inhibition

DL-AP5 is the racemic form of a selective N-methyl-D-aspartate (NMDA) receptor antagonist with anticonvulsant effects.

Nevadensin is an important herb-based constituent inhibiting estragole bioactivation. Nevadensin protects against a methyleugenol-induced marker of hepatocarcinogenicity in male F344 rat. It also exhibits inhibition activity against Mycobacterium tuberculosis, with equal MIC value of 200 microg/mL.

1. Rhapontin (Ponticin) can alleviate liver steatosis and improve blood glucose and lipid profiles in KK/Ay diabetic mice, indicates that rhaponticin has a noticeable antidiabetic effect and could be potentially used as a new agent to treat type 2 diabetes mellitus and its complications.

15-Lipoxygenase Inhibitor 1 is a selective inhibitor of 15-lipoxygenase, with an IC50 of 18 μM. 4-MMPB (15-Lipoxygenase Inhibitor 1) has IC50s of 19.5 μM and 19.1 μM for soybean 15-lipoxygenase (SLO) and human 15-lipoxygenase-1 (15-LOX-1), respectively. 4-MMPB has potential for the research of prostate cancer.

Triflumuron is an insecticide belonging to the group of so-called insect growth regulators. It inhibits the synthesis of chitin by the insect larvae, causing the die.

Mupirocin calcium hydrate is an antibiotic produced by Pseudomonas fluorescens, showed a high level of activity against staphylococci and streptococci and against certain gram-negative bacteria

BAMB-4 (ITPKA-IN-C14) is a highly membrane-permeable inhibitor of inositol-1,4,5-trisphosphate-3-kinase A (ITPKA), effectively suppressing the metastasis-promoting effect of ITPKA in lung tumor cells (with IC50 of 37 μM in ADP-Glo Assay).

AS057278 (3-Methylpyrazole-5-carboxylic acid) is an D-amino acid oxidase (DAAO) inhibitor.

Norethynodrel (Lynestrol) is a synthetic progestational hormone with actions and uses similar to those of PROGESTERONE. It has been used in the treatment of functional uterine bleeding and endometriosis. As a contraceptive, it has usually been administered in combination with MESTRANOL.

Oritavancin diphosphate (LY333328 diphosphate) is a novel semisynthetic glycopeptide antibiotic developed for treating serious Gram-positive bacterial infections.

TMPH is an inhibitor of nAChR and inhibits nAChRs lacking α5, α6, or β3 subunits. TMPH can be used in studies about nAChR dysfunction or neurological disorders.

Mupirocin (BRL-4910A) is a RNA synthetase inhibitor antibacterial. It has shown excellent activity against gram-positive staphylococci and streptococci.

SKLB4771 (FLT3-IN-1) is a novel potent and selective Flt3 inhibitor.

Itacnosertib (TP-0184) is an orally available ACRV1 (ALK-2), FLT3 and JAK2 inhibitor that inhibits the growth of tumor cells overexpressing ALK-2, overcomes FLT3 inhibitor resistance and synergistically inhibits AML growth with venetoclax, and possesses potential antitumor and antileukemic activity.

Cholesterol oxidase is a flavoenzyme that catalyzes the oxidation and isomerization of cholesterol to cholest-4-en-3-one. ChOx, an important virulence factor for Mycobacterium tuberculosis (Mtb), competitively inhibits TLR2 thereby inducing enhanced reactive oxygen species production by macrophages.

(+)-Hopeaphenol is isolated from A. indica (L.) and V. indica Linn with an IC50 value of 21.21 μM in α-glucosidase inhibition assay.

5-Fluorouracil (5-FU) is a uracil analog and inhibitor of DNA synthesis, exhibiting antitumor activity by affecting pyrimidine synthesis through thymidylate synthase inhibition; it induces apoptosis and autophagy.

ML385 is an NRF2 inhibitor (IC50=1.9 μM) with novelty and specificity. ML385 has anti-inflammatory activity by modulating anti-oxidative stress through the inhibition of NRF2. ML385 also exhibits anti-tumor activity.

Candoxatril (UK 79300) is an orally active neutral peptide endonuclease (NEP, EC 3.4.24.11) inhibitor that improves exercise capacity in patients with chronic heart failure undergoing angiotensin-converting enzyme inhibition.

OSMI-4 is a low nanomolar O-GlcNAc transferase (OGT) inhibitor (EC50 of 3 μM in cells) that can be used to study OGT inhibition in different human cell lines.

JNK-IN-8 (JNK Inhibitor XVI) is an irreversible JNK1/2/4 inhibitor (IC50: 4.7/18.7/1 nM) with over 10-fold selectivity compared to MNK2 and Fms, and no inhibition of Met, c-Kit, or PDGFRβ in the A375 cell line.

ITSA-1 is membrane permeable and specifically suppresses TSA inhibition of HDAC (histone deacetylase), but shows no activity towards other HDAC inhibitors.

Ivosidenib (AG-120) is an orally available inhibitor of isocitrate dehydrogenase type 1 (IDH1) with potential antineoplastic activity. It specifically inhibits a mutated form of IDH1 in the cytoplasm, preventing the formation of the oncometabolite 2-hydroxyglutarate (2 hG), which may induce cellular differentiation and inhibit cellular proliferation in IDH1-expressing tumor cells.

1. Ginkgetin has anti-influenza virus and anti-fungal activities. 2. Ginkgetin has anti-inflammatory activity, can down-regulates COX-2 induction in vivo against skin inflammatory responses. 3. Ginkgetin is a good STAT3 inhibitor and may be a useful lead