NC-001 (NC 001, NC001, az-NC-001) is a potent, specific, cell-permeable inhibitor of immunoproteasome caspase-like sites (β1i and β1), does not correlate with inhibition of chymotrypsin-like sites..

GCPII-IN-1 TFA is a glutamate carboxypeptidase II (GCPII, or PSMA) inhibitor scaffold with a Ki of 44.3 nM.

VTI-1002 is a potent and specific inhibitor of human (K i = 4.4 ± 2.0 nM) and murine (IC 50 = 179 ± 18 nM) GzmB, with minimal activity (IC 50 > 300 nM) against Cathepsin-G, neutrophil elastase and caspases (−3, −4, −5, −7, −8 and −9). In addition to its high specificity for GzmB, VTI-1002 is retained in murine skin for up to 24 hours and exhibits minimal toxicity in vivo with no observed adverse effects after 30 consecutive days of systemic administration in mice [31]. VTI-1002-mediated GzmB inhibition was first reported to augment type I collagen fibrillogenesis and improve tensile strength in a murine diabetic burn model, notably by preventing decorin cleavage and dermal fibrillar collagen network disorganization.

Org 34167 HCl salt is a broad-spectrum inhibitor of HCN channels with IC50 of 23.4, 8.2 and 9.2 uM for HCN1, HCN2 and HCN4 channels, respectively, slowing activation and causing a hyperpolarising shift in voltage-dependence of activation.

USP10-IN-3 is a HBX19818 analog, potent and selective USP10 inhibitor, but does not inhibit USP7 (IC50>100 uM).

Aflatoxin M2 is a major metabolite of Aflatoxin B1. Aflatoxin M2 is a mycotoxin produced by the fungi Aspergillus flavus and Aspergillus parasiticus. The level of toxicity associated with Aflatoxin is Aflatoxin B1>Aflatoxin M1>Aflatoxin G1>Aflatoxin B2>Aflatoxin M2>Aflatoxin G2.

Patulin (Terinin) is a mycotoxin produced by fungi including the Aspergillus, Penicillium, and Byssochlamys species, causes chromosome breakage, mutation, teratogenic and cytotoxic. Patulin induces autophagy-dependent apoptosis through lysosomal-mitochondrial axis, and causes DNA damage.

YD23 is a potent and highly selective degrader of SMARCA2. YD23 has potent tumor growth inhibitory activity in SMARCA4-mutant xenografts.

BI-9787 is a potent zwitterionic ketohexokinase inhibitor with nanomolar activity against hKHK-C, hKHK-A, mKHK-C and rKHK-C. BI-9787 shows >100-fold selectivity for all targets except PDE4D2.

VVD-130037 is an oral covalent activator of KEAP/NRF2 degrader.

EDP-235 is a SARS-CoV-2 3CLpro inhibitor with potent nanomolar activity against all SARS-CoV-2 variants, as well as clinically relevant human and zoonotic coronaviruses. EDP-235 maintains potency against variants bearing mutations associated with nirmatrelvir resistance. EDP-235 demonstrates a ≥ 500-fold selectivity index against multiple host proteases.

GSK3335103 is a highly potent and orally bioavailable nonpeptidic αvβ6 integrin inhibitor with pIC50 of 8.0. GSK3335103 shows high desirable oral pharmacokinetic profiles in rat, dog, and minipig, with low to moderate clearance, moderate volumes of distributio, high to complete oral bioavailabilities and high solubility in all physiological media.

JAB-3312 is a potent SHP2 allosteric inhibitor with binding Kd of 0.37 nM, enzymatic IC50 of 1.9 nM, KYSE-520 antiproliferative IC50 of 7.4 nM and p-ERK inhibitory IC50 of 0.23 nM, respectively.

QR-6401 is a highly potent and selective macrocyclic CDK2 inhibitor with IV50 of 0.37 nM. QR-6401 exhibits good selectivity against other closely related kinases, such as CDK1, CDK4, CDK6, CDK9 and GSK3β. QR-6401 demonstrates robust antitumor efficacy in an OVCAR3 ovarian cancer xenograft model via oral administration.

JNJ-74856665 is an orally bioavailable, potent, and selective DHODH inhibitor with IC50 of 0.40 nM. JNJ-74856665 shows favorable physicochemical properties and has been selected for clinical development in patients with AML and myelodysplastic syndromes (MDS).

Suvorexant (MK-4305) is a potent, selective, and orally bioavailable antagonist of OX1R and OX2R currently under clinical investigation as a novel therapy for insomnia.Suvorexant is an analytical reference standard categorized as a diazepane sedative.Formulations containing suvorexant show abuse potential similar to zolpidem in recreational polydrug users with a history of sedative and psychedelic drug use.2 Suvorexant is regulated as a Schedule IV compound in the United States. This product is intended for use in analytical forensic applications.

Sterculic acid is a stearoyl-CoA desaturase-1 (SCD1) inhibitor. Sterculic acid specifically inhibits the delta-9 desaturase (Δ9D) activity with an IC50 value of 0.9 μM.

DL-TBOA ammonium is a potent non-transportable inhibitor of excitatory amino acid transporters with IC50s of 70 μM, 6 μM and 6 μM for excitatory amino acid transporter-1 (EAAT1), EAAT2 and EAAT3, respectively. DL-TBOA ammonium inhibits the uptake of [14C]

DL-TBOA is a potent non-transportable inhibitor of excitatory amino acid transporters with IC50s of 70 μM, 6 μM and 6 μM for excitatory amino acid transporter-1 (EAAT1), EAAT2 and EAAT3, respectively. DL-TBOA inhibits the uptake of [14C]glutamate in COS-1 cells expressing the human EAAT1 and EAAT2 with Ki valuesof 42 μM and 5.7 μM, respectively. DL-TBOA blocks EAAT4 and EAAT5 in a competitive manner with Ki values of 4.4 μM and 3.2 μM, respectively.

TFB-TBOA (CF3-Bza-TBOA) is a potent glutamate transporter blocker that potently suppresses the activity of glial transporters. TFB-TBOA shows IC50 values of 22, 17, and 300 nM for glutamate transporters EAAT1, EAAT2, and EAAT3 respectively in an uptake assay using cells transiently expressing EAATs.

Specific inhibitor of vaccinia-related kinase 1 (VRK1)-mediated phosphorylation of barrier-to-autointegration factor (BAF)

BPA-B9 (Bipyridine amide B9) is a small molecule RXRα-targeted anti-mitotic agent, binds to RXRα (Kd=39 nM) and selectively inhibits the p-RXRα/PLK1 interaction to induce mitotic arrest and catastrophe in cancer cells.

Orlistat is a drug designed to treat obesity. Orlistat's primary function is preventing the absorption of fats from the human diet by acting as a lipase inhibitor, thereby reducing caloric intake. Orlistat is intended for use in conjunction with a healthcare provider-supervised reduced-calorie diet.

A-61603 is a selective α1A-adrenergic receptor agonist. A-61603 increases the frequency of spontaneous Ca2+ transients in rat ventricular myocytes in vitro.

RGT-419B is a CDK inhibitor and not only actively inhibits CDK2, CDK4 and CDK6, but also demonstrates strong anti-proliferation activities.

RGT-587 is a CDK inhibitor and selectively inhibits CDK4 but also has excellent brain penetration.

ZZ2 is a YPEL5-GID/CTLH-dependent BRD4 degrader with CD50 of 169 nM.

ZZ1 is a YPEL5-GID/CTLH-dependent BRD4 degrader with CD50 of 502 nM. ZZ1 induces selective degradation of BET proteins (BRD3 and BRD4).

Z6466608628 is a CRBN molecular gluewith EC50 of 0.34 µM. Z6466608628 selectively recruits PPIL4, along with its binding partner DHX40.

Compound 23 (LRRK2 inhibitor) is a potent, selective, and CNS penetrant LRRK2 inhibitor with IC50 of 5 nM.