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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
20 Results for "
homologous targeting
" in MedChemExpress (MCE) Product Catalog:
Products (20)
20 Results for "homologous targeting" in MCE Product Catalog:
3
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Tecovirimat (ST-246) is an orally bioavailable and selective compound against orthopoxviruses including vaccinia, monkeypox, camelpox, cowpox, ectromelia (mousepox), smallpox and variola viruses. Tecovirimat is evaluated against vaccinia, cowpox virus, ectromelia virus with EC50 values of 0.01 μM, 0.48 μM and 0.05 μM, respectively. Tecovirimat targets the orthopoxvirus protein VP37 which is necessary for membrane envelopment of intracellular mature virus particles to form enveloped virus. Tecovirimat exerts antiviral activity on the target of the cowpox virus V061 gene, which is homologous to vaccinia virus F13L, encoding a major envelope protein (p37) required for production of extracellular virus .
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3 Cited Publications
Synonyms: ST-246 monohydrate
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Tecovirimat (ST-246) monohydrate is the monohydrate form of Tecovirimat (HY-14805). Tecovirimat monohydrate is an orally bioavailable and selective compound against orthopoxviruses [including vaccinia, monkeypox, camelpox, cowpox, ectromelia (mousepox), smallpox and variola viruses]. Tecovirimat monohydrate is evaluated against vaccinia, cowpox virus, ectromelia virus with EC50 values of 0.01 μM, 0.48 μM and 0.05 μM, respectively. Tecovirimat monohydrate targets the orthopoxvirus protein VP37 which is necessary for membrane envelopment of intracellular mature virus particles to form enveloped virus. Tecovirimat monohydrate exerts antiviral activity on the target of the cowpox virus V061 gene, which is homologous to vaccinia virus F13L, encoding a major envelope protein (p37) required for production of extracellular virus. Tecovirimat monohydrate could be used in the study for orthopoxvirus-induced diseases .
Cat. No.: HY-174374
CAS No.: 3076446-44-8
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Topobexin is a TOP2B-selective inhibitor with IC50 values of 0.19 μM and 4.8 μM for TOP2B and TOP2A (DNA decatenation assay). Topobexin binds to non-homologous residues in the obex pocket and targets the ATPase domain of TOP2B. Topobexin prevents anthracycline-induced DNA double-strand break formation, apoptotic signaling mediated by caspase 3/7, 8 and 9, cardiomyocyte morphological changes, mitochondrial depolarization/loss, left ventricular systolic dysfunction, extracellular matrix remodeling, fibrotic alterations, and increases in plasma cardiac troponin T and BNP. Topobexin does not impair the antiproliferative effects of anthracyclines in cancer cells, exhibits no intrinsic cytotoxicity in cardiomyocytes, and is well tolerated in rabbits. Topobexin can be used in studies related to anthracycline-induced cardiotoxicity .
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RECQL5-IN-1 (Compound 4a) acts as an orally effective RECQL5 inhibitor (targeting both enzymatic and nonenzymatic domain). RECQL5-IN-1 is a potent inhibitor of RECQL5 helicase activity (IC50=46.3 nM), stabilizes the interaction between RECQL5-RAD51 proteins, causes RAD51 aggregation and homologous recombination repair (HRR) inhibition, thereby exhibiting selective cytotoxicity in RECQL5-expressing cancer cells .
Synonyms: NCD
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Naphthyridine carbamate dimer (NCD) is a molecular glue. Naphthyridine carbamate dimer induces designed structural changes in target functional DNA, thereby regulating its function. As a molecular glue, naphthyridine carbamate dimer stabilizes non-spontaneously formed GG homologous mismatched double-stranded DNA. Naphthyridine carbamate dimer reduces the formation of toxic RNA foci and regulates CGG repeat instability associated with fragile X syndrome and spinocerebellar ataxia type 31. Naphthyridine carbamate dimer can be used in research related to fragile X syndrome and spinocerebellar ataxia type 31 .
Cat. No.: HY-W023758
CAS No.: 166196-54-9
Synonyms: 4-(4-Bromo-1H-pyrazol-5-yl)pyridine
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HDGFRP2/PSIP1-IN-1 (compound BPP) is a dual inhibitor targeting the PWWP domain of hepatocarcinogenic growth factor-related protein 2 (HDGFRP2) and its homologous protein PSIP1, hinder the development and progression of diffuse intrinsic pontine glioma (DIPG). HDGFRP2/PSIP1-IN-1 binds to HDGFRP2 with a Kd value of 7 μM and a ligand efficiency of 0.47; it binds to the PSIP1 PWWP domain with a Kd value of 27 μM; meanwhile, it has a Kd value of 14 μM for HDGFRP3, indicating its effectiveness as an inhibitor of the HDGFRP2 PWWP subfamily .
Synonyms: ST-246-d4
Cat. No.: HY-174499
Cas9 Nickase D10A mRNA expresses a version of the Streptococcus pyogenes SF370 Cas9 protein (CRISPR Associated Protein 9) that contains a D10A amino acid substitution. This mRNA also contains a C-terminal nuclear localization signal followed by a HA tag.Cas9 functions as part of the CRISPR (clustered regularly interspaced short palindromic repeats) genome editing system. In the CRISPR system, an RNA guide sequence targets the site of interest and the Cas9 protein is employed to perform the DNA cleavage. While wild-type Cas9 creates a double-stranded break at the target site, Cas9 nickase creates a single-stranded break. This favors homology-directed repair and decreases the occurrence of non-homologous end joining.
Cat. No.: HY-175466
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BER-IN-1 is a base excision repair (BER) inhibtor, targeting DNA abasic sites. BER-IN-1 cleaves abasic sites via β- and β,δ-elimination mechanisms, disrupts the base excision repair (BER) pathway and leads to DNA double-strand breaks (DSBs). BER-IN-1 can enhance the effectiveness of the PARP inhibitor Olaparib (HY-10162) in homologous recombination (HR)-proficient cancer cells (MDA-MB-231, HeLa, and SKOV3). BER-IN-1 induces an S-phase arrest and apoptosis companied with Olaparib (HY-10162). BER-IN-1 can be used for the research of cancer, such as breast, cervical and ovarian cancer .
Cat. No.: HY-149489
CAS No.: 742104-91-2
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JH-131e-153, a diacylglycerol (DAG)-lactone, is a small molecule activator of Munc13-1, targeting the C1 domain. The activation sequence of JH-131e-153 on Munc13-1 is WT>I590≈R592A≈W588A. The C1 domain of Munc13-1 and protein kinase C (PKC) are homologous in sequence and structure. The activation sequence of JH-131e-153 on Munc13-1 and PKC was PKCα>Munc13-1>PKCε. JH-131e-153 regulates neuronal processes through Munc13-1 and can be further used in the study of neurodegenerative diseases .
Cat. No.: HY-120750
CAS No.: 111783-54-1
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A 62176 hydrochloride is a compound that targets DNA topoisomerase II and has the activity of inhibiting purine synthesis in cancer cells. A 62176 hydrochloride interferes with c-MYC mRNA expression by interacting with G-quadruplex. The main mechanism of action of A 62176 hydrochloride is by displacing nucleosomes from the quadruplex of non-template strand rDNA, resulting in rapid redistribution of nucleosomes. The application potential of A 62176 hydrochloride is that it causes DNA damage and relies on BRCA1/2-mediated homologous recombination and DNA-PK-mediated non-homologous end-joining pathways to repair the damage .
Cat. No.: HY-N10648
CAS No.: 3001295-81-1
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Cat. No.: HY-168646
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SJ46411-Br is one of CRL2 KLHDC2 targeting Ligands for E3 Ligase. SJ46411-Br can bind to KLHDC2 to form a complex to promote cooperative homologous selective ternary complex formation. SJ46411-Br can be coupled to BET ligand JQ1 (HY-13030) through PROTAC linker to synthesize corresponding PROTACs .
Cat. No.: HY-P11231
CAS No.: 2780353-11-7
Synonyms: FUS(364-369)-TAT
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Cat. No.: HY-L244
761 compounds
In this era of rapid advancement in gene-editing technology, the CRISPR-Cas system, with its powerful programmability, is leading a transformation in life sciences research. It enables efficient and precise targeted modification of an organism's genome, providing a robust tool for studying gene function, treating genetic diseases, and improving crop varieties. However, bottlenecks such as insufficient editing efficiency, low homologous directed repair efficiency, and potential off-target risks remain major challenges in achieving precise genetic modifications and developing gene therapies.
To overcome these limitations, the MCE High-Efficiency Gene Editing Compound Library systematically includes 761 small molecules that are known or have the potential to enhance gene-editing efficiency. These compounds work by targeting and modulating the DNA damage repair network, mechanistically inhibiting non-homologous end joining, promoting homologous directed repair, or regulating chromatin states and cellular responses, thereby significantly optimizing editing outcomes. This library is suitable for developing "CRISPR-small molecule" combination therapy strategies, improving gene-editing efficiency, and providing a powerful tool for in-depth research into the mechanisms of DNA damage repair in gene editing.
Cat. No.: HY-P992033
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Cat. No.: HY-181694
SeSA-HCPT is an orally active dual-target inhibitor integrating Topo I and HDAC inhibition. SeSA-HCPT induces potent DNA damage, apoptosis, S-phase arrest in prostate cancer cells. SeSA-HCPT inhibits cancer cells proliferation and migration. SeSA-HCPT impairs homologous recombination by suppressing KIF4A-RAD51 signaling. SeSA-HCPT markedly inhibits CRPC tumor growth with minimal systemic toxicity .
Cat. No.: HY-P11757
CAS No.: 2251785-27-8
Cat. No.: HY-P992365
Cat. No.: HY-189225
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PP-048 is a selective dual inhibitor of Polθ/PARP1, with IC50 values of 4.9 nM and 6.8 nM for the Polθ helicase/ATPase domain and PARP1, respectively. PP-048 impairs the compensatory DNA repair capacity of homologous recombination-deficient cells by simultaneously inhibiting the DNA repair functions associated with Polθ and PARP1, thereby exacerbating DNA double-strand damage and inducing apoptosis. PP-048 exhibits more potent selective antiproliferative activity against HR-deficient cancer cells. PP-048 can be used in studies related to Polθ/PARP1 dual-target inhibition, synthetic lethality, DNA damage repair, and HR-deficient triple-negative breast cancer .
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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
