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
24 Results for "
Polθ
" in MedChemExpress (MCE) Product Catalog:
Products (24)
24 Results for "Polθ" 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:
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 .
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.
1
1 Cited Publications
Cat. No.: HY-162859
CAS No.: 2565637-94-5
Target:
Research Areas:
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 .
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-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) .
Target:
Research Areas:
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) .
Cat. No.: HY-158346
CAS No.: 2922287-81-6
Target:
Research Areas:
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 .
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-161431
CAS No.: 3035072-48-8
Target:
Research Areas:
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 .
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-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-141520G
CAS No.: 2603528-97-6
Cat. No.: HY-139593S
CAS No.: 2598122-35-9
Cat. No.: HY-179413
CAS No.: 3050552-13-8
Target:
Research Areas:
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 .
- 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
