nr 1

Rheb inhibitor NR1 is a Rheb inhibitor and selective mTORC1 inhibitor.Rheb inhibitor NR1 inhibits the phosphorylation of T389pS6K1 and promotes the phosphorylation of S473pAKT.

NR2F1 agonist 1, a specific nuclear receptor NR2F1 activator, initiates dormancy programs in cancer cells by upregulating NR2F1 and its target genes controlling dormancy. This compound promotes neural crest-like features and suppresses growth in head and neck squamous cell carcinoma (HNSCC) through NR2F1 activation. Moreover, NR2F1 agonist 1 demonstrates tumor growth inhibition in a mouse primary tumor model.

NR2F6 modulator-1 is a potent modulator of nuclear receptor subfamily 2, group F, member 6 (NR2F6). NR2F6 modulator-1 can be used to study immune regulation and modulation of tumour stem cell activity.

Tat-NR2B9c acetate (NA-1 acetate) is a postsynaptic density-95 (PSD-95) inhibitor, with EC50 values of 6.7 nM and 670 nM for PSD-95d2 (PSD-95 PDZ domain 2) and PSD-95d1, respectively. Tat-NR2B9c acetate disrupts the PSD-95/NMDAR interaction, inhibiting NR2A and NR2B binding to PSD-95 with IC50 values of 0.5 μM and 8 μM, respectively. Tat-NR2B9c acetate also inhibits neuronal nitric oxide synthase (nNOS)/PSD-95 interaction, and possesses neuroprotective efficacy.

CK1-IN-2 (compound Nr.4) is a potent inhibitor of CK1, exhibiting IC50 values of 123 nM for CK1a, 19.8 nM for CK1d, 26.8 nM for CK1e, and 74.3 nM for p38a [1].

NR-NO2 is a prospective therapeutic agent with targeted delivery and image-guided capability for use in antitumor studies, also demonstrating antibacterial effects [1].

SRC-1 (686-700) is a bioactive peptide encompassing amino acids 686 to 700, which include the second LXXLL motif from NR box II of steroid receptor coactivator (SRC1). These coactivator proteins facilitate transcription by ligand-dependent interaction with nuclear receptors.

NR-7h is a potent and selective degrader of p38α and p38β, exhibiting DC50 values of 24 nM for p38α in T47D cells and 27.2 nM in MB-MDA-231 cells, respectively [1].

Tat-NR2B9c TFA is a 20-aa peptide, and acts as an inhibitor of postsynaptic density-95 (PSD-95)(EC50 of 6.7 nM for PSD-95d2), and possesses neuroprotective efficacy.

NR1H4 activator 1 is a potent and selective agonist of Famesoid X Receptor (FXR).

Tat-NR2B9c (NA-1) is a postsynaptic density-95 (PSD-95) inhibitor with neuroprotective and antiepileptic effects.Tat-NR2B9c inhibits PSD-95d2, PSD-95d1, and PSD-95, which prevents the activation of NMDA-induced NADPH oxidase in neurons, thereby blocking the production of superoxide, which reduces ischemic injury in the acute phase after stroke.