Enniatin B1 is a Fusarium mycotoxin. Enniatin B1 inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity with an IC50 of 73 μM in an enzyme assay using rat liver microsomes[1]. Enniatin B1 crosss the blood-brain barrier[2]. Enniatin B1 decreases the activation of ERK (p44/p42). Enniatin B1 inhibits moderately TNF-α-induced NF-κB activation[3].
Bortezomib (PS-341) is a potent 20S proteasome inhibitor with a Ki of 0.6 nM.
Tripterin (Celastrol) is a proteasome inhibitor which potently and preferentially inhibits the chymotrypsin-like activity of a purified 20S proteasome with IC50 of 2.5 μM.
Rennin, also known as Chymosin, is a pepsin-related proteolytic enzyme synthesized by cells in the stomach of certain animals that efficiently converts liquid milk into a semi-solid, allowing it to remain in the stomach for longer. The natural substrate of Rennin is K-casein, which is specifically cleaved at the peptide bond between amino acid residues 105 and 106, phenylalanine and methionine, and is widely used in cheese production[1].
Saxagliptin(BMS477118) is a selective and reversible DPP4 inhibitor with IC50 of 26 nM and Ki of 1.3 nM.IC50 value: 26 nM [1]Target: DPP4in vitro: Saxagliptin has an inhibition constant Ki of 1.3 nM for DPP4 inhibition, which is 10-fold more potent than either vildagliptin or sitagliptin (another two DPP4 inhibitors) with Ki of 13 and 18 nM. In addition, Saxagliptin demonstrates greater specificity for DPP4 than for either the DPP8 or DPP9 enzymes (400- and 75- fold, respectively). The active metablite of saxagliptin is two-fold less potent than the parent. Both Saxagliptin and its metabolite are highly selective (>4000-fold) for the prevention of DPP4 compared with a range of other proteases (selectivity of sitagliptin and vildagliptin for DPP4 is >2600 and <250-fold, respectively, compared with DPP8 and DPP9) [2]. Saxagliptin reduces the degradation of the incretin hormone glucagon-like peptide-1, thereby enhancing its actions, and is associated with improved β-cell function and suppression of glucagon secretion.in vivo: Saxagliptin is highly effective at eliciting marked dose-dependent enhancements in glucose clearance in the dose range 0.13-1.3 mg/kg in ob/ob mice relative to controls. Saxagliptin dose-dependently elevate plasma insulin significantly at 15 min post-oGTT, with concomitant improvement in the glucose clearance curves at 60 min post-oGTT [4].
SB-435495 hydrochloride is a potent, selective, reversible, non-covalent and orally active Lp-PLA2 inhibitor with an IC50 of 0.06 nM[1][3].
HFI-419 is an insulin-regulated aminopeptidase (IRAP) inhibitor. HFI-419 has inhibitory potency for IRAP with Ki value of 0.48 μM. HFI-419 can be used for the research of cognitive and memory impairments such as Alzheimer's disease, brain trauma, and stroke[1].
hCAIX-IN-10 (Compound 6i) is a selective carbonic anhydrase IX and XII inhibitor with Ki s of 61.5 and 586.8 nM for hCA IX and hCA XII, respectively. hCA IX and hCA XII are transmembrane isoforms which have been characterized as biomarkers for several types of tumors. The hCA XII assists in maintenance of acid-base homoeostasis in normal as well as tumor cells[1].
Leupeptin hemisulfate is a reversible, competitive serine/cysteine protease inhibitor.
Sorbinil, is an Aldose reductase inhibitor (ARI).Sorbinil plays therapeutic role in treating diabetes and diabetic complications, decreases AR activity and inhibits polyol pathway, it to be found comparatively safer than other ARIs for human use[1].
H-Ile-Pro-Pro-OH, a milk-derived peptide[1], inhibits angiotensin-converting enzyme (ACE)[1] with an IC50 of 5 μM[2]. Antihypertensive tripeptides[1].
PTP1B-IN-3 is a potent and selective PTP1B inhibitor with IC50s of 120 nM (PTP1B) and 120 nM (TCPTP), respectively.
ZD-0892 is a selective and potent inhibitor of a neutrophil elastase with Kis of 6.7 and 200 nM for human neutrophil elastase and porcine pancreatic elastase, respectively.
CM-10-18 is a potent inhibitor of ER α-glucosidase. CM-10-18 demonstrated superior in vitro antiviral activity against representative viruses from four viral families causing hemorrhagic fever. CM-10-18 efficiently protected the lethality of dengue virus infection of mice.
HB007 is a small ubiquitin-related modifier 1 (SUMO1) degrader. HB007 induces ubiquitination and degradation of SUMO1, resulting in reduced tumor growth in vivo. HB007 can be used for the research of brain, breast, colon, and lung cancers[1][2].
Ecallantide (DX-88) is a specific recombinant plasma kallikrein inhibitor. Ecallantide inhibits the production of bradykinin. Ecallantide can be used to prevent acute attacks of angioedema[1].
L-689502 is a potent inhibitor of HIV-l protease with an IC50 of 1 nM.
Fitusiran (ALN-AT3SC), an small interfering RNA, specifically targets antithrombin (AT) messenger RNA to lower production of AT in the liver. Fitusiran increases thrombin generation and has the potential for the research of the hemophilia[1].
FAAH/cPLA2α-IN-1 is a dual inhibitor of FAAH and cPLA2α with IC50s of 32 and 47 nM, respectively[1].
Anecortave acetate is a potent ocular angiostatic agent. Anecortave acetate inhibits neovascularization which is induced by many different angiogenic factors, and increases plasminogen activator inhibitor-1 (PAI-1) mRNA expression. Anecortave acetate can be used to research ocular neovascular diseases[1][2].
PF-4191834 (PF-04191834) is an orally active, noniron chelating, and non-redox inhibitor of the 5-Lipoxygenase (LOX) (IC50=229 nM), displays ~300-fold selectivity for 5-LOX over 12-LOX and 15-LOX, shows no activity toward the cyclooxygenase enzymes, and is effective in inflammation and pain[1].
Bestatin is a natural, broad-spectrum, and competitive aminopeptidase inhibitor.
MMP3 inhibitor 1 is a potent and highly selective MMP-3 inhibitor with an IC50 of 1 nM[1].
Deoxyarbutin is a new effective lighten ingredient, can effectively inhibit tyrosinase activity and melanin synthesis to get significant and lasting lightening effect.
CCT129957 is an indole derivative and a potent phospholipase C-γ (PLC-γ) inhibitor with an IC50 of ~3 μM and a GC50 of 15 μM. CCT129957 inhibits Ca2+ release in squamous carcinoma cells at ~15 μM[1][2].
Tarenflurbil ((R)-Flurbiprofen) is the R-enantiomer of the racemate NSAID Flurbiprofen, Tarenflurbil ((R)-Flurbiprofen) inhibits the binding of [3H]9-cis-RA to RXRα LBD with IC50 of 75 μM.
ML226 is a potent α/β hydrolase domain-containing protein 11 (ABHD11) inhibitor in vitro and in situ with IC50s of 15 and 0.68 nM, respectively[1].
Microcystin-LR is a potent inhibitor of type 1 and type 2A protein phosphatases (PP1 and PP2A), with IC50s of 1.7 nM and 0.04 nM, respectively. Sequence: Ala-D-Ala-Leu-D-{Bas}-Arg-{Oaa}-D-{Ggu}.
NP-313 is a potent antithrombotic agent that inhibits platelet aggregation and activation. NP-313 has dual inhibition of thromboxane A 2 synthesis and selective inhibition of SOCC-mediated Ca2+ inward flow[1].
Quinidine sulfate dihydrate is a potent and selective inhibitor of cytochrome P450db and inhibits amphetamine metabolism in vivo[1]. Quinidine sulfate dihydrate enhances the cytotoxicity of vincristine (VCR) in tumor cells and especially in VCR-resistant sublines of P388 leukemia (P388/VCR) and human myelogenous leukemia[2].