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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
53 Results for "
human Pol
" in MedChemExpress (MCE) Product Catalog:
Products (53)
53 Results for "human Pol" in MCE Product Catalog:
12
12 Publications Verification
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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 .
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4 Cited Publications
Cat. No.: HY-78726
CAS No.: 226700-79-4
Synonyms: Amprenavir phosphate; GW 433908
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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 .
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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.: HY-P3293
CAS No.: 906547-89-5
Synonyms: Pol6014
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Cat. No.: HY-158346
CAS No.: 2922287-81-6
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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-100513
CAS No.: 34279-44-2
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Cat. No.: HY-161916
CAS No.: 3043810-73-4
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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-P3293A
Synonyms: Pol6014 TFA
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Cat. No.: HY-78726S
CAS No.: 1133702-41-6
Synonyms: Amprenavir phosphate-d4; GW 433908-d4
Cat. No.: HY-178201
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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) .
Cat. No.: HY-E70659
CDK12/CycK Recombinant Human Active Protein Kinase is a cyclin-dependent kinase that phosphorylates the C-terminal domain (CTD) of RNA polymerase II (Pol II), thereby regulating different phases of the transcription cycle from transcription initiation to elongation and termination .
Cat. No.: HY-E70689
CDK7/CycH/MAT1 Recombinant Human Active Protein Kinase acts as a cyclin-dependent kinase activating kinase. CDK7 exists in several forms including a core tri-partite CDK7/CycH/MAT1 complex known as CAK (cyclin-dependent kinase activating kinase), as a component in the general transcription factor TFIIH and as a component of larger complexes containing pol II and other transcription factors .
Cat. No.: HY-78726A
CAS No.: 226700-80-7
Synonyms: Amprenavir phosphate sodium; GW 433908 sodium
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Fosamprenavir sodium is an orally active inhibitor targeting HIV-1 protease and is a prodrug of Amprenavir (HY-17430). Fosamprenavir sodium 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 sodium can be used for the study of human immunodeficiency virus (HIV-1) infection .
Cat. No.: HY-12814A
CAS No.: 1640282-30-9
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TH588 hydrochloride is a highly selective human MTH1 inhibitor (IC50=5 nM) with additional microtubule-targeting properties. TH588 hydrochloride interferes with mitotic progression, induces genomic 8-oxodG formation, DNA damage and cell cycle arrest, and exhibits significant cytotoxicity. Combined with phenethyl isothiocyanate, TH588 hydrochloride enhances ROS-mediated effects and effectively inhibits the growth of visceral metastases of malignant melanoma in mice. TH588 hydrochloride is widely applicable to research related to cancers, pancreatic cancer, leukemia, lymphoma, malignant melanoma and lung cancer .
Cat. No.: HY-78726S2
Synonyms: Amprenavir phosphate-13C6; GW 433908-13C6
Cat. No.: HY-17431R
CAS No.: 226700-81-8
Synonyms: GW433908G (Standard)
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Cat. No.: HY-181611
CAS No.: 3068829-46-6
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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 .
Cat. No.: HY-179413
CAS No.: 3050552-13-8
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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 .
Cat. No.: HY-183748
CAS No.: 3082173-75-6
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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-187358
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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 .
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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
