DSBs) repairs to evade Cisplatin-resistance in non-small cell lung cancer (NSCLC). NHEJ inhibitor-1 inhibits the damage repair proteins Ku70 and Rad51 to make tumors re-sensitive to Cisplatin. NHEJ inhibitor-1 also induces ROS generation and MMP deduction .
Cat. No.: HY-189225
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PP-048 is a selective dual inhibitor of Polθ/PARP1, with IC50 values of 4.9 nM and 6.8 nM for the Polθ helicase/ATPase domain and PARP1, respectively. PP-048 impairs the compensatory DNA repair capacity of homologous recombination-deficient cells by simultaneously inhibiting the DNA repair functions associated with Polθ and PARP1, thereby exacerbating DNA double-strand damage and inducing apoptosis. PP-048 exhibits more potent selective antiproliferative activity against HR-deficient cancer cells. PP-048 can be used in studies related to Polθ/PARP1 dual-target inhibition, synthetic lethality, DNA damage repair, and HR-deficient triple-negative breast cancer .
Cat. No.: HY-P85594
Synonyms: hHR 23b; hHR23B; HR 23B; HR23B; mHR 23B; mHR23B; P58; RAD 23B; RAD23; S. cerevisiae; homolog B; RAD23 homolog B; S. cerevisiae; RAD23 homolog B; RAD23 yeast homolog of B; RAD23B; RD23B_HUMAN; UV excision repair protein RAD23 homolog B; XP C repair complementing complex 58 kDa; XP C repair complementing complex 58 kDa protein; XP C repair complementing protein; XP-C repair-complementing complex 58 kDa protein; XPC repair complementing complex 58 kDa; XPC repair complementing complex 58 kDa protein; XPC repair complementing protein.
Cat. No.: HY-181611
CAS No.: 3068829-46-6
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Polθ-IN-10 is an orally active Polθ-pol inhibitor (with a human IC50 of 1.3 nM) that exhibits oral bioavailability in mice and rats. Polθ-IN-10 binds to the allosteric site of Polθ-pol, disrupts the microhomology-mediated end-joining DNA repair pathway, and inhibits CYP2C9 (IC50=1.63 μM). Polθ-IN-10 selectively inhibits the proliferation of HR-deficient cancer cells and induces apoptosis. Polθ-IN-10 is applicable to the research of HR-deficient cancers .
Cat. No.: HY-181840
CAS No.: 1846587-13-0
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MU262 is a MUS81 inhibitor with an IC50 value of 0.87 μM. MU262 directly inhibits the catalytic activity of MUS81 without interfering with DNA binding, induces genomic instability in tumor cells, and specifically inhibits the HR/BIR repair pathway. The combination of MU262 with Cisplatin (HY-17394) significantly enhances the chemotherapeutic killing effect. MU262 serves as a chemical biology tool for studying MUS81 function, and also acts as a lead compound for the development of anticancer therapies that exploit DNA repair defects in cancer cells .
Cat. No.: HY-181557
CAS No.: 3077714-09-8
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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 .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
