Dihydromorin, a natural flavanonol compound, is a tyrosinase inhibitor[1].
Ovalbumin (154-159) is a fragment from ovalbumin. Ovalbumin (154-159) is a potent angiotensin-converting enzyme (ACE) inhibitor. Ovalbumin (154-159) can be used for research of hypertension[1][2].
Resorcinolnaphthalein is a specific angiotensin-converting enzyme 2 (ACE2) enhancer and activates ACE2 activity with an EC50 value of 19.5 μM. Resorcinolnaphthalein can be used for the investigation of hypertension and renal fibrosis[1].
SREBP/SCAP-IN-2(compound 13) is a selectiveSREBP/SCAPinhibitor[1].
CB 300919 is a water-soluble analogue of CB30865; has a continuous exposure (96 h) growth inhibition IC50 value of 2 nM in human CH1 ovarian tumor xenograft.IC50 value:Target: Nampt
Protamine sulfate, polycationic peptide and a antiheparin agent, could neutralize the anticoagulant action of heparin and enhances lipid-mediated gene transfer[1][2][3].
(+)-Talarozole is a potent inhibitor of retinoic acid metabolism extracted from patent WO 1997049704 A1.
Cathepsin X-IN-1 (compound 25) is a potent Cathepsin X inhibitor with an IC50 of 7.13 µM. Cathepsin X-IN-1 decreases PC-3 cell migration with low cytotoxic[1].
Darunavir ethanolate (TMC114 ethanolate) is a potent HIV protease inhibitor used to treat and prevent HIV/AIDS. Darunavir has a Ki of 1 nM for wild type HIV-1 protease.
MDL 27399 is an inhibitor of human neutrophil cathepsin G (Ki = 7 μM). MDL 27399 can be used for research of inflammatory diseases[1].
Atractylochromene is a potent dual inhibitor of 5-LOX/COX-1 with IC50s of 0.6 and 3.3 μM, respectively[1].
Tiprelestat is a potent human neutrophil elastase inhibitor. Tiprelestat has antimicrobial and anti-inflammatory activities. Tiprelestat can be used in the research of inflammation/immune disease[1].
Genistein 8-c-glucoside (G8CG) is a natural glucoside isolated from flowers of Lupinus luteus L. Genistein 8-c-glucoside induces mitochondrial membrane depolarization and induces apoptosis[1].
Faldaprevir (BI 201335) is a potent, orally active and selective noncovalent inhibitor of NS3/4A protease of HCV (hepatitis C virus) genotypes 1a and 1b, with Ki values of 2.6 and 2.0 nM, respectively. Faldaprevir inhibits HCV RNA replication, with EC50 values of 6.5 and 3.1 nM, respectively. Faldaprevir has potent antiviral activity against chronic HCV infection[1][2].
Endoproteinase Asp-N (Asp-N) is a metalloprotease that can specifically cleave the N-terminal side of aspartyl and cysteic acid residues[1].
JNJ-42226314 is a competitive, highly selective and reversible non-covalent monoacylglycerol lipase (MAGL) inhibitor. JNJ-42226314 demonstrates dose-dependent enhancement of the major endocannabinoid 2-arachidonoylglycerol (2-AG) as well as efficacy in models of neuropathic and inflammatory pain[1].
TRC051384 hydrochloride is a potent inducer of heat shock protein 70 (HSP70). TRC051384 hydrochloride exhibits protective effects against neuronal trauma via inhibition of necroptosis. TRC051384 hydrochloride can be used for the research of ischemic stroke[1][2].
Baceridin is a proteasome inhibitor and a cyclic hexapeptide. Baceridin can be isolated from the culture medium of Epiphytic Bacillus. Baceridin can inhibit cell cycle progression and induce tumor cell apoptosis through a p53-independent pathway. Baceridin can be used in cancer research[1].
Diaminopropionoyl tripeptide-33isa bioactive peptide with protects skin cells from UVA-induced DNA damages and has been reported used as a cosmetic ingredient[1].
(+)-Medioresinol Di-O-β-D-glucopyranoside is a lignan glucoside with strong inhibitory activity of 3', 5'-cyclic monophosphate (cyclic AMP) phosphodiesterase[1].
Dabigatran-13C6 is the 13C labeled Dabigatran[1]. Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM)[2][3].
Indinavir sulfate ethanolate (MK-639 ethanolate) is an orally active and selective HIV-1 protease inhibitor with a Ki of 0.54 nM for PR. Indinavir sulfate ethanolate exhibits anticancer activity by inhibiting the activation of MMPs-2 hydrolysis, anti-angiogenesis and inducing apoptosis. Indinavir sulfate ethanolate is also a SARS-CoV 3CLpro inhibitor[1][2][3][4].
DPP-IV-IN-2 is an inhibitor of both dipeptidyl peptidase IV (DPIV) and DP8/9 with IC50s of 0.1 and 0.95 μM, respectively.
Nepicastat Hcl(SYN117 Hcl; RS-25560-197 Hcl) is a dopamine beta-hydroxylase inhibitor with IC50 of 8.5 ± 0.8 and 9.0 ± 0.8 nM for bovine and human, respectively. IC50 value: 8.5/9.0 nM(bovine/human dopamine beta-hydroxylase)Dopamine beta-hydroxylase is an enzyme that catalyzes the conversion of dopamine to norepinephrine. Nepicastat (SYN117; RS-25560-197) has been studied as a possible treatment for congestive heart failure, and appears to be well tolerated as such.
Diosmetin is a natural flavonoid which inhibits human CYP1A enzyme activity with an IC50 of 40 μM in HepG2 cell.
Rhapontigenin is a natural analog of resveratrol with anticancer, antioxidant, antifungal and antibacterial activities. Rhapontigenin is amechanism-based, potent and selective cytochrome P450 1A1 inactivator (IC50 = 400 nM). Rhapontigenin exhibits 400-fold and 23-fold selectivity for P450 1A1 over P450 1A2 and P450 1B1, respectively[1].
(3S,5S)-Atorvastatin is a inactive enantiomer of Atorvastatin. (3S,5S)-Atorvastatin can activate pregnane X receptor (PXR). Atorvastatin is an orally active HMG-CoA reductase inhibitor, has the ability to effectively decrease blood lipids[1][2].
Carbonic anhydrase inhibitor 7 (compound 5b) is a potent inhibitor of human carbonic anhydrase (hCA), with Kis of 6.5 nM, 7.1 nM, 72.1 nM, and 255.8 nM for hCA IX, hCA II, hCA XII and hCA I, respectively[1].
LXRβ agonist-2 is a highly potent and β-selective liver X receptor (LXRβ) agonist with EC50 of 7 nM, displays 28.5-fold selectivity over LXRα (EC50=200 nM) and used in the treatment of atherosclerosis[1].
(S)-BI-1001 (Compound 11) is an active S-enantiomer of BI-1001. (S)-BI-1001 exhibits antiviral potency against HIV-1 integrase with an IC50 of 28 nM, an EC50 of 450 nM and a Kd of 4.7 μM[1].