at 101

Gossypol acetic acid (AT101), a polyphenolic compound isolated from cottonseeds, binds with Bcl-2, Bcl-xL, Mcl-1, and does not inhibit BIR3 domain and BID.

(R)-(-)-Gossypol acetic acid (AT101 acetate), the R-(-) enantiomer of Gossypol acetic acid, binds with Bcl-2, Bcl-xL, and Mcl-1 with Ki values of 0.32 μM, 0.48 μM, and 0.18 μM, respectively; it does not inhibit the BIR3 domain or BID. [Phase 2]

UK-101 is a potent and selective inhibitor of the immunoproteasome LMP2, inhibiting β1i (LMP2), β1c (LMP2), and β5 (LMP2), with IC50s of 104 nM, 15 μM, and 1 μM, respectively. UK-101 exhibits a 144-fold and 10-fold higher affinity for β1i than for the distribution of β1c and β5 subunits. UK-101 induces apoptosis and can be used to study prostate cancer-related diseases.

XY101 is a selective, metabolically stable and orally available agonist of RORγ inverse(IC50 of 30 nM and a Kd of 380 nM).

KYN-101 is an orally active and selective aryl hydrocarbon receptor (AHR) inhibitor with anticancer activity. KYN-101 decreases CYP1A1 mRNA expression and can be used in the study of breast cancer and acute myeloid leukemia. KYN-101 is an orally active and selective aryl hydrocarbon receptor (AHR) inhibitor with anticancer activity.

ULK-101 is a potent and selective inhibitor of ULK1 (IC50s: 8.3/30 nM for ULK1/ULK2). It can suppress autophagy.

RB 101 suppresses enkephalinase and aminopeptidases; biologically cleaved at disulfide to produce inhibitors of both aminopeptidase N and neutral endopeptidase.

PKUMDL-LC-101-D04 is a potent allosteric activator of glutathione peroxidase 4 (GPX4), a regulator of ferroptosis. GPX4 activity was increased to 150% of control levels when used at a concentration of 20 μM in a cell-free assay, and at a concentration of 61 μM in wild-type, but not Gpx4-/-, mouse embryonic fibroblast (MEF) extracts.PKUMDL-LC-101-D04 (200 μM) reduced cholesterol peroxide-induced MEF death.

EVT-101 is a GluN2B antagonist, binding at the same GluN1/GluN2B dimer interface as ifenprodil but adopting a remarkably different binding mode involving a distinct subcavity and receptor interactions.

SWE101 is a potent human and rat soluble epoxide hydrolase (sEH)-P inhibitor(IC50s of 4 μM and 2.8 μM, respectively).

Enmetazobactam (AAI101) is an extended-spectrum β-lactamase inhibitor used to treat multi-drug resistant gram-negative bacterial infections.

CMPD101 is a membrane-permeable small-molecule inhibitor of GRK2/3 (IC50: 18 nM and 5.4 nM). Which can be used for the study of heart failure. CMPD101 exhibits less selectively against GRK1, GRK5, ROCK-2 and PKCα with IC50s of 3.1 μM , 2.3 μM, 1.4 μM and 8.1 μM, respectively.

ORIC-101 is a highly effective and selective glucocorticoid receptor antagonist (EC50: 5.6 nM). It also has anti-cancer activity.

VH 101, phenol is a VHL ligand based on VH032. It is able to utilize linkers to ligands of target proteins to yield PROTAC molecules such as PROTAC 1. PROTAC 1 is a partial degrader of SMARCA2 and SMARCA4.

HP-101 is the first dual substrate inhibitor of HPPK to demonstrate cellular permeability.

SARS-CoV-2-IN-101 (compound 10O) is an effective orally active inhibitor of SARS-CoV-2 with an EC50 value of 0.64 µM against HCoV-229E. This compound exhibits cytotoxicity and can reduce the expression levels of HCoV-229E N protein and RNA. Additionally, SARS-CoV-2-IN-101 has broad-spectrum antiviral activity against coronaviruses.

KL101 is a novel CRY1 stabilizer with selective action.

Lipid U-101 is an ionizable cationic lipid extensively used in the formulation of lipid nanoparticles (LNPs) for mRNA delivery.

trans-VH 101-Thiol-C-cyclohexane-p-C-OTs is a conjugate of the E3 ligase VHL ligand and linker, employed for the synthesis of the PROTAC degrader dBAZ2.

VH 101-amide-piperidine-Pip-alkyne is an E3LigaseLigand-Linker Conjugate used in the synthesis of PROTAC degraders. The linker component is tert-Butyl 4-ethynyl-[1,4'-bipiperidine]-1'-carboxylate, and the VHL-based E3 ubiquitin ligase ligand is VH 101, acid.

ENX-101 is an orally active partial positive allosteric modulator (PAM) of the (GABAA) receptor. It selectively targets the α2β2γ2L (EC50= 0.76 nM), α2β3γ2L (EC50= 0.61 nM), α3 (EC50= 1.97 nM), and α5 (EC50= 0.85 nM) subunits of the GABA receptor. ENX-101 demonstrates anticonvulsant activity in various animal models.

Anti-inflammatory agent 101 (Compound C04) is an orally active anti-inflammatory agent with notable anti-lipid accumulation, anti-inflammatory, and anti-fibrotic properties. It functions by reducing fatty acid uptake, enhancing fatty acid oxidation, and alleviating inflammation, making it applicable in the study of NASH and related liver fibrosis.

E3LigaseLigand-linker Conjugate 101 is a conjugate consisting of an E3 ligase ligand and a linker, specifically made up of (S,R,S)-AHPC and a corresponding linker. (S,R,S)-AHPC is a von Hippel-Lindau (VHL) ligand based on VH032, capable of recruiting VHL protein. This conjugate is a crucial intermediate for synthesizing complete PROTACs molecules.

HSD17B13-IN-101 is a selective inhibitor of 17β-hydroxysteroid dehydrogenase (HSD17B13), exhibiting an IC50 value of less than 0.1 μM for estradiol. It is applicable in research on non-alcoholic fatty liver disease (WO2023146897A1; compound 94).