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Results for "

polymerase+theta

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (2) DNA/RNA Synthesis (15) IKK (1) PARP (2) PD-1/PD-L1 (1) STAT (1) STING (1)
By Research Areas:	Cancer (15)

Inhibitors & Agonists

Fluorescent Dyes

Biochemical Assay Reagents

Isotope-Labeled Compounds

GMP Molecules

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-141520

ART558 45+ Cited Publications	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 .

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.

HY-161430

RTx-161	DNA/RNA Synthesis Apoptosis PARP	Cancer
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 .

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 .

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 .

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) .

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 K_ms 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 .

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 .

HY-153755

Polθ-IN-7	DNA/RNA Synthesis	Cancer
Polθ-IN-7 (example 12) is a *DNA polymerase theta* (Polθ) inhibitor with a K_i** of 1.27 nM .

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 .

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 .

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 .

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 .

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 .

HY-183630

AZD4956	DNA/RNA Synthesis	Cancer
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 .

ART558	Fluorescent Dyes
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	Biochemical Assay Reagents
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 .

Cat. No.	Product Name	Chemical Structure

HY-179219S

RTx-303
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 .

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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 .

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BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.

BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

MedchemExpress Validation 03

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred

MedchemExpress Validation 04

MedchemExpress Validation

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