4sc-101

Zotiraciclib, also known as TG02 and SB1317, is a novel small molecule potent CDK JAK2 FLT3 inhibitor. Zotiraciclib may be useful for the treatment of cancer that crosses the blood brain barrier and acts by depleting Myc through the inhibition of cyclin-dependent kinase 9 (CDK9). It is one of a number of CDK inhibitors under investigation; others targeting CDK9 for the treatment of acute myeloid leukemia include alvocidib and atuveciclib. Myc overexpression is a known factor in many cancers, with 80 percent of glioblastomas characterized by this property.

Vidofludimus hemicalcium (4sc-101; SC12267) is an orally active compound that acts as a dihydroorotate dehydrogenase (DHODH) inhibitor and serves as a novel modulator of the farnesoid X receptor (FXR). This immunomodulatory agent is utilized in the research of autoimmune disorders, including inflammatory bowel disease (IBD), and is explored for its potential in fatty liver disease research through FXR targeting.

Vidofludimus (SC12267) (4SC-101, SC12267) is a novel small molecule inhibitor of dihydroorotate dehydrogenase (DHODH).

C188-9 (TTI-101) is a Stat3 inhibitor with an IC50 of 4-7 μM.

AV-101 (4-Cl-KYN) , a prodrug antagonist at the glycine site of the NMDA receptor, has antidepressant activity and reduces levodopa-induced dyskinesia in MPTP monkeys.

KIN101 (3-(4-Bromophenyl)-7-[(methylsulfonyl)oxy]-4-oxo-4H-chromene), an isoflavone agonist of IRF-3 dependent signaling, induces IRF-3 nuclear translocation. KIN101 has antiviral activity against RNA viruses, HCV, and RSV.

Gemcitabine elaidate (CP-4126) hydrochloride is a lipophilic pro-drug of Gemcitabine, converted to Gemcitabine by esterases for phosphorylation. Unlike gemcitabine, Gemcitabine elaidate hydrochloride can be administered orally, displaying schedule and dose-dependent toxicity and antitumor activity.

Tyropeptin A-4 is used as a proteasome inhibitor.

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].

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).

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.

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.

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

KR-67607, also known as NTX-101 is novel selective 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1) inhibitor. KR-67607 decreased 4-hydroxynonenal expression and increased antioxidant and mucus secretion in BAC-treated rat eyes. KR-67607 showed its protective effects against ischemia-reperfusion-induced eye injury. KR-67607 effectively reduced cortisol levels in mouse eyes and maintained the trabecular meshwork (TM) structure in the presence of transient ischemic stress. Furthermore, KR-67607 reversed the elevation of intra-ocular pressure (IOP), suggesting that the TM structure maintained by KR-67607 prevented the excessive rise in IOP that exacerbates glaucoma.

INBRX-105 is a recombinant humanized bispecific antibody that targets programmed death-ligand 1 (PD-L1) and 4-1BB (CD137), exhibiting potential checkpoint inhibition, immune stimulation, and anti-tumor activity. By binding to 4-1BB on activated T-lymphocytes and PD-L1 on tumor cells, INBRX-105 enhances T-cell co-stimulation and inhibits PD-L1-mediated T-cell suppression, potentially reducing tumor growth. It demonstrates anti-tumor efficacy and increased T-cell frequency in patients with solid tumors and in vivo. Molecular weight: 101.9 kD.