reversible

SP600125 (JNK Inhibitor II) is a JNK inhibitor that inhibits JNK1, JNK2, and JNK3 (IC50=40 40 90 nM) with oral potency, reversibility, and ATP-competitive properties. SP600125 inhibits autophagy and induces apoptosis.

LDN-27219 is a potent hTGase inhibitor with IC50 of 0.6 uM.

Bortezomib (LDP 341) is a 20S proteasome inhibitor (Ki=0.6 nM) that is reversible and selective. Bortezomib has antitumor activity and inhibits NF-κB, which can disrupt the cell cycle and induce apoptosis.

Iptacopan hydrochloride (LNP023 hydrochloride) is an orally bioavailable, highly potent and highly selective factor B inhibitor with an IC50 of 10 nM. Iptacopan hydrochloride shows direct, reversible, and high-affinity binding to human factor B with a KD of 7.9 nM.

(+)-JQ-1 (JQ1) is a specific, reversible BET bromine domain inhibitor that targets BRD4 (1 2) with IC50 values of 77 33 nM. (+)-JQ-1 induces cell autophagy and inhibits cell proliferation.

Leupeptin hemisulfate is a protease inhibitor with cell membrane-permeable, reversible, competitive, and oral activities. Leupeptin hemisulfate inhibits the activity of Cathepsin B, Cathepsin H, and Cathepsin L, and blocks fusion of amphipathic lysosomes. Leupeptin hemisulfate also has anti-inflammatory activity.

Ulixertinib (VRT752271) (BVD-523, VRT752271) is an effective and reversible ERK1 ERK2 inhibitor. The IC50 of Ulixertinib is less than 0.3 nM for ERK2.

Trichostatin A (TSA), a natural derivative of diene isohydroxamic acids, is a specific and reversible histone deacetylase inhibitor (IC50=1.8 nM) that induces hyperacetylation of core histones to regulate chromatin structure.

Clozic (ICI 55897) exhibits reversible anti-proliferative effects and can be used in studies about serving as a potential anti-arthritic agent.

TVB-3664 is an orally active, selective, reversible, and highly bioavailable fatty acid synthase inhibitor (FASN) with an IC50 for palmitate synthesis of 18 nM in human and 12 nM in mouse.Significantly inhibits microtubule protein palmitoylation and mRNA expression.

PND-1186 (VS-4718) is a specific and reversible FAK inhibitor with an IC50 of 1.5 nM.

GSK484 hydrochloride (GTPL8577) is a reversible peptidyl-arginine deiminase 4 (PAD4) inhibitor. It binds to PAD4 with high affinity, with IC50 of 250 and 50 nM in the presence and absence of 2 mM calcium, respectively. GSK484 promotes the radiosensitivity of colorectal cancer (CRC) and inhibits NET formation in vitro and in vivo.

GSK3685032 is a non-covalent and selective DNMT1 inhibitor(IC50 = 36 nM). The inhibitory effect is time-independent and reversible. GSK3685032 induces loss of DNA methylation and transcriptional activation and inhibits cancer cell growth.

Bafilomycin A1 belongs to the macrolide class of antibiotics and is a V-ATPase inhibitor (IC50=0.44 nM) that is specific and reversible. Bafilomycin A1 is an inhibitor of the late phase of autophagy, blocking the fusion of autophagosomes with lysosomes. Bafilomycin A1 also induces apoptosis.

MG-132 (Z-Leu-Leu-Leu-al) is a 26S proteasome inhibitor (IC50=100 nM) that is cell-permeable and reversible. MG-132 acts as an autophagy activator and also induces apoptosis.

Finrozole (MPV 2213ad) is a novel selective aromatase inhibitor that is partially reversible for breast development.

β-NETA (α-NETA) is a stable, noncompetitive, slowly reversible choline acetyltransferase (ChAT) inhibitor with an IC50 of 9 μM and is a potent chemokine-like receptor-1 (CMKLR1) antagonist. β-NETA has anti-cancer activity[1][2]. β-NETA weakly inhibits cholinesterase (IC50=84 µM) and acetylcholinesterase (IC50=300 µM).

RMM-46 is a reversible covalent inhibitor with high ligand efficiency and selectivity for MSK RSK family kinases.

Esuprone (LU-43839) is a novel reversible and highly selective MAO-A inhibitor with anticonvulsant activity for the treatment of depression.

Abeprazan hydrochloride (Fexuprazan hydrochloride) is an effective reversible potassium-competitive acid blocker with oral activity, inhibiting H+, K+ -atPase by competitive binding to potassium ions without acid activation. Abeprazan hydrochloride is a proton pump inhibitor (PPI) that acts by reducing gastric acid production and is used to treat gastric acid-related disorders, such as gastroesophageal reflux disease (GERD) and peptic ulcers.

Elinogrel (PRT060128) is a competitive and reversible antagonist of platelet P2Y12 with IC50 of 20 nM and exhibits potent antiplatelet effects.

nor-NOHA acetate (Nω-Hydroxy-nor-L-arginine acetate) is a reversible inhibitor of arginase with anti-leukemic activity, effective in treating endothelial dysfunction, immunosuppression, and metabolism regulation.

MLS000544460 is a highly selective and reversible Eya2 phosphatase inhibitor (Kd: 2.0 μM, IC50: 4 μM) that exhibits inhibitory effects on Eya2 phosphatase-mediated cell migration and has anticancer activity.

Elubrixin (SB-656933) inhibits neutrophil CD11b upregulation (IC50 of 260.7 nM) and shape change (IC50 of 310.5 nM). Elubrixin can be used for inflammatory diseases such as inflammatory bowel disease and airway inflammation. Elubrixin is a potent, selective, competitive, reversible and orally active CXCR2 antagonist and an IL-8 receptor antagonist.