as 101

Ossirene (AS101), a potent in vitro and in vivo immunomodulator, is a novel inhibitor of IL-1beta converting enzyme.

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.

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.

OY-101, an orally active compound, serves as a potent and specific inhibitor of P-glycoprotein (P-gp). It has the capability to sensitize drug-resistant tumors and counteract tumor multidrug resistance efficiently. Compared to Tetrandrine [1], OY-101 demonstrates enhanced water-solubility, cytotoxicity, and reversal activity.

EVT-101, also known as ENS-101, is an experimental medication which originated from Roche and is under development by Evotec AG for the treatment of major depressive disorder. It acts as a selective NMDA receptor subunit 2B (NR2B) antagonist.

INU-101 is an 11β-HSD1 inhibitor. In KKAy mice, ob/ob mice, and ZDF rats, oral administration of INU-101 led to enhanced insulin sensitivity and the lowering of the fasting level of glucose in the blood. INU-101 therefore shows promise as a potential treatment for type 2 diabetes and metabolic syndrome.

VMY-1-101 is a synthesized fluorescent CDK inhibitor. VMY-1-101 demonstrates potent CDK inhibitory activity, enhanced induction of G2/M arrest and modest apoptosis as compared to purvalanol B.

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.

Caveolin-1 (82-101) amide (human, mouse, rat), also known as Caveolin-1 scaffolding domain peptide, mitigates aging-related detrimental alterations in various organs and inhibits tyrosine kinases [1].

VH 101, a thiol (compound 20), serves as a VHL ligand essential for PROTAC synthesis [1].

AMY-101 TFA is a cyclic peptide that acts as an inhibitor of complement C3 and an immunomodulator, used for the treatment of gingivitis and periodontitis. It significantly reduces inflammation and lowers levels of MMP-8 and MMP-9. AMY-101 TFA also has a mitigating effect on lung inflammation/damage in patients with COVID-19-induced ARDS and acute kidney injury associated with SARS-CoV-2.

Poloxamer 101 L31 is a block copolymer of polyethylene oxide and polypropylene oxide, with an average molecular weight of 1100. It forms hydrogels and is used as a surfactant and emulsifier. Poloxamer 101 L31 may cause mild alveolitis.

(S)-OY-101 serves as the isomer of OY-101.

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.

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.