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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
39 Results for "
DNA-binding domain
" in MedChemExpress (MCE) Product Catalog:
Products (39)
39 Results for "DNA-binding domain" in MCE Product Catalog:
7
7 Publications Verification
DTHIB is a direct and selective heat shock factor 1 (HSF1) inhibitor with a Kd of 160 nM for DTHIB binding to the HSF1 DNA binding domain (DBD). DTHIB inhibits HSF1 cancer gene signature (HSF1 CaSig) and selectively stimulates degradation of nuclear HSF1. DTHIB has potently anticancer activities and can be used for prostate cancer research .
3
3 Cited Publications
Cat. No.: HY-163731
CAS No.: 3077196-25-6
Research Areas:
EGR-1-IN-1 is a EGR-1 inhibitor with an IC50 of 1.86 μM. EGR-1-IN-1 binds to the zinc finger DNA-binding domain of EGR-1 and promotes the dissociation of the EGR-1-DNA complex. EGR-1-IN-1 reduces the mRNA expression levels of EGR-1-regulated inflammatory genes induced by TNFα. EGR-1-IN-1 alleviates atopic dermatitis-like lesions in the ear skin of mice. EGR-1-IN-1 serves as a lead compound for the development of targeted compounds for inflammatory skin diseases. EGR-1-IN-1 can be used in studies related to atopic dermatitis .
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3 Cited Publications
SCH529074 is a potent and orally active p53 activator. SCH529074 binds specifically and conformation-dependently to p53 DBD ( DNA binding domain) with a Ki of 1-2 μM in a saturable manner. SCH529074 restores mutant p53 function and interrupts HDM2-mediated ubiquitination of wild Type p53. SCH529074 can be used for the study of non-small-cell lung carcinoma (NSCLC) .
1
1 Cited Publications
Synonyms: PROTAC AR-V7 degrader-2
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MTX-23 is a PROTAC degrader targeting androgen receptor splice variant 7 (AR-V7) and full-length androgen receptor (AR-FL), with DC50 values of 0.37 μM and 2 μM, respectively. MTX-23 binds to the DNA-binding domains of AR-V7 and AR-FL, recruits the VHL E3 ubiquitin ligase (E3 ubiquitin ligase) and induces their degradation. MTX-23 reduces the proliferation of prostate cancer cells, promotes their apoptosis (apoptosis), and also inhibits tumor growth in mouse models. MTX-23 can be used for the research of prostate cancer .
Cat. No.: HY-W013049
CAS No.: 112-85-6
Synonyms: Behenic acid
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Glycerol kinase, microorganism (GyK) acts as a NR4A1 inhibitor with enzymatic activity. It directly binds to and inhibits the transcription factor NR4A1, thereby negatively regulating hepatic gluconeogenesis and reducing blood glucose levels. Glycerol kinase, microorganism positively regulates UCP1 expression via partial dependence on the β-adrenergic receptor-cAMP-CREB pathway, promotes browning of white adipose tissue and thermogenesis, and further modulates intracellular fatty acid composition and energy metabolism. In diabetic mouse models, overexpression of Glycerol kinase effectively antagonizes NR4A1-induced hyperglycemia, demonstrating potential for improving glucose homeostasis. Glycerol kinase, microorganism can be used for studies on diabetes and obesity .
Cat. No.: HY-U00447
CAS No.: 38275-34-2
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PK11000 is an alkylating agent, and stabilizes the DNA-binding domain of both WT and mutant p53 proteins by covalent cysteine modification without compromising DNA binding. PK11000 has anti-tumor activities .
Cat. No.: HY-W035137
CAS No.: 22112-89-6
Synonyms: 5,15-DPP
5,15-Diphenylporphyrin (5,15-DPP) is an inhibitor of the oncogenic transcription factor STAT3. 5,15-Diphenylporphyrin specifically binds to the SH2 domain of STAT3, blocking the pTyr-SH2 interaction, thereby inhibiting the dimerization, nuclear translocation and DNA binding activity of STAT3, and ultimately inhibiting the expression of cancer cell-related genes. 5,15-Diphenylporphyrin can be used in research fields related to the development of anticancer drugs[1][2].
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VPC-14449 is a potent and selective inhibitor of the DNA-binding domain of the androgen receptor (AR-DBD), with IC50 of 0.34 μM for full-length human AR. VPC-14449 reduces the ability of full-length AR as well as AR variants to interact with chromatin. VPC-14449 can be used for the research of prostate cancer .
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NSC15520 is a small molecular inhibitor of Replication Protein A (RPA). NSC15520 specifically recognizes the RPA N-terminal DNA binding domain (DBD), and blocks the interaction of RPA with p53 or RAD9. NSC15520 also inhibtis helix destabilization of a duplex DNA (dsDNA) oligonucleotide, involves in DNA replication, DNA repair, DNA recombination, and DNA damage response signaling .
Cat. No.: HY-W013049S3
CAS No.: 1193721-67-3
Synonyms: Behenic acid-d3
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VPC-14228 is an inhibitor that selectively targets androgen receptor DNA binding domain (AR-DBD). VPC-14228 inhibits the interaction between AR and DNA, thereby blocking AR-mediated transcriptional activation. VPC-14228 does not rely on nuclear localization inhibition, but rather inhibits the activity of full-length AR and splice variant AR-V7 by interfering with AR binding to chromatin. And VPC-14228 has high selectivity for other nuclear receptors such as ER and PR. VPC-14228 can be used in the study of prostate cancer [2].
Cat. No.: HY-162265A
UCM-13369 (Compound 4b) is a NPM1 inhibitor. UCM-13369 downregulates the pathway associated with mutant NPM1 C+, and specifically recognizes the C-end DNA-binding domain of NPM1 C+. UCM-13369 induces apoptosis in AML cell lines and primary cells. UCM-13369 can be used for leukemia research .
Cat. No.: HY-172767
STAT3-D11-PROTAC-VHL (Compound D11-PROTAC) is a PROTAC degrader targeting Signal Transducer and Activator of Transcription 3 (STAT3). STAT3-D11-PROTAC-VHL exhibits anti-tumor activity with IC50 values of 1335 nM and 1973 nM against HeLa and MCF-7 cells, respectively. STAT3-D11-PROTAC-VHL binds to the DNA-binding domain of STAT3 and recruits the E3 ligase VHL to form a ternary complex, leading to the ubiquitination of STAT3 and subsequent degradation by the proteasome. STAT3-D11-PROTAC-VHL also inhibits tumor cell growth, induces cell cycle arrest and apoptosis, and suppresses tumor immune evasion .
Cat. No.: HY-W013049S1
CAS No.: 29823-26-5
Synonyms: Behenic acid-d43
Cat. No.: HY-W013049S4
CAS No.: 1219804-98-4
Synonyms: Behenic acid-d4-1
Cat. No.: HY-175455
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LYA914 is an orally active AR/AR-V7 PROTAC degrader. LYA914 targets the proteolytic degradation of the conserved DNA binding domain (DBD) of the androgen receptor (AR). LYA914 exhibits potent antiproliferative effects in Enzalutamide (HY-70002)-insensitive/resistant cells. LYA914 inhibits tumor growth in VCaP/LNCaP tumor mouse models. LYA914 can be used to study castration-resistant prostate cancer (CRPC) .
Cat. No.: HY-162265
CAS No.: 2921944-77-4
UCM-13369 (Compound 4b) is a NPM1 inhibitor. UCM-13369 downregulates the pathway associated with mutant NPM1 C+, and specifically recognizes the C-end DNA-binding domain of NPM1 C+. UCM-13369 induces apoptosis in AML cell lines and primary cells, that can be used for the research of AML .
Cat. No.: HY-P11164
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Cat. No.: HY-W013049S6
CAS No.: 2785462-39-5
Synonyms: Behenic acid-13C4
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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
