subunit-selective

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]

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)

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.

Icerguastat (IFB-088) is a selective inhibitor of holophosphatase. Sephin1 safely and selectively inhibited a regulatory subunit of protein phosphatase 1 in vivo.

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

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.

DQP 1105 is a NMDA receptor antagonist.

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.

σ receptor agonist and NR2B subunit-selective NMDA receptor antagonist

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.

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).

Dezapelisib is an orally bioavailable, selective inhibitor of the delta isoform of the 110 kDa catalytic subunit of class I phosphoinositide-3 kinases (PI3K). INCB040093 prevents both the production of the second messenger phosphatidylinositol-3,4,5-trisp

Rp-8-CPT-cAMP is a structural combination of the lipophilic and non-hydrolyzable cAMP analogs, 8-CPT-cyclic AMP and Rp-cyclic AMPS .[1] It functions as a site-selective inhibitor of protein kinase A (PKA) type I and II, with preference towards site A of type I and site B of type II.2 By occupying cAMP binding sites at the regulatory subunit of PKA, Rp-8-CPT-cAMP prevents the kinase holoenzyme from dissociative activation.[2],[3]

ONX-0914 (PR-957) TFA is a selective, noncompetitive, irreversible inhibitor of the chymotrypsin-like subunit (LMP7) of the immunoproteasome, effectively blocking cytokine production and mitigating experimental arthritis progression. With a K_i value of 5.2 μM against the mycobacterial proteasome, ONX-0914 TFA also reactivates latent HIV-1 by inducing p-TEFb activation through HSF-1 mediation [1] [2] [3].

pdTp is a highly selective, small-molecule miRNA regulatory complex RISC subunit SND1 inhibitor.

GluN2B receptor modulator-1 is a potent and selective allosteric modulator of the GluN2B receptor, demonstrating negative modulation by inhibiting receptor activity and exhibiting high selectivity towards the GluN2B subunit, with an IC50 value of 31 nM.

Besonprodil is a drug that acts as an NMDA antagonist and is selective for the NR2B subunit.

UBP714 is a derivative of the NMDA receptor negative allosteric modulator UBP608. It also enhanced NMDAR mediated field EPSPs in the CA1 region of the hippocampus. UBP714 is a novel template for the development of potent and subunit selective NMDAR potent

Traxoprodil Mesylate is a potent noncompetitive N-methyl-D-aspartate (NMDA) receptors antagonist and has selective for the NR2B subunit.

Nemvaleukin alfa (ALKS 4230) is an interleukin 2 fusion protein, a selective agonist of the medium-affinity IL-2 receptor, produced by fusion of the IL-2Ralpha subunit of the circularly arranged interleukin-2 (IL-2) and IL-2 receptor (IL-2R) complexes, which drives antitumor Immunity and inhibits tumor growth in small cell lung cancer.

Brazikumab (AMG 139) is a humanized antibody targeting IL-23 by binding to the P19 subunit. It is a selective IL23p19 antagonist and can be used in Crohn's disease research.

Br-PBTC is a highly potent, 2/4 subtype-selective positive allosteric modulator of nicotinic acetylcholine receptors (nAChRs). It specifically targets α2β2, α2β4, α4β2, α4β4, (α4β2)2α4, and (α4β2)2β2 subtypes of nAChRs, with EC50 values ranging from 0.1 to 0.6 μM. Br-PBTC exerts its activity by binding to the c-tail region of an α subunit.

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

BMS 195614 (BMS614) is a selective RARα antagonist. BMS 195614 can bind to the RARα subunit.