as 101

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.

KHS101 is a novel inhibitor of transforming acidic coiled-coil protein 3 (TACC3). It is a selective inducer of neuronal differentiation.

AVN-101 is a highly potent 5-HT7 receptor antagonist with a Ki value of 153 pM. AVN-101 also exhibits considerable affinity for histamine H1 (Ki value of 0.58 nM) and adrenergic α2A, α2B and α2C (Ki values ​​of 0.41-3.6 nM) receptors. AVN-101 has shown good oral bioavailability and brain-blood barrier permeability, low toxicity and reasonable efficacy in animal models of central nervous system diseases.

UFP-101 acetate is a selective and competitive antagonist of the NOP receptor (pKi = 10.24) with >3000-fold selectivity over δ, μ, and κ opioid receptors.

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.

GlyH-101 is a cell-permeable glycinyl hydrazone compound that blocks CFTR with Ki of 1.4 uM.

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

UCPH-101 is an inhibitor of excitatory amino acid transporter subtype 1 (EAAT1) with an IC50 of 0.66 μM.

CUDC-101 is a potent inhibitor of HDAC, EGFR, and HER2 with IC50s of 4.4 nM, 2.4 nM, and 15.7 nM, respectively.

UCF 101 is a specific inhibitor of HtrA2 and reduces apoptosis in PC12 cells.

JI-101 (CGI-1842) is an oral multi-kinase inhibitor that targets vascular endothelial growth factor receptor type 2 (VEGFR-2), platelet derived growth factor receptor β (PDGFR-β), and ephrin type-B receptor 4 (EphB4).

RG-101 is a hepatocyte-targeted N-acetylgalactosamine conjugated oligonucleotide that functions as an antagonist for miR-122, an essential host factor in the replication of the hepatitis C virus (HCV).

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.

Complement component C3 plays a particularly versatile role in this process by keeping the cascade alert, acting as a point of convergence of activation pathways, fueling the amplification of the complement response, exerting direct effector functions, and helping to coordinate downstream immune responses[3]. In C3-/- mice alcohol-induced liver steatosis is absent or strongly reduced after chronic or acute alcohol exposure. This suggests that the complement system and its component C3 contribute to the development of alcohol-induced fatty liver and its consequences[4].AMY-101 TFA (Cp40 TFA) is a peptidic inhibitor of the central complement component C3 (KD: 0.5 nM). It shows a favorable anti-inflammatory activity in models with COVID-19 severe pneumonia with systemic hyper inflammation[5].a daily subcutaneous dose of AMY-101 (4 mg/kg bodyweight) was protective against NHP periodontitis, suggesting that patients treated for systemic disorders (e.g., paroxysmal nocturnal hemoglobinuria) can additionally benefit in terms of improved periodontal condition[6].Plasma concentrations of both C3 and Cp40 were measured periodically and complete saturation of plasma C3 was confirmed. No differences in hematological, biochemical, or immunological parameters were identified in the blood or tissues of animals treated with Cp40 when compared to those injected with vehicle alone. Further, skin wounds showed no signs of infection in those treated with Cp40.Cp40 treatment was associated with a trend toward accelerated wound healing when compared with the control group. In addition, a biodistribution study in a rhesus monkey indicated that the distribution of Cp40 in the body is associated with the presence of C3, concentrating in organs that accumulate blood and produce C3[7].

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.

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.

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.

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].

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.

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

Retrocyclin-101 is an antimicrobial peptide exhibiting activity against bacterial and viral pathogens [1].

ZJ-101, a structurally simplified analog of the marine natural product superstolide A, exhibits potent antiproliferative activity by targeting and inhibiting O-glycosylation, thereby modulating the endomembrane system and inhibiting cell-cell adhesion [1].

MZ-101 is an inhibitor of glycogen synthase 1 (GYS1) and can be used to study diseases mediated by GYS1 [1].

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

Yellow 101 is a bioactive chemical.

ORP-101 is a new chemical entity designed with intent to create a large stable molecule and to confer partial μ agonist and full κ-antagonist receptor pharmacology.

Antibacterial agent 101 exhibited antibacterial and antifungal effects (MIC=4-32 μg/mL).

AQ-101 is a inhibitor of MDM2, which induces MDM2 protein degradation through a self-ubiquitination and proteasome-mediated mechanism.

VH 101, acid, a functionalized von-Hippel-Lindau (VHL) protein ligand, facilitates PROTAC research and development. It comprises an E3 ligase ligand and an alkyl linker featuring a terminal amine for easy conjugation to target protein ligands [1].

UWA-101 hydrochloride is a selective, non-cytotoxic inhibitor of DAT/SERT, demonstrating EC50 values of 3.6 µM for DAT and 2.3 µM for SERT inhibition. It mitigates motor disorders and other side effects associated with dopaminergic agent use (e.g., L-DOPA) without exhibiting psychotropic effects. This compound is utilized in research focused on neurodegenerative conditions like Parkinson's disease [1] [2].

JTK-101 is a potent and selective Tat-dependent HIV-1 replication inhibitor.

Mvt 101 is a peptide inhibitor.

Antitumor agent-101 is a selective, covalent inhibitor targeting lysine methyltransferases G9a GLP, demonstrating IC50 values of 8.5 nM for G9a and 5.5 nM for GLP. It exhibits antitumor efficacy in the PANC-1 xenograft model [1].

KRP-101, a PPARɑ agonist, is used potentially for the treatment of diabetes and hyperlipidaemia.

IAXO-101 interferes with TLR4/CD14 signals in humans, rats, and mice.

MAL3-101 is a molecular chaperone inhibitor of heat shock protein 70 (Hsp 70).

Functionalized von-Hippel-Lindau protein ligand (VHL) for PROTAC research and development; incorporates an E3 ligase ligand plus an alkylC6 linker with terminal amine ready for conjugation to a target protein ligand. Part of a range of functionalized tool molecules for PROTAC R&D. PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license.

LEI-101 is a potent, selective, and orally bioavailable cannabinoid CB2 receptor agonist, with a pEC50 of 8 for hCB2, and a pKi of less than 4 for hERG. LEI-101 is approximately 100-fold more potent in binding to CB2 receptors than to CB1 receptors. It has therapeutic potential in diseases associated with inflammation and or oxidative stress, including kidney disease [1] [2].

LEI 101 hydrochloride is potent and selective CB2 partial agonist.

KHS 101 hydrochloride is a neuronal differentiation inducer

PLM-101 is an anticancer compound orally active against acute myeloid leukemia by targeting FLT3 and RET. It impedes RET function, promoting autophagic breakdown of FLT3, and suppresses the PI3K and Ras/ERK pathways, contributing to its anti-leukemic effects. The compound's antitumor efficacy is demonstrated in both a mouse MV4-11 flank xenograft model (doses of 3 and 10 mg/kg; po) and an allogeneic xenograft mouse model (dose of 40 mg/kg; po) [1].

PHI-101 is an orally available and selective checkpoint kinase 2 (Chk2) inhibitor for the study of refractory acute myelogenous leukemia (AML) and ovarian cancer.

Anticancer Agent 101, a tetracaine derivative, exhibits anti-cancer activity [1].

AVN-101 is a very potent 5-HT7 receptor antagonist, with slightly lesser potency toward 5-HT6, 5-HT2A, and 5HT-2C receptors. It is a multi-target drug candidate for the treatment of CNS disorders.

Functionalized von-Hippel-Lindau protein ligand (VHL) for PROTAC research and development; incorporates an E3 ligase ligand plus an alkylC4 linker with terminal amine ready for conjugation to a target protein ligand. Part of a range of functionalized tool molecules for PROTAC R&D. PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license.

AMY-101 is a peptidic inhibitor of the central complement component C3 (KD: 0.5 nM). AMY-101 shows a favorable anti-inflammatory activity in models with COVID-19 severe pneumonia with systemic hyper inflammation.

Sulforhodamine 101 DHPE, a fluorescent probe, results from the conjugation of sulforhodamine 101, a red fluorescent dye with excitation/emission spectra of 586/605 nm, to the phospholipid 1,2-dipalmitoyl-sn-glycero-3-PE. It effectively integrates into phospholipid bilayers and is utilized for imaging solid supported lipid bilayers, detecting protein-ligand interactions on bilayers, and monitoring lipid probe colocalization in liposomes through resonance energy transfer (RET).

EGFR-IN-101 (I-10), a 2-phenylamino pyrimidine derivative, is an EGFR inhibitor with IC50 values of 33.26 nM for EGFR L858R T790M C797S and 106.4 nM for Ba F3-EGFR L858R T790M C797S. It is applicable in the study of non-small cell lung cancer (NSCLC) [1].