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Results for "

Pol�� Inhibitors

" in MedChemExpress (MCE) Product Catalog:

By Targets:	ADC Payload (1) Antibiotic (1) Apoptosis (15) Bacterial (5) Bcl-2 Family (3) c-Myc (3) Caspase (3) CDK (10) Cytochrome P450 (1) DNA Alkylator/Crosslinker (1) DNA/RNA Synthesis (51) Drug Intermediate (6) Drug Isomer (2) DYRK (2) Elastase (2) Environmental Pollutants (1) HIV (9) HIV Protease (8) HSV (1) IKK (1) Isotope-Labeled Compounds (4) MDM-2/p53 (1) Monoamine Oxidase (3) NF-κB (3) PARP (4) PD-1/PD-L1 (1) PI3K (1) Pyroptosis (1) Reference Standards (4) Reverse Transcriptase (1) STAT (1) STING (1) TNF Receptor (3)
By Research Areas:	Cancer (52) Infection (17) Inflammation/Immunology (6) Metabolic Disease (1) Neurological Disease (1)

By Targets:

ADC Payload (1)

Antibiotic (1)

Apoptosis (15)

Bacterial (5)

Bcl-2 Family (3)

c-Myc (3)

Caspase (3)

CDK (10)

Cytochrome P450 (1)

DNA Alkylator/Crosslinker (1)

DNA/RNA Synthesis (51)

Drug Intermediate (6)

Drug Isomer (2)

DYRK (2)

Elastase (2)

Environmental Pollutants (1)

HIV (9)

HIV Protease (8)

HSV (1)

IKK (1)

Isotope-Labeled Compounds (4)

MDM-2/p53 (1)

Monoamine Oxidase (3)

NF-κB (3)

PARP (4)

PD-1/PD-L1 (1)

PI3K (1)

Pyroptosis (1)

Reference Standards (4)

Reverse Transcriptase (1)

STAT (1)

STING (1)

TNF Receptor (3)

By Research Areas:

Cancer (52)

Infection (17)

Inflammation/Immunology (6)

Metabolic Disease (1)

Neurological Disease (1)

Inhibitors & Agonists

Fluorescent Dyes

Biochemical Assay Reagents

Peptides

Natural
Products

Isotope-Labeled Compounds

GMP Molecules

Targets Recommended: Serpin

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-12484

BMH-21 10+ Cited Publications	DNA/RNA Synthesis	Cancer
BMH-21 is a first-in-class DNA intercalator which inhibits RNA polymerase I (Pol I) transcription. BMH-21 possesses anticancer activity .

HY-X0009

Tambiciclib 1 Publications Verification GFH009; JSH-009; SLS009	CDK DYRK Apoptosis Bcl-2 Family c-Myc Caspase PARP DNA/RNA Synthesis	Metabolic Disease Inflammation/Immunology Cancer
Tambiciclib (GFH009, JSH-009) is an orally active, highly potent and selective CDK9 inhibitor (IC₅₀ = 1 nM), demonstrating >200-fold selectivity over other CDKs, >100-fold selectivity over DYRK1A/B, and excellent selectivity over 468 kinases/mutants. Tambiciclib demonstrates potent in vitro and in vivo antileukemic efficacy in acute myeloid leukemia (AML) mouse models by inhibiting *RNA Pol* II phosphorylation, downregulating MCL1 and MYC, and inducing apoptosis**. Tambiciclib can be used for AML research .

HY-122122

ML-60218 5+ Cited Publications	DNA/RNA Synthesis	Infection Cancer
ML-60218 is a broad-spectrum *RNA pol* III** inhibitor, with IC₅₀s of 32 and 27 μM for Saccharomyces cerevisiae and human. ML-60218 disrupts already assembled viroplasms and to hamper the formation of new ones without the need for de novo transcription of cellular RNAs .

HY-126214

JH-RE-06 4 Publications Verification	DNA/RNA Synthesis	Cancer
JH-RE-06, a potent REV1-REV7 interface inhibitor (IC₅₀=0.78 μM; K_d=0.42 μM), targets REV1 that interacts with the REV7 subunit of POLζ. JH-RE-06 disrupts mutagenic translesion synthesis (TLS) by preventing recruitment of mutagenic POLζ. JH-RE-06 improves chemotherapy .

HY-78726

Fosamprenavir 4 Publications Verification Amprenavir phosphate; GW 433908	Drug Intermediate HIV HIV Protease	Infection
Fosamprenavir is an orally active inhibitor targeting HIV-1 protease and is a prodrug of Amprenavir (HY-17430). Fosamprenavir is hydrolyzed into Amprenavir (VX-478) by cell phosphatases in the intestinal epithelium. Amprenavir binds to the active site of HIV-1 protease, preventing the processing of viral gag and gag-pol polyprotein precursors, thereby inhibiting the formation of mature infectious virus particles and exerting anti-HIV-1 infection activity. Fosamprenavir can be used for the study of human immunodeficiency virus (HIV-1) infection .

HY-103019A

(±)-Enitociclib (±)-BAY-1251152; (±)-VIP152	CDK Apoptosis DNA/RNA Synthesis	Cancer
(±)-Enitociclib ((±)-BAY-1251152) is the racemic mixture of Enitociclib (HY-103019E). Enitociclib is a selective CDK9 inhibitor and apoptosis inducer. Enitociclib inhibits CDK9 activity and reduces the phosphorylation of Ser2 in the carboxyl-terminal domain (CTD) of *RNA polymerase Pol* II, thereby downregulating the transcription of key oncogenes such as MYC and MCL1**. Enitociclib has anti-proliferative activity targeting MYC ⁺ lymphoma and multiple myeloma (MM) cells, and has synergistic effects with Bortezomib (HY-10227) and Lenalidomide (HY-A0003), and can be used in the research of hematological malignancies .

HY-13323A

CX-5461 dihydrochloride Maximum Cited Publications 66 Publications Verification	DNA/RNA Synthesis	Cancer
CX-5461 dihydrochloride is a potent and orally bioavailable inhibitor of Pol I-mediated rRNA synthesis, with IC₅₀s of 142 nM in HCT-116, 113 nM in A375, and 54 nM in MIA PaCa-2 cells, and shows little or no effect on Pol II (IC₅₀ ≥25 μM).

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) .

HY-14776

Quarfloxin 5+ Cited Publications CX-3543	DNA/RNA Synthesis	Cancer
Quarfloxin (CX-3543), a fluoroquinolone derivative with antineoplastic activity, targets and inhibits *RNA pol* I** activity, with IC₅₀ values in the nanomolar range in neuroblastoma cells. Quarfloxin disrupts the interaction between the nucleolin protein and a G-quadruplex DNA structure in the ribosomal DNA (rDNA) template .

HY-120118

Metarrestin ML246	DNA/RNA Synthesis	Cancer
Metarrestin (ML246) is an orally active, first-in-class and specific perinucleolar compartment inhibitor. Metarrestin disrupts the nucleolar structure and inhibits *RNA polymerase (Pol) I* transcription, at least in part by interacting with the translation elongation factor eEF1A2. Metarrestin blocks metastatic development and extends survival in mouse cancer models .

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) .

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-123972

SEC inhibitor KL-2 1 Publications Verification KL-2	DNA/RNA Synthesis	Cancer
SEC inhibitor KL-2 (KL-2), a peptidomimetic lead compound, is a potent, selective super elongation complex (SEC) inhibitor and disrupts the interaction between the SEC scaffolding protein AFF4 and P-TEFb, resulting in impaired release of Pol II from promoter-proximal pause sites and a reduced average rate of processive transcription elongation. SEC inhibitor KL-2 exhibits an dose-dependent inhibitory effect on AFF4-CCNT1 interaction with a Ki of 1.50 μM .

HY-W015490

1,4-Naphthoquinone 3 Publications Verification	Environmental Pollutants DNA/RNA Synthesis NF-κB Monoamine Oxidase TNF Receptor Bacterial	Infection Inflammation/Immunology Cancer
1,4-Naphthoquinone is an inhibitor with broad-spectrum inhibitory activity targeting DNA polymerase, NF-κB and monoamine oxidase (MAO-A/B), with antibacterial and anti-biofilm efficacy. 1,4-Naphthoquinone is a competitive inhibitor of MAO-B (Ki=1.4 μM) and a non-competitive inhibitor of MAO-A (Ki=7.7 μM). 1,4-Naphthoquinone inhibits DNA polymerase pol α, β, γ, δ, ε, λ with IC₅₀ ranging from 5.57-128 μM. 1,4-Naphthoquinone inhibits tumor cell proliferation, induces apoptosis and necrosis, and has anti-angiogenic and anti-inflammatory activities by inducing oxidative stress, depleting glutathione (GSH), inhibiting DNA polymerase-mediated DNA synthesis and blocking NF-κB nuclear translocation. 1,4-Naphthoquinone can be used in anti-bacterial , anti-tumor and anti-inflammatory studies, including inhibition of melanoma and colon cancer cell growth and endothelial cell function, as well as LPS-induced inflammation models .

HY-N2566

Euscaphic acid 1 Publications Verification	DNA/RNA Synthesis PI3K Apoptosis	Cancer
Euscaphic acid, a DNA polymerase inhibitor, is a triterpene from the root of the R. alceaefolius Poir. Euscaphic inhibits calf DNA polymerase α (pol α) and rat DNA polymerase β (pol β) with IC₅₀ values of 61 and 108 μM . Euscaphic acid induces apoptosis .

HY-128357

Ibezapolstat 4 Publications Verification ACX-362E; GLS-362E	Bacterial DNA/RNA Synthesis	Infection
Ibezapolstat (ACX-362E) is a first-in-class, orally active *DNA polymerase IIIC (pol* IIIC)** inhibitor, with a K_i of 0.325 μM for the DNA pol IIIC from C. difficile. Ibezapolstat is developed for the research of C. difficile infection(CDI) .

HY-162919

YK-2168	CDK Apoptosis c-Myc	Cancer
YK-2168 is a potent and selective CDK9 inhibitor with an IC50 of 5.9 nM. YK-2168 inhibits phosphorylation of the CDK9 substrate pS2-RNA Pol II C-terminal domain. YK-2168 induces apoptosis in tumor cells, suppresses expression of CDK9-regulated genes including MYC and Mcl1, and inhibits tumor growth in CDX mice models. YK-2168 can be used for the research of cancer, such as leukemia .

HY-153225

PYR01	HIV Reverse Transcriptase	Infection
PYR01 is a non-nucleoside reverse transcriptase inhibitor and a killing activator targeting HIV infected cells. PYR01 has cytokilling and antiviral properties of HIV-1 infection with the IC₅₀ values of 27.5nM and 39.7nM, respectively. PYR01 leads to selective cytotoxicity by promoting HIV-1 Gag-Pol dimerization and HIV-1 protease intracellular activation. PYR01 can be used in the study of HIV .

HY-17431

Fosamprenavir Calcium Salt 4 Publications Verification GW433908G	Drug Intermediate HIV HIV Protease	Infection
Fosamprenavir Calcium Salt (GW433908G) is an orally active inhibitor targeting HIV-1 protease and is a prodrug of Amprenavir (HY-17430). Fosamprenavir Calcium Salt is hydrolyzed into Amprenavir (VX-478) by cell phosphatases in the intestinal epithelium. Amprenavir binds to the active site of HIV-1 protease, preventing the processing of viral gag and gag-pol polyprotein precursors, thereby inhibiting the formation of mature infectious virus particles and exerting anti-HIV-1 infection activity. Fosamprenavir Calcium Salt can be used for the study of human immunodeficiency virus (HIV-1) infection .

HY-112062

POL1-IN-1	DNA/RNA Synthesis Apoptosis	Cancer
POL1-IN-1 is a class of RNA polymerase I inhibitors with broad-spectrum antiproliferative activity against tumor cells, while selectively inhibiting RNA polymerase I transcription. By blocking RNA polymerase I-mediated rRNA synthesis, POL1-IN-1 impairs ribosome biogenesis, thereby inhibiting tumor cell proliferation and inducing apoptosis. POL1-IN-1 can be used for the research of malignant tumors .

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-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 .

HY-103019B

(-)-Enitociclib 2 Publications Verification (R)-Enitociclib; (-)-BAY-1251152; (-)-VIP152	Drug Isomer CDK Apoptosis DNA/RNA Synthesis	Cancer
(-)-Enitociclib ((R)-Enitociclib) is an enantiomer of Enitociclib (HY-103019E) with an optical rotation of (-). Enitociclib is a selective CDK9 inhibitor and apoptosis inducer. Enitociclib inhibits CDK9 activity and reduces the phosphorylation of Ser2 in the carboxyl-terminal domain (CTD) of *RNA polymerase Pol* II, thereby downregulating the transcription of key oncogenes such as MYC and MCL1**. Enitociclib has anti-proliferative activity targeting MYC ⁺ lymphoma and multiple myeloma (MM) cells, and has synergistic effects with Bortezomib (HY-10227) and Lenalidomide (HY-A0003), and can be used in the research of hematological malignancies .

HY-P3293

Lonodelestat POL6014	Elastase	Inflammation/Immunology
Lonodelestat (POL6014) is a potent, orally active and selective peptide inhibitor of human neutrophil elastase (hNE). Lonodelestat (POL6014) has the potential for the research of cystic fibrosis (CF) .

HY-153244

MFH290 1 Publications Verification	CDK	Cancer
MFH290 is a potent and highly selective cyclin-dependent kinase 12/13 (CDK12/13) covalent inhibitor. MFH290 forms a covalent bond with Cys-1039 of CDK12 and exhibits excellent kinome selectivity and inhibits the phosphorylation of serine-2 in the C-terminal domain (CTD) of RNA-polymerase II (Pol II). MFH290 is used for cancer research .

HY-W015490S

1,4-Naphthoquinone-d6	Isotope-Labeled Compounds DNA/RNA Synthesis NF-κB Monoamine Oxidase TNF Receptor Bacterial	Infection Inflammation/Immunology Cancer
1,4-Naphthoquinone-d₆ is the deuterium labeled 1,4-Naphthoquinone. 1,4-Naphthoquinone is an inhibitor with broad-spectrum inhibitory activity targeting DNA polymerase, NF-κB and monoamine oxidase (MAO-A/B), with antibacterial and anti-biofilm efficacy. 1,4-Naphthoquinone is a competitive inhibitor of MAO-B (Ki=1.4 μM) and a non-competitive inhibitor of MAO-A (Ki=7.7 μM). 1,4-Naphthoquinone inhibits DNA polymerase pol α, β, γ, δ, ε, λ with IC₅₀ ranging from 5.57-128 μM. 1,4-Naphthoquinone inhibits tumor cell proliferation, induces apoptosis and necrosis, and has anti-angiogenic and anti-inflammatory activities by inducing oxidative stress, depleting glutathione (GSH), inhibiting DNA polymerase-mediated DNA synthesis and blocking NF-κB nuclear translocation. 1,4-Naphthoquinone can be used in anti-bacterial , anti-tumor and anti-inflammatory studies, including inhibition of melanoma and colon cancer cell growth and endothelial cell function, as well as LPS-induced inflammation models .

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 .

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-147917

RNA polymerase II-IN-2	ADC Payload DNA/RNA Synthesis	Cancer
RNA polymerase II-IN-2 is a RNA polymerase II inhibitor with a K_i value of 74.1 nM. RNA polymerase II-IN-2 inhibits Pol II-mediated transcription and induces cytotoxicity in mammalian cells. RNA polymerase II-IN-2 serves as a payload for antibody-drug conjugates (ADC) and is applicable for cancer research .

HY-118723

BMH-22	DNA/RNA Synthesis	Cancer
BMH-22, a benzonaphthyridin, is a *RNA polymerase I (Pol* I) transcription** inhibitor independent of p53 function. BMH-22 causes reorganization of nucleolar marker proteins consistent with segregation of the nucleolus. BMH-22 destabilizes RPA194 in a proteasome-dependent manner and inhibits nascent rRNA synthesis and expression of the 45S rRNA precursor. BMH-22 shows potent anticancer activity across many tumor types .

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-120105

NSC666715	DNA/RNA Synthesis Apoptosis MDM-2/p53 Bcl-2 Family Caspase PARP	Cancer
NSC666715 is a DNA polymerase β (Pol-β) inhibitor. NSC666715 directly and specifically interacts with *Pol-β, interferes with its binding to damaged DNA, blocks its dRP* lyase activity, and inhibits *Pol-β*-mediated SN- and LP-BER. NSC666715 induces AP site accumulation and S-phase cell cycle arrest, and triggers senescence and apoptosis (apoptosis) via the p53/p21 pathway in colorectal cancer cells. NSC666715 enhances TMZ (HY-17364)-induced DNA damage, senescence and apoptosis, and potentiates the cytotoxicity of TMZ. NSC666715 inhibits tumor growth in colon cancer xenograft models. NSC666715 can be used in research related to colorectal cancer .

HY-P3293A

Lonodelestat TFA POL6014 TFA	Elastase	Inflammation/Immunology
Lonodelestat TFA (POL6014 TFA) is a potent, orally active and selective peptide inhibitor of human neutrophil elastase (hNE). Lonodelestat TFA has the potential for the research of cystic fibrosis (CF) .

HY-100513

(±)-Dehydroaltenusin	DNA/RNA Synthesis Apoptosis Antibiotic	Cancer
(±)-Dehydroaltenusin, an antibiotic, is a selective eukaryotic *DNA polymerase α (pol* α)** inhibitor with an IC₅₀ of 0.68 μM. (±)-Dehydroaltenusin can be isolated from fungus Alternaria tenuis. (±)-Dehydroaltenusin competitively inhibits the DNA template primer (K_i: 0.23 μM) and non-competitively suppresses the 2'-deoxyribonucleoside 5'-triphosphate substrate (K_i: 0.18 μM). (±)-Dehydroaltenusin induces the cancer cell S-phase cycle arrest and apoptosis. (±)-Dehydroaltenusin can be used for cancers like human adenocarcinoma research .

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 .

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-78726S

Fosamprenavir-d4 Amprenavir phosphate-d₄; GW 433908-d₄	Isotope-Labeled Compounds Drug Intermediate HIV HIV Protease	Infection
Fosamprenavir-d₄ is the Deuterium-labeled Fosamprenavir (HY-78726). Fosamprenavir is an orally active inhibitor targeting HIV-1 protease and is a prodrug of Amprenavir (HY-17430). Fosamprenavir is hydrolyzed into Amprenavir (VX-478) by cell phosphatases in the intestinal epithelium. Amprenavir binds to the active site of HIV-1 protease, preventing the processing of viral gag and gag-pol polyprotein precursors, thereby inhibiting the formation of mature infectious virus particles and exerting anti-HIV-1 infection activity. Fosamprenavir can be used for the study of human immunodeficiency virus (HIV-1) infection .

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-145840

Pol I-IN-1	DNA/RNA Synthesis	Cancer
Pol I-IN-1 is a potent RNA polymerase I *(Pol* I)** inhibitor with IC₅₀ 0.21 µM for the Pol I large catalytic subunit RPA194 .

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-178201

JLJ648	HIV Pyroptosis	Infection
JLJ648 is a Gag-Pol dimerizer with antiviral activity. JLJ648 can inhibit HIV replication and induce infected cell pyroptosis. JLJ648 can be used for the research of infection, such as HIV (human immunodeficiency virus) .

HY-105448

U-75875	HIV Protease	Infection
U-75875 is a HIV-1 protease inhibitor. U-75875 can block Gag-Pol protein processing and viral maturation and replication. U-75875 can be used for the research of infection .

HY-126214S

JH-RE-06-d6	DNA/RNA Synthesis	Cancer
JH-RE-06-d6 is deuterium labele JH-RE-06. JH-RE-06, a potent REV1-REV7 interface inhibitor (IC₅₀=0.78 μM; K_i=0.42 μM), targets REV1 that interacts with the REV7 subunit of POLζ. JH-RE-06 disrupts mutagenic translesion synthesis (TLS) by preventing recruitment of mutagenic POLζ. JH-RE-06 improves chemotherapy .

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-X0009A

Tambiciclib dimaleate 1 Publications Verification GFH009 dimaleate; JSH-009 dimaleate; SLS009 dimaleate	CDK DYRK Apoptosis Bcl-2 Family c-Myc Caspase PARP DNA/RNA Synthesis	Cancer
Tambiciclib (GFH009, JSH-009) dimaleate is an orally active, highly potent and selective CDK9 inhibitor (IC₅₀ = 1 nM), demonstrating >200-fold selectivity over other CDKs, >100-fold selectivity over DYRK1A/B, and excellent selectivity over 468 kinases/mutants. Tambiciclib dimaleate demonstrates potent in vitro and in vivo antileukemic efficacy in acute myeloid leukemia (AML) mouse models by inhibiting *RNA Pol* II phosphorylation, downregulating MCL1 and MYC, and inducing apoptosis**. Tambiciclib dimaleate can be used for AML research .

HY-156296

CDK9-Cyclin T1 PPI-IN-1	CDK Apoptosis	Cancer
CDK9-Cyclin T1 PPI-IN-1 (Compound B19) is a selective CDK9-Cyclin T1 protein-protein interaction (PPI) inhibitor. CDK9-Cyclin T1 PPI-IN-1 inhibits cell proliferation in TNBC MDA-MB-231 cells (IC₅₀: 0.044 μM), and induces apoptosis. CDK9-Cyclin T1 PPI-IN-1 inhibits CDK9 transcription activity, reduces the phosphorylation of RNA Pol II CTD ser2. CDK9-Cyclin T1 PPI-IN-1 inhibits tumor growth in a TNBC 4T1 mouse model .

HY-W015490R

1,4-Naphthoquinone (Standard)	Reference Standards DNA/RNA Synthesis NF-κB Monoamine Oxidase TNF Receptor Bacterial	Infection Inflammation/Immunology Cancer
1,4-Naphthoquinone is an inhibitor with broad-spectrum inhibitory activity targeting DNA polymerase, NF-κB and monoamine oxidase (MAO-A/B), with antibacterial and anti-biofilm efficacy. 1,4-Naphthoquinone is a competitive inhibitor of MAO-B (Ki=1.4 μM) and a non-competitive inhibitor of MAO-A (Ki=7.7 μM). 1,4-Naphthoquinone inhibits DNA polymerase pol α, β, γ, δ, ε, λ with IC50 ranging from 5.57-128 μM. 1,4-Naphthoquinone inhibits tumor cell proliferation, induces apoptosis and necrosis, and has anti-angiogenic and anti-inflammatory activities by inducing oxidative stress, depleting glutathione (GSH), inhibiting DNA polymerase-mediated DNA synthesis and blocking NF-κB nuclear translocation. 1,4-Naphthoquinone can be used in anti-bacterial , anti-tumor and anti-inflammatory studies, including inhibition of melanoma and colon cancer cell growth and endothelial cell function, as well as LPS-induced inflammation models .

Cat. No.	Product Name	Target	Research Area

HY-P3293

Lonodelestat POL6014	Elastase	Inflammation/Immunology
Lonodelestat (POL6014) is a potent, orally active and selective peptide inhibitor of human neutrophil elastase (hNE). Lonodelestat (POL6014) has the potential for the research of cystic fibrosis (CF) .

HY-P3293A

Lonodelestat TFA POL6014 TFA	Elastase	Inflammation/Immunology
Lonodelestat TFA (POL6014 TFA) is a potent, orally active and selective peptide inhibitor of human neutrophil elastase (hNE). Lonodelestat TFA has the potential for the research of cystic fibrosis (CF) .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-78726

Fosamprenavir 4 Publications Verification Amprenavir phosphate; GW 433908	Infection Natural Products Classification of Application Fields Endogenous metabolite Disease Research Fields Source Classification	Drug Intermediate HIV HIV Protease
Fosamprenavir is an orally active inhibitor targeting HIV-1 protease and is a prodrug of Amprenavir (HY-17430). Fosamprenavir is hydrolyzed into Amprenavir (VX-478) by cell phosphatases in the intestinal epithelium. Amprenavir binds to the active site of HIV-1 protease, preventing the processing of viral gag and gag-pol polyprotein precursors, thereby inhibiting the formation of mature infectious virus particles and exerting anti-HIV-1 infection activity. Fosamprenavir can be used for the study of human immunodeficiency virus (HIV-1) infection .

HY-N2566

Euscaphic acid 1 Publications Verification	Triterpenes Structural Classification other families Classification of Application Fields Terpenoids Plants Disease Research Fields Source Classification Cancer	DNA/RNA Synthesis PI3K Apoptosis
Euscaphic acid, a DNA polymerase inhibitor, is a triterpene from the root of the R. alceaefolius Poir. Euscaphic inhibits calf DNA polymerase α (pol α) and rat DNA polymerase β (pol β) with IC₅₀ values of 61 and 108 μM . Euscaphic acid induces apoptosis .

HY-17431

Fosamprenavir Calcium Salt 4 Publications Verification GW433908G	Infection Natural Products Classification of Application Fields Endogenous metabolite Disease Research Fields Source Classification	Drug Intermediate HIV HIV Protease
Fosamprenavir Calcium Salt (GW433908G) is an orally active inhibitor targeting HIV-1 protease and is a prodrug of Amprenavir (HY-17430). Fosamprenavir Calcium Salt is hydrolyzed into Amprenavir (VX-478) by cell phosphatases in the intestinal epithelium. Amprenavir binds to the active site of HIV-1 protease, preventing the processing of viral gag and gag-pol polyprotein precursors, thereby inhibiting the formation of mature infectious virus particles and exerting anti-HIV-1 infection activity. Fosamprenavir Calcium Salt can be used for the study of human immunodeficiency virus (HIV-1) infection .

HY-100513

(±)-Dehydroaltenusin	Structural Classification Microorganisms Antibiotics Source Classification	DNA/RNA Synthesis Apoptosis Antibiotic
(±)-Dehydroaltenusin, an antibiotic, is a selective eukaryotic *DNA polymerase α (pol* α)** inhibitor with an IC₅₀ of 0.68 μM. (±)-Dehydroaltenusin can be isolated from fungus Alternaria tenuis. (±)-Dehydroaltenusin competitively inhibits the DNA template primer (K_i: 0.23 μM) and non-competitively suppresses the 2'-deoxyribonucleoside 5'-triphosphate substrate (K_i: 0.18 μM). (±)-Dehydroaltenusin induces the cancer cell S-phase cycle arrest and apoptosis. (±)-Dehydroaltenusin can be used for cancers like human adenocarcinoma research .

HY-17431R

Fosamprenavir Calcium Salt (Standard) GW433908G (Standard)	Structural Classification Natural Products Endogenous metabolite Source Classification	Reference Standards Drug Intermediate HIV HIV Protease
Fosamprenavir Calcium Salt (GW433908G) (Standard) is the analytical standard of Fosamprenavir Calcium Salt (HY-17431R). This product is intended for research and analytical applications. Fosamprenavir Calcium Salt (GW433908G) is an orally active inhibitor targeting HIV-1 protease and is a prodrug of Amprenavir (HY-17430). Fosamprenavir Calcium Salt is hydrolyzed into Amprenavir (VX-478) by cell phosphatases in the intestinal epithelium. Amprenavir binds to the active site of HIV-1 protease, preventing the processing of viral gag and gag-pol polyprotein precursors, thereby inhibiting the formation of mature infectious virus particles and exerting anti-HIV-1 infection activity. Fosamprenavir Calcium Salt can be used for the study of human immunodeficiency virus (HIV-1) infection .

Cat. No.	Product Name	Chemical Structure

HY-W015490S

1,4-Naphthoquinone-d6

1,4-Naphthoquinone-d₆ is the deuterium labeled 1,4-Naphthoquinone. 1,4-Naphthoquinone is an inhibitor with broad-spectrum inhibitory activity targeting DNA polymerase, NF-κB and monoamine oxidase (MAO-A/B), with antibacterial and anti-biofilm efficacy. 1,4-Naphthoquinone is a competitive inhibitor of MAO-B (Ki=1.4 μM) and a non-competitive inhibitor of MAO-A (Ki=7.7 μM). 1,4-Naphthoquinone inhibits DNA polymerase pol α, β, γ, δ, ε, λ with IC₅₀ ranging from 5.57-128 μM. 1,4-Naphthoquinone inhibits tumor cell proliferation, induces apoptosis and necrosis, and has anti-angiogenic and anti-inflammatory activities by inducing oxidative stress, depleting glutathione (GSH), inhibiting DNA polymerase-mediated DNA synthesis and blocking NF-κB nuclear translocation. 1,4-Naphthoquinone can be used in anti-bacterial , anti-tumor and anti-inflammatory studies, including inhibition of melanoma and colon cancer cell growth and endothelial cell function, as well as LPS-induced inflammation models .

HY-139289S

ART899
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 .

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 .

HY-78726S

Fosamprenavir-d4

Fosamprenavir-d₄ is the Deuterium-labeled Fosamprenavir (HY-78726). Fosamprenavir is an orally active inhibitor targeting HIV-1 protease and is a prodrug of Amprenavir (HY-17430). Fosamprenavir is hydrolyzed into Amprenavir (VX-478) by cell phosphatases in the intestinal epithelium. Amprenavir binds to the active site of HIV-1 protease, preventing the processing of viral gag and gag-pol polyprotein precursors, thereby inhibiting the formation of mature infectious virus particles and exerting anti-HIV-1 infection activity. Fosamprenavir can be used for the study of human immunodeficiency virus (HIV-1) infection .

HY-126214S

JH-RE-06-d6
JH-RE-06-d6 is deuterium labele JH-RE-06. JH-RE-06, a potent REV1-REV7 interface inhibitor (IC₅₀=0.78 μM; K_i=0.42 μM), targets REV1 that interacts with the REV7 subunit of POLζ. JH-RE-06 disrupts mutagenic translesion synthesis (TLS) by preventing recruitment of mutagenic POLζ. JH-RE-06 improves chemotherapy .

HY-139593S

Polθ-IN-1-d3
Polθ-IN-1-d3 (example 1) is a deuterated Polθ inhibitor used for cancer study (extracted from patent WO2021028670) .

HY-78726S2

Fosamprenavir-13C6

Fosamprenavir- ¹³C₆ is the ¹³C-labeled Fosamprenavir (HY-78726). Fosamprenavir is an orally active inhibitor targeting HIV-1 protease and is a prodrug of Amprenavir (HY-17430). Fosamprenavir is hydrolyzed into Amprenavir (VX-478) by cell phosphatases in the intestinal epithelium. Amprenavir binds to the active site of HIV-1 protease, preventing the processing of viral gag and gag-pol polyprotein precursors, thereby inhibiting the formation of mature infectious virus particles and exerting anti-HIV-1 infection activity. Fosamprenavir can be used for the study of human immunodeficiency virus (HIV-1) infection .

Targets Recommended: Serpin

Cat. No.	Product Name	Target	Research Areas	Chemical Structure