n-51

CDK8/19-IN-51 is an orally active and highly effective dual inhibitor of CDK8 and CDK19, with anticancer activity. Its IC50 values for CDK8 and CDK19 are 5.1 nM and 5.6 nM, respectively. It is used in studies of colorectal and gastric cancers.

HDAC-IN-51 is an HDAC inhibitor.

HPK1-IN-51, serving as a PROTAC target protein ligand (Ligands for Target Protein for PROTACs), is utilized in synthesis processes.

PD-1 PD-L1-IN-51 (Compound III-4) is an inhibitor of PD-1 PD-L1 (IC50: hPD-L1 at 2.9 nM). It binds directly to PD-L1, blocking the interaction between PD-1 and PD-L1, and enhancing the release of IFN-γ. Additionally, PD-1 PD-L1-IN-51 exhibits antitumor activity.

NLRP3-IN-51 (Compound 3q) is an effective activator of the cholinergic anti-inflammatory pathway (CAP). This compound demonstrates potential for treating gouty arthritis as it inhibits the production of IL-1β in THP-1 cells induced by monosodium urate (MSU). Furthermore, NLRP3-IN-51 suppresses the phosphorylation of NF-κBp65 triggered by MSU without impacting the self-cleavage and activation of NLRP3, pro-caspase 1, or the second messenger caspase-1. Therefore, the initial stage of NLRP3 inhibition by NLRP3-IN-51 occurs through the activation of CAP.

HDAC6-IN-51 (Compound 7e) is a selective inhibitor of HDAC6, exhibiting an IC50 value of 42.9 nM. This compound demonstrates effective anti-pulmonary fibrosis activity.

COX-2-IN-51 (E25) is a potent COX-2 inhibitor with an IC50 of 70.7 nM. It significantly suppresses LPS-induced release of NO and PGE2, the expression of COX-2 and iNOS, and the activation of the NF-κB pathway. Displaying anti-inflammatory and analgesic effects in various mouse models through NF-κB pathway inhibition, COX-2-IN-51 has lower gastrointestinal side effects compared to Indomethacin.

HBV-IN-51 (Compound 17e) is an effective hepatitis B virus (HBV) capsid assembly modulator. It demonstrates significant anti-HBV activity with an EC50 value of 0.033 μM in HepAD38 cells. HBV-IN-51 exhibits good metabolic stability in plasma and is rapidly metabolized in human liver microsomes.

EGFR-IN-51 (Compound 6) is a highly potent EGFR inhibitor with IC50 values of 0.493, 102.60, and 461.63 μM against EGFR, EGFR L858R-TK, and EGFR T790M-TK targets, respectively. Additionally, EGFR-IN-51 exhibits cytotoxicity against cancer cell lines, effectively inducing apoptosis [1].

(23S,50S)-50-((((9H-Fluoren-9-yl)methoxy)carbonyl)amino)-23-(tert-butoxycarbonyl)-2,2-dimethyl-4,21,26,35,44-pentaoxo-3,30,33,39,42-pentaoxa-22,27,36,45-tetraazahenpentacontan-51-oic acid is a useful organic compound for research related to life sciences and the catalog number is T64767.

GlmU-IN-5175178 is an inhibitor of the acetyltransferase activity of Escherichia coli N-acetylglucosamine-1-phosphate-uridyltransferase glucosamine-1-phosphate-acetyltransferase (GlmU).

SARS-CoV-2-IN-51 (S-10), a lead compound for Omicron fusion inhibition, demonstrates potent activity against Omicron and other SARS-CoV-2 variants, with EC50 values ranging from 0.82-5.45 μM. It functions by directly interacting with the spike (S) protein in the prefusion state [1], thereby preventing viral entry.

Tubulin Polymerization-IN-51 (compound 7u) serves as a tubulin polymerization inhibitor, exhibiting an IC50 range of 2.55 - 17.89μM against SK-Mel-28 cells, and is applicable in cancer research [1].

ICMT-IN-51 (compound 43) is an ICMT inhibitor with an IC50 value of 0.55 μM [1].

HSD17B13-IN-51 (Compound 82), an inhibitor targeting hydroxysteroid 17β-dehydrogenase 13 (HSD17B13), exhibits potent activity with an IC50 value of ≤ 0.1 μM against estradiol. This compound is useful in researching various conditions including liver, metabolic, and cardiovascular diseases—specifically NAFLD, NASH, and drug-induced liver injury (DILI) [1].

PI3K-IN-51, characterized as a PI3K inhibitor, exhibits IC50 values below 500 nM for p120γ and p110δ p85α (WO2016204429A1; Example 10) [1].

VEGFR-2-IN-51 (compound 19) is an orally active dual-target inhibitor of VEGFR-2 (IC50=15.33 μM) and tubulin (IC50=0.76 μM) that exhibits antitumor activity. This compound induces apoptosis in tumor cells by reducing mitochondrial membrane potential and increasing levels of reactive oxygen species (ROS). Additionally, VEGFR-2-IN-51 suppresses angiogenesis through inhibition of the VEGFR-2 PI3K AKT signaling pathway. Moreover, it demonstrates significant antiproliferative effects on the gastric cancer cell line MGC-803 (IC50=0.005 μM).

5-(N,N-Hexamethylene)-amiloride (5-HMA) is an amiloride derivative that inhibits TRPA1-mediated calcium signaling (IC50: 35 μM). It functions as an inhibitor of the Na+ H+ exchanger (NHE) with Ki values ranging from 0.013 to 2.4 μM for various NHE isoforms. Additionally, 5-HMA blocks ASIC3 channels by 51% at 20 μM.

N-FormylglycineEthylEster is a useful organic compound for research related to life sciences. The catalog number is T65359 and the CAS number is 3154-51-6.

N-(4-Cyano-3-(trifluoromethyl)phenyl)-2-methyloxirane-2-carboxamide is a useful organic compound for research related to life sciences. The catalog number is T66252 and the CAS number is 90357-51-0.

(±)-Atropine-d3 (N-methyl-d3) is a deuterated compound of (±)-Atropine. (±)-Atropine has a CAS number of 51-55-8. Atropine Sulfate is the sulfate salt of atropine, a naturally-occurring alkaloid isolated from the plant Atropa belladonna. Atropine functions as a sympathetic, competitive antagonist of muscarinic cholinergic receptors, thereby abolishing the effects of parasympathetic stimulation.