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Results for "

Polθ

" in MedChemExpress (MCE) Product Catalog:

23

阻害剤およびアゴニスト

1

蛍光色素

1

生化学アッセイ試薬

3

同位体標識化合物

製品番号 製品名 Target 研究分野 構造式
  • 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-150279
    PolQi2
    3 Publications Verification

    		 DNA/RNA Synthesis Others
    PolQi2 is a PolΘ inhibitor that targets and inhibits alt-EJ (alternative end-joining) repair by inhibiting the helicase domain at the N-terminus of PolΘ. PolQi2 enhances the precision and integration efficiency of gene editing at different loci and in various cell lines. Furthermore, the combined use of PolQi2 with DNA-PK inhibitors reduces the off-target effects of Cas9. PolQi2 can be used in gene editing research .
    PolQi2
  • HY-139289
    ART812
    3 Publications Verification

    		 DNA/RNA Synthesis Cancer
    ART812 is an orally active DNA polymerase Polθ inhibitor with an IC50 value of 7.6 nM. ART812 has an IC50 value of 240 nM for cell based microhomology-mediated end joining (MMEJ) .
    ART812
  • HY-151462
    RP-6685
    3 Publications Verification

    		 DNA/RNA Synthesis Cancer
    RP-6685 is a potent, selective and orally active DNA polymerase theta (Polθ) inhibitor with an IC50 value of 5.8 nM (PicoGreen assay). RP-6685 shows antitumor efficacy in mouse tumor xenograft model . RP-6685 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    RP-6685
  • HY-159078
    PolQi1

    		DNA/RNA Synthesis Cancer
    PolQi1 is a selective inhibitor targeting the Polθ domain of DNA polymerase. PolQi1 inhibits the Polθ-mediated microhomology end joining (TMEJ/alt-EJ) pathway, reducing insertion/deletion (Indels) and imprecise editing events during DNA repair. PolQi1 can enhance the efficiency and accuracy of homology-directed repair (HDR) or Prime editing, and reduce off-target effects; and in combination with DNA-PK inhibitor AZD-7648 (HY-111783), exert efficient genome editing capabilities with dual pathway regulation. PolQi1 can be mainly used in gene editing research (such as CRISPR-Cas9 or Prime editing system optimization) to improve the precision editing efficiency of difficult-to-edit cells (such as primary hepatocytes and mouse embryos) .
    PolQi1
  • HY-161302
    Polθ/PARP-IN-1

    		Apoptosis DNA/RNA Synthesis PARP Cancer
    Polθ/PARP-IN-1 (compound 25d) is a potent dual DNA polymerase theta (Polθ) and PARP inhibitor with IC50 values of 45.6, 5.4 nM, respectively. Polθ/PARP-IN-1 shows antiproliferative activity. Polθ/PARP-IN-1 induces apoptosis and cell cycle arrest at G2/M phase, causes DNA damage. Polθ/PARP-IN-1 shows anti-tumor activity .
    Polθ/PARP-IN-1
  • HY-162859
    AB25583
    1 Publications Verification

    		 DNA/RNA Synthesis Cancer
    AB25583 is a Polθ helicase (Polθ-hel) small molecule inhibitor, with an IC50 value of 6 nM. AB25583 selectively kills BRCA1/2 deficient cells and works in synergy with Olaparib (HY-10162) in cancer cells carrying pathogenic BRCA1/2 mutations. AB25583 can be used for tumor research .
    AB25583
  • HY-171421
    Polθ-IN-8

    		DNA/RNA Synthesis Cancer
    Polθ-IN-8 (example 77) is a DNA polymerase theta (Polθ) inhibitor with an c of <100 nM for Polθ ATPase activity. Polθ-IN-8 can be used to study diseases related to Polθ activity (such as cancer) .
    Polθ-IN-8
  • HY-145056
    ART615

    		DNA/RNA Synthesis Cancer
    ART615 is the related isomer of ART558. ART615, the inactive of ART558, elicits <10% Polθ inhibition at 12 µM, thus serving as a control for ART558 (IC50=7.9 nM) .
    ART615
  • 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 .
    RP-2119
  • HY-161916
    Polθ-IN-4

    		DNA/RNA Synthesis Cancer
    Polθ-IN-4 is an orally active prodrug of a DNA polymerase θ (Polθ) inhibitor with Kms of 3.7, 3.7 and 5.2 μM in human, mouse and rat recombinant alkaline phosphatases. Polθ-IN-4 that inhibits Polθ activity by targeting its ATP-dependent helicase domain. Polθ-IN-4 demonstrates significant anti-tumor activity in multiple animal experiments. Polθ-IN-4 can be used for the studies of breast cancer and ovarian cancer .
    Polθ-IN-4
  • HY-161431
    RTx-152

    		DNA/RNA Synthesis Cancer
    RTx-152 traps Polθ on DNA and is an allosteric Polθ-pol inhibitor (IC50: 6.2 nM). RTx-152 selectively kills HR-deficient cancer cells, and suppresses PARP inhibitor resistance in multiple genetic backgrounds, including homologous recombination (HR)-proficient cells. RTx-152 selectively kills BRCA2-null cells .
    RTx-152
  • HY-153755
    Polθ-IN-7

    		DNA/RNA Synthesis Cancer
    Polθ-IN-7 (example 12) is a DNA polymerase theta (Polθ) inhibitor with a Ki of 1.27 nM .
    Polθ-IN-7
  • HY-169284
    Polθ-IN-5

    		DNA/RNA Synthesis Cancer
    Polθ-IN-5 (Compound 139) is a DNA polymerase theta (Polθ) inhibitor. Polθ-IN-5 has antitumor activity .
    Polθ-IN-5
  • HY-169285
    Polθ-IN-6

    		DNA/RNA Synthesis Cancer
    Polθ-IN-6 (Compound 89) is a DNA polymerase theta (Polθ) inhibitor. Polθ-IN-6 has antitumor activity .
    Polθ-IN-6
  • HY-179219S
    RTx-303

    		DNA/RNA Synthesis Cancer
    RTx-303 is an orally active, selective DNA polymerase θ (Polθ) inhibitor (IC50 = 5.1 nM). RTx-303 exhibits significantly high cellular potency and strongly potentiates PARPi in BRCA1/2 mutant cells and patient-derived xenograft models. RTx-303 can be used for the study of BRCA2-mutated breast cancer .
    RTx-303
  • HY-139289S
    ART899

    		DNA/RNA Synthesis Cancer
    ART899 is a highly specific allosteric inhibitor of the Polθ DNA polymerase domain. ART899 can effectively enhance the radiosensitivity of tumor cells, shows good tolerance when combined with fractionated radiation, and significantly reduces tumor growth compared to radiation alone .
    ART899
  • 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-139593S
    Polθ-IN-1-d3

    		Isotope-Labeled Compounds Cancer
    Polθ-IN-1-d3 (example 1) is a deuterated Polθ inhibitor used for cancer study (extracted from patent WO2021028670) .
    Polθ-IN-1-d3
  • HY-179413
    Polθ-IN-9

    		DNA/RNA Synthesis Cancer
    Polθ-IN-9 is an orally active Polθ polymerase inhibitor (IC50 = 9.6 nM, Kd = 47.5 nM). Polθ-IN-9 shows remarkable selectivity with no inhibitory activity against other human DNA polymerases, including Pol α, Pol ε, Pol γ, Pol λ, and Pol μ. Polθ-IN-9 exhibits strong antiproliferative activity in DLD1 BRCA2 KO cells (IC50 = 2.9 μM), and high sensitivity to MDA-MB-436 cells (IC50 = 4.9 μM). Polθ-IN-9 increases DNA damage accumulation, induces γH2AX levels, and inhibits tumor growth in combination with Olaparib (HY-10162), in the MDA-MB-436 xenograft model. Polθ-IN-9 can be used for the research of homologous recombination (HR)-deficient cancers such as breast cancer .
    Polθ-IN-9
  • 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-181611
    Polθ-IN-10

    		DNA/RNA Synthesis Apoptosis Cytochrome P450 Cancer
    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 .
    Polθ-IN-10
  • HY-183748
    XL-20

    		DNA/RNA Synthesis PD-1/PD-L1 IKK STAT STING Cancer
    XL-20 is an orally active DNA polymerase θ (Polθ) ATPase inhibitor with an IC50 of 4.3 nM against human targets. XL-20 activates the cGAS-STING pathway. XL-20 upregulates the expression of PD-L1 in HR-deficient cancer cells. XL-20 acts synergistically with PARP inhibition in HR-deficient cancer cells and in vivo xenograft models. XL-20 can be used in studies related to HR-deficient cancers .
    XL-20

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