T21414

Sivelestat sodium (EI 546 sodium) is a highly efficient inhibitor of human neutrophil elastase, improving sepsis-induced myocardial dysfunction by activating the PI3K/AKT/mTOR signaling pathway. It can be used in acute lung injury/acute respiratory distress syndrome research.

TopoisomeraseI/IIα-IN-1 (Compound 20i) is an inhibitor of TopoisomeraseI/IIα. MDM2-IN-27 effectively blocks the inhibition of p53 by MDM2, thereby activating the p53 pathway. However, MDM2-IN-27 shows relatively poor antiproliferative activity against breast cancer, colon cancer, and cutaneous squamous cell carcinoma.

STAT3-IN-51 is a STAT3 inhibitor that binds directly to the SH2 domain of STAT3. This compound induces apoptosis, ferroptosis, and immunogenic cell death (ICD), enhancing antitumor immunity. It suppresses STAT3 activation (phosphorylation, p-STAT3) and its downstream signaling, while prompting reactive oxygen species (ROS) generation, decreasing Bcl-2 expression, disrupting mitochondrial functions, inhibiting GPX4 activity, and promoting lipid peroxidation. STAT3-IN-51 is applicable in research on colorectal cancer, breast adenocarcinoma, non-small cell lung cancer (NSCLC), and cisplatin-resistant lung adenocarcinoma.

4-Fluoro-α-Ethylaminoisohexanophenone hydrochloride is a drug derivative (Drug Derivative) employed in the research of neurological disorders.

Omigapil (CGP3466B free base) is an orally active inhibitor of GAPDH nitrosylation that can prevent tau acetylation, memory deficits, and motor dysfunction induced by Aβ1-42 in mice, highlighting its potential for Alzheimer's disease research. It is an effective inhibitor of apoptosis and is applicable in studies of congenital muscular dystrophy (CMD). Additionally, Omigapil serves as a click chemistry reagent due to its Alkyne group, which can engage in copper-catalyzed azide-alkyne cycloaddition (CuAAc) reactions with Azide-containing molecules.

(S)-(-)-Felodipine is the S-enantiomer of Felodipine and functions as an antihypertensive agent. As a derivative of 1,4-dihydropyridine, it acts as a vascular-selective calcium channel blocker. Felodipine inhibits activation of vascular effector cells and disrupts the contraction process in vitro. In canine models, it reduces mean arterial blood pressure by 20%. (S)-(-)-Felodipine exhibits a high metabolic rate in rat and canine liver microsomes.

KRASG12C IN-18 is an orally active covalent inhibitor of KRASG12C, achieving complete covalent binding to KRASG12C in both GDP- and GMPPNP-bound states. It exhibits significant antiproliferative activity against KRASG12C and its resistant mutations (including KRASG12C/R68S) with an IC50 in the low nanomolar range. KRASG12C IN-18 demonstrates notable in vivo efficacy in KRASG12C-driven solid tumors and KRASG12C/R68S xenograft models, making it applicable for colorectal adenocarcinoma research.

Cbz-QFR-kbt is a ketobenzothiazolone-based TMPRSS2 inhibitor with an IC50 of 0.42 nM. It also exhibits inhibitory activity against Matriptase, Hepsin, HGFA, and Factor Xa, with IC50 values of 1, 1.3, 85, and 85 nM, respectively. Furthermore, Cbz-QFR-kbt demonstrates significant inhibitory effects on SARS-CoV-2 and H1N1 (IC50= 60 nM) and is applicable for antiviral research.

Glucokinase activator10 is a thiazole compound that acts as a liver-selective, orally bioavailable activator of glucokinase (glucokinase), with an EC50 of 42 nM. It demonstrates significant glucose-lowering effects in oral glucose tolerance tests (OGTT) involving acutely diet-induced obese mice. Glucokinase activator10 is suitable for research in metabolic disorders.

MGMT-IN-1 (Compound 2) is a photoactivatable inhibitor of MGMT. It only effectively enhances the cytotoxicity of Temozolomide (TMZ) under light exposure, significantly increasing TMZ-induced DNA damage. MGMT-IN-1 is applicable for research in toe giant cell tumor.

SSTR4 agonist6 (Compound 1) is an agonist of SSTR4 that can be used in pain research.