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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
35 Results for "
NTD
" in MedChemExpress (MCE) Product Catalog:
Products (35)
35 Results for "NTD" in MCE Product Catalog:
2
2 Cited Publications
Cat. No.: HY-P83706
Synonyms: DF 5L; DF5L; DFNA 5L; DFNA5L; FKSG 10; FKSG10; FLJ12150; Gasdermin D; Gasdermin domain containing 1; Gasdermin domain containing protein 1; Gasdermin domain-containing protein 1; Gasdermin-D; GasderminD; GSDMD_HUMAN; GSDMDC 1; GSDMDC1; Gasdermin-D, N-terminal; GSDMD-NT; hGSDMD-NTD; Gasdermin-D, C-terminal; GSDMD-CT; hGSDMD-CTD.
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EPI-001, a selective inhibitor of Androgen Receptor (AR), targets transactivation unit 5 (Tau-5) of the AR. EPI-001 can inhibit transactivation of the AR amino-terminal domain (NTD), with an IC50 of ~6 μM. EPI-001 is also a selective modulator of PPARγ. EPI-001 is active against castration-resistant prostate cancer .
Synonyms: EPI-002
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Ralaniten (EPI-002) is a potent and orally active antagonist of the androgen receptor-N-terminal domain (AR-NTD). Ralaniten inhibits AR transcriptional activity, with IC50 of 7.4 μM. Ralaniten can be used for the research of castration-resistant prostate cancer (CRPC) .
Synonyms: EPI-506
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Ralaniten triacetate (EPI-506), the pro-agent of Ralaniten, is a first-in-class, orally active androgen receptor (AR) N-terminal domain (NTD) inhibitor. Ralaniten triacetate shows activity against both full length and resistance-related AR species, including AR-v7 .
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BWA-522 is an orally active PROTAC degrader targeting full-length androgen receptor (AR-FL) and androgen receptor splice variant 7 (AR-V7). BWA-522 antagonizes the N-terminal domain (AR-NTD) of the androgen receptor, suppresses AR downstream signaling proteins and induces cancer cells apoptosis. BWA-522 inhibits tumor growth in LNCaP xenograft mouse model. BWA-522 can be used for the research of prostate cancer .
Cat. No.: HY-153575
BacPROTAC-1 is a BacPROTAC degrader that induces the degradation of the target protein mSA by recruiting ClpC/ClpC1. BacPROTAC-1 binds to mSA, Bacillus subtilis ClpCNTD and Mycobacterium smegmatis ClpC1NTD with Kd values of 3.9, 2.8 and 0.69 μM, respectively. BacPROTAC-1 forms a ternary complex between the substrate and ClpC, promotes ClpC reassembly and activation, and induces ATP-dependent degradation of mSA and mSA fusion model substrates via the ClpCP or ClpC1P1P2 protease system. BacPROTAC-1 can be used in studies on bacterial targeted protein degradation, bacterial protein homeostasis and antibacterial target discovery .
Cat. No.: HY-P991611
CAS No.: 3058434-76-4
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I-XW-053 is a specific anti-HIV-1 capsid inhibitor (IC50=164.2 μM). By binding to the CA NTD-NTD hexamerization interface and the R173 region of CTD (Kd=66.3 μM), I-XW-053 disrupts capsid function and reduces polymerization levels. I-XW-053 effectively blocks HIV-1 uncoating, inhibits reverse transcription and early replication, and exhibits broad-spectrum activity against primary HIV-1 isolates in peripheral blood mononuclear cells. I-XW-053 can be widely used in studies related to HIV-1 infection .
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Androgen receptor-IN-6 (compound 16) is an orally available androgen receptor (Androgen Receptor) potent inhibitor (IC50=0.12 μM in vitro), targeting the disordered N-terminal domain (NTD). Androgen receptor-IN-6 has good Caco2 cell membrane permeability and has an oral activity (F/%) of 16% in male CD-1 mice .
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8MDP is a potent equilibrative nucleoside transporter 1 (ENT1) inhibitor with an IC50 of 0.43 nM. 8MDP inhibits hENT1 and hENT2 uptake of [H 3] uridine by K562 cells and K15NTD cells .
Cat. No.: HY-103078A
CAS No.: 1644644-89-2
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I-XW-053 sodium is a specific anti-HIV-1 capsid inhibitor (IC50=164.2 μM). By binding to the CA NTD-NTD hexamerization interface and the R173 region of CTD (Kd=66.3 μM), I-XW-053 sodium disrupts capsid function and reduces polymerization levels. I-XW-053 sodium effectively blocks HIV-1 uncoating, inhibits reverse transcription and early replication, and exhibits broad-spectrum activity against primary HIV-1 isolates in peripheral blood mononuclear cells. I-XW-053 sodium can be widely used in studies related to HIV-1 infection .
Cat. No.: HY-149434
CAS No.: 3032601-92-3
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PROTAC AR-NTD antagonist 1 (compound 18) is a small molecule protein-targeting chimera (PROTACs) targeting the Androgen Receptor AR-V7. PROTAC AR-NTD antagonist 1 antagonizes the N-terminal domain of AR (AR-NTD), degrades AR-V7 protein, and induces apoptosis in prostate cancer (PC) cells. The efficiencies of PROTAC AR-NTD antagonist 1 in degrading AR-V7 in VCaP cells were 62.2% (1 μM) and 71.1% (5 μM), respectively .
Cat. No.: HY-P990816
Cat. No.: HY-178938
CAS No.: 1182011-65-9
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AR Degrader-3 is an orally active molecular glue that targets AR/ARV7 and induces the degradation of AR and ARV7 through the ubiquitin-proteasome pathway (UPP). AR Degrader-3 directly interacts with the ligand-binding domain (LBD) and the N-terminal domain (NTD) of AR. AR Degrader-3 effectively suppresses the transcriptional activity of wild-type AR (AR-WT), AR mutants, and ARV7. AR Degrader-3 downregulates the mRNA and protein levels of downstream AR target genes, thereby overcoming antiandrogen resistance mediated by ARV7 and AR point mutations. AR Degrader-3 induces apoptosis in Enzalutamide (HY-70002) (ENZa)-resistant cells and increases cleaved caspase-3 protein levels. AR Degrader-3 can be used for the study of castration-resistant prostate cancer (CRPC) .
Cat. No.: HY-RS05161
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FUZ Human Pre-designed siRNA Set A contains three designed siRNAs for FUZ gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
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5-Benzyloxygramine is a N protein PPI orthosteric stabilizer that exhibits both antiviral and N-NTD protein-stabilizing activities .
Cat. No.: HY-N15327
CAS No.: 138355-07-4
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Cat. No.: HY-155845
Antileishmanial agent-21 (compound 4e) is an antileishmanial agent that targets the Leishmania pteridine reductase 1 (Lm-PTR1). Antileishmanial agent-21 has an anti-folate mechanism, and folic acid and leucovorin can reverse the anti-leishmanial activity of Antileishmanial agent-21. Antileishmanial agent-21 inhibits the Chloroquine (HY-17589A)-resistant strain of Plasmodium falciparum (RKL9) with an IC50 of 0.0198-0.096 μM .
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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
