Scientific Reviews
Product Guides
Blogs
Topics
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
21 Results for "
DNA polymerase theta
" in MedChemExpress (MCE) Product Catalog:
Products (21)
21 Results for "DNA polymerase theta" in MCE Product Catalog:
52
52 Publications Verification
Target:
Research Areas:
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 .
4
4 Cited Publications
Target:
Research Areas:
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) .
3
3 Cited Publications
Target:
Research Areas:
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.
Target:
Research Areas:
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) .
Cat. No.: HY-161302
CAS No.: 3056709-95-3
Target:
Research Areas:
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 .
Cat. No.: HY-161430
CAS No.: 3035072-49-9
Target:
Research Areas:
RTx-161 is a DNA polymerase θ inhibitor with an IC50 of 4.1 nM. RTx-161 induces DNA damage, PARP cleavage, apoptosis, and selectively kills homologous recombination-deficient (HRD) cells. RTx-161 acts synergistically with PARP inhibitors to suppress PARP inhibitor resistance in cancer cells. RTx-161 can be used for the research of BRCA G12C mutant cancer and HR-deficient cancers .
Cat. No.: HY-171421
CAS No.: 3056743-98-4
Target:
Research Areas:
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) .
Cat. No.: HY-161916
CAS No.: 3043810-73-4
Target:
Research Areas:
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 .
Cat. No.: HY-179219S
CAS No.: 3035072-99-9
Cat. No.: HY-139289S
CAS No.: 2607139-85-3
Cat. No.: HY-153755
CAS No.: 2923356-52-7
Synonyms: Polθ-IN-7
Target:
Research Areas:
ART6043 (Polθ-IN-7) is an orally active, selective allosteric DNA polymerase θ (Polθ) inhibitor with an IC50 of 1.3 nM. ART6043 blocks microhomology-mediated end joining (MMEJ) by inhibiting the polymerase function of Polθ. ART6043 suppresses the survival of homologous recombination-deficient (HRD) cells and enhances the antitumor effects of PARP inhibitors. ART6043 can be used in studies of HRD tumors, including BRCA1-mutant triple-negative breast cancer, BRCA2-deficient colorectal cancer, RAD51C-deficient gastric cancer, and others .
Cat. No.: HY-169284
CAS No.: 3058636-12-4
Target:
Research Areas:
Polθ-IN-5 (Compound 139) is a DNA polymerase theta (Polθ) inhibitor. Polθ-IN-5 has antitumor activity .
Cat. No.: HY-169285
CAS No.: 3058496-94-6
Target:
Research Areas:
Polθ-IN-6 (Compound 89) is a DNA polymerase theta (Polθ) inhibitor. Polθ-IN-6 has antitumor activity .
Cat. No.: HY-141520G
CAS No.: 2603528-97-6
Cat. No.: HY-182322
CAS No.: 3109024-27-0
Target:
Research Areas:
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 .
Cat. No.: HY-183748
CAS No.: 3082173-75-6
Target:
Research Areas:
Polθ-IN-11 is an orally active DNA polymerase θ (Polθ) ATPase inhibitor with an IC50 of 4.3 nM against human targets. Polθ-IN-11 activates the cGAS-STING pathway. Polθ-IN-11 upregulates the expression of PD-L1 in HR-deficient cancer cells. Polθ-IN-11 acts synergistically with PARP inhibition in HR-deficient cancer cells and in vivo xenograft models. Polθ-IN-11 can be used in studies related to HR-deficient cancers .
Cat. No.: HY-P703612
Purity: ≥ 90%, as determined by reducing SDS-PAGE.
Synonyms: POLQ; DNA polymerase Eta; DNA polymerase theta; PRO0327; POLH; polymerase (DNA Directed), theta, Isoform CRA_c; polymerase (DNA Directed), theta; Epididymis Secretory Sperm Binding Protein; polymerase (DNA) theta
Species:
Human
Source:
Sf9 insect cells
Cat. No.: HY-181557
CAS No.: 3077714-09-8
Research Areas:
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 .
Cat. No.: HY-183630
CAS No.: 3045469-78-8
Target:
Research Areas:
AZD4956 is a potent and selective DNA polymerase theta (POLQ) inhibitor. AZD4956 exhibits an IC50 value of less than 3 μmol/L against POLQ and 3.4 μmol/L against MMEJ. AZD4956 suppresses the MMEJ pathway and enhances the activity of DNA-damaging agents in HRR-deficient cellular contexts. AZD4956 shows antitumor activity in BRCA1/2-mutated triple-negative breast cancer and prostate cancer models. AZD4956 can be used for the study of homologous recombination-deficient tumors .
Cat. No.: HY-187358
Target:
Research Areas:
Polθ-IN-12 is a DNA polymerase θ (PolQ) polymerase domain inhibitor with a human pIC50 of 8.3. Polθ-IN-12 binds to the allosteric pocket of the PolQ polymerase domain, forming salt bridge interactions with residues Arg-2347 and Arg-2419. Polθ-IN-12 displays improved human metabolic stability and high kinetic solubility at pH 7.4. Polθ-IN-12 shows low CACO-2 permeability and acts as a modest efflux substrate .
- 1
- 2
-
-
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
