subunit-selective

DQP 1105 is a NMDA receptor antagonist.

CSN5i-3 is a potent, selective, and orally available inhibitor of the proteolytic subunit of the CSN complex, CSN5. It inhibits CSN-catalyzed Cul1 deneddylation with an IC50 value of 5.8 nM. CSN5i-3 has a killing effect on a variety of cancer cells and can be used as an anticancer drug. [2]

UK-101 is a small molecule inhibitor and a selective inhibitor of the immunoproteasome β1i (LMP2) subunit (IC50=104 nM), with 144-fold and 10-fold selectivity over the β1c and β5 subunits, respectively. This compound can induce apoptosis, possesses antitumor activity, and can be used for prostate cancer-related research.

Thiacloprid is a neonicotinoid insecticide that acts as a selective agonist at insect nicotinic acetylcholine receptors (nAChRs) with IC50values of 2.7 and 860 nM forDrosophilanAChRs and M10 mouse fibroblast cells expressing α4β2 subunit-containing nAChRs, respectively.1It is active against aphids, whiteflies, various species of beetle, andLepidopteraspecies when used at concentrations ranging from 48 to 180 g AI/hectare.2It has anti-estrogenic activity in a yeast estrogen screen and is toxic to adult female houseflies and mice (LD50s = 0.03 and 28 mg/kg, respectively).1,3Formulations containing thiacloprid have been used in the control of insects in agriculture. 1.Tomizawa, M., and Casida, J.E.Selective toxicity of neonicotinoids attributable to specificity of insect and mammalian nicotinic receptorsAnnu. Rev. Entomol.48339-364(2003) 2.Elbert, A., Erdelen, C., Kuhnhold, J., et al.Thiacloprid, a novel neonicotinoid insecticide for foliar applicationProc. Brighton Crop. Prot. Conf. - Pests and Diseases121-26(2000) 3.Westlund, P., and Yargeau, V.Investigation of the presence and endocrine activities of pesticides found in wastewater effluent using yeast-based bioassaysSci. Total Environ.607-608744-751(2017)

BMS-986169 is a high-affinity and selective negative allosteric modulator of the NMDA receptor GluN2B subunit, with an IC50 of 24 nM in oocytes, and exhibits antidepressant-like activity in mice, making it a potential treatment for treatment-resistant depression.

BMT-108908 FA is a selective negative allosteric modulator of the NMDA receptor GluN2B subunit, with an IC50 of 4.2 nM in oocytes and antidepressant-like activity in mice, and can be used for treatment-resistant depression.

(S)-BMT 108908 FA is the enantiomer of BMT 108908. BMT-108908 FA is a selective negative allosteric modulator of the NMDA receptor GluN2B subunit.

GSK3494245 is a Leishmania donovani inhibitor that suppresses trypsin-like activity catalyzed by the β5 subunit of L. donovani proteasome, applicable for visceral leishmaniasis (VL) studies.

Loreclezole is a selective GABAA receptor modulator and acts as a positive allosteric modulator of β2 or β3-subunit-containing receptors.

AZD-4573 is a selective and short-acting inhibitor of the serine/threonine cyclin-dependent kinase 9, the catalytic subunit of the RNA polymerase II elongation factor positive transcription elongation factor b. It also has a potential antineoplastic activ

Ro 25-6981 is a potent and selective activity-dependent NMDA receptors blocker containing the NR2B subunit with IC50s of 0.009 and 52 μM for cloned receptor subunit combinations NR1C/NR2B and NR1C/NR2A respectively. Ro 25-6981 can be used in studies about Parkinson's disease.

Ro 25-6981 Maleate is a potent and selective activity-dependent NMDA receptor blocker, specifically targeting the NR2B subunit (IC50 values are 0.009 μM for NR1C/NR2B and 52 μM for NR1C/NR2A receptor subunit combinations).

ILS-920 is a Rapamycin analog characterized by diminished immunosuppressive effects but remarkable neuroprotective properties. It exhibits selective binding affinity towards the immunophilin FKBP52 as well as the β1-subunit of L-type voltage-gated calcium channels (VGCC). ILS-920 displays a notable 200-fold preference for FKBP52 over FKBP12.

CIQ is a subunit-selective potentiator of NMDA receptors containing the NR2C or NR2D subunit, with EC50 values of 2.7 μM for NR2C and 2.8 μM for NR2D.

Helenalin is a selective inhibitor of transcription factor NF-κB by direct targeting of p65. It is an anti-inflammatory sesquiterpene lactone compound with alkylating activity. Through its ability to target the cysteine sulfhydryl groups in the p65 subunit of NF-κB, helenalin effectively inhibits its DNA binding.

NFPS exerts neuroprotection via glyR alpha1 subunit in the rat model of transient focal cerebral ischaemia and reperfusion. NFPS is a selective and non-competitive glycine transporter-1 (GlyT1) inhibitor (IC50s: 2.8 nM and 9.8 nM for hGlyT1 and rGlyT1, respectively).

PR-924 is a selective inhibitor of tripeptide epoxyketone immunoproteasome subunit LMP-7 (IC50: 22 nM). PR-924 inhibits growth and triggers apoptosis in multiple myeloma (MM) cells. PR-924 has antitumor activities. PR-924 covalently modifies proteasomal N-terminal threonine active sites.

Rpn11-IN-1 is an effective and selective inhibitor of proteasome subunit Rpn11 (IC50: 390 nM).

UBP 302 is an effective and selective GLUK5-subunit-containing kainate receptor antagonist (apparent Kd=402 nM) and displays very little affinity on GluK2 kainate receptors.

Immunoproteasome Activator 1 (compound A) is a selective immunoproteasome activator that enhances the presentation of individual MHC-I binding peptides by over 100 times. It binds to the proteasomal structural subunit PSMA1 and facilitates the association of the proteasome activators PA28α/β (PSME1/PSME2) with the immunoproteasome.

α5-GABAA receptor modulator 1 (Compound A-4) is a selective silent allosteric modulator (SAM) targeting the α5 subunit of GABAA receptors, useful for research into central nervous system (CNS) disorders.

NS11394 is a effective and subtype-selective GABA(A) receptor-positive modulator; possesses a functional efficacy selectivity profile of α(5) > α(3) > α(2) > α(1) at GABA(A) alpha subunit-containing receptors.

TCL1 acts as a selective non-covalent inhibitor targeting the Pru domain of the Rpn-13 subunit within the 19S regulatory particle (19S RP) of the proteasome, with an IC50 value around 26 μM. It disrupts the recognition and transport of ubiquitinated proteins by Rpn-13, thus inhibiting proteasomal degradation and affecting intracellular protein metabolism balance. TCL1 holds potential for research in hematologic malignancies.

FLY26 is a selective partial antagonist of GluN2B, with an IC50 value of 0.64 μM. FLY26 inhibits the GluN2B subunit of NMDA receptors, reducing calcium ion influx and reactive oxygen species (ROS) production. It also activates the BDNF/TrkB/CREB neuroprotective signaling pathway, mitigating excitotoxicity and mitochondrial dysfunction. FLY26 holds potential for treating neurological deficits caused by cerebral ischemia-reperfusion injury.