ntd

EPI-001 is an androgen receptor N-terminal domain antagonist with IC50 of ～6 μM and a selective PPAR-gamma modulator.

PROTAC AR-NTD antagonist 1 (compound 18) is a small molecule from the protein-targeting chimeras (PROTACs) that selectively targets the N-terminal domain (AR-NTD) of the Androgen Receptor variant AR-V7. By antagonizing AR-NTD, it effectively degrades AR-V7 protein and induces apoptosis in prostate cancer (PC) cells, with degradation efficiencies of 62.2% (1 μM) and 71.1% (5 μM) in VCaP cells [1].

Anti-SARS-CoV-2 S protein Antibody (NTD, SARS2-29) is a mouse-derived IgG1 kappa antibody that specifically targets the SARS-CoV-2 S protein. The recommended isotype control for this antibody is Mouse IgG1 kappa, Isotype Control.

Ralaniten (EPI-002) is a potent, specific, and orally active antagonist of the androgen receptor N-terminal structural domain (AR-NTD), inhibiting AR transcriptional activity with an IC50 value of 7.4 μM. Ralaniten exhibits anticancer activity and is used to study desmoplasia-resistant prostate cancer (CRPC).

Ralaniten triacetate (EPI-506), a precursor of Ralaniten, is a first-of-its-kind, orally active androgen receptor N-terminal structural domain (AR-NTD) inhibitor with anticancer activity and can be used to study prostate and breast cancer.

I-XW-053 is a micromolar affinity inhibitor of capsid-targeted HIV-1 replication, utilizing a hybrid structure-based method to block the interface between CA N-terminal domains (NTD-NTD interface).

5-Benzyloxygramine is an N protein PPI orthosteric stabilizer that exhibits both antiviral and N-NTD protein-stabilizing activities. It stabilizes the N-NTD dimers through simultaneous hydrophobic interactions with both partners, resulting in abnormal N protein oligomerization, which was further confirmed in cell studies[1]. [1]. Shan-Meng Lin, et al. Structure-Based Stabilization of Non-native Protein-Protein Interactions of Coronavirus Nucleocapsid Proteins in Antiviral Drug Design. J Med Chem. 2020 Mar 26;63(6):3131-3141.

NSC145366 is an inhibitor of Hsp90 activities which targets the Hsp90 C-terminal domain to induce allosteric inhibition and selective client downregulation. NSC145366 increases Hsp90 oligomerization resulting in allosteric inhibition of NTD ATPase activity (IC50=119μM) but does not compete with NTD or CTD-ATP binding.

Homo-BacPROTAC6, a ClpC1 NTD BacPROTAC degrader, effectively targets ClpC2, while Homo-BacPROTAC7 has been shown to efficiently kill M. tuberculosis [1].

Homo-BacPROTAC7, a ClpC1 NTD BacPROTAC degrader, targets ClpC2 and efficiently kills M. tuberculosis [1].

BacPROTAC-1, a potent mSA BacPROTAC degrader, exhibits high affinity for both mSA and the N-terminal domain (NTD) of ClpC, with dissociation constants (K D) of 3.9 μM and 2.8 μM, respectively [1].

BWA-522 is a small molecule, orally available protein-targeting chimera (PROTAC) that potentates the degradation of both full-length androgen receptor (AR-FL) and the AR-V7 splice variant. It specifically antagonizes the N-terminal domain (AR-NTD) of the androgen receptor (Androgen Receptor), prompting apoptosis in prostate cancer (PC) cells. In LNCaP xenograft models, BWA-522 demonstrated tumor growth inhibition (60 mg kg, po; TGI=76%). The compound effectively reduced levels of AR-V7 and AR-FL by 77.3% at 1 μM and 72.0% at 5 μM, respectively, in VCaP and LNCaP cell lines [1].

(±)-Pantothenic acid ((±)-Pantothenate), a B-vitamin, is crucial for coenzyme A (CoA) biosynthesis in mammalian cells and protects against valproic acid (VPA)-induced neural tube defects (NTD) in CD-1 mice [1].