(E/Z)-Ensifentrine is a dual inhibitor of PDE3/4. (E/Z)-Ensifentrine reduces the inflammatory cells into the airways. (E/Z)-Ensifentrine has bronchodilatory and anti-inflammatory activities in vitro and in vivo model[1].
HIV Protease Substrate IV is a substrate of HIV protease. HIV Protease Substrate IV can be used to measure the activity of HIV (human immunodeficiency virus) -1 protease[1].
VTP-27999 Hcl is an alkyl amine Renin inhibitor; VTP-27999 is useful for Hypertension and End-Organ Diseases.IC50 value:Target: Renin
JP104, a aryl carbamate, is an irreversible FAAH inhibitor with a pIC50 of ~8[1].
Anagrelide Hydrochloride(BL4162A) is a drug used for the treatment of essential thrombocytosis.Target: PDEAnagrelide hydrochloride is an oral imidazoquinazoline agent that has been shown to reduce elevated platelet counts and the risk of thrombosis in patients with thrombocythaemia in various myeloproliferative disorders (MPD). It is currently approved by the FDA as oral treatment for essential thrombocythaemia (ET) and thrombocythaemia associated with polycythaemia vera (PV). Anagrelide is known to inhibit platelet cyclic adenosine monophosphate (cAMP) phosphodiesterase at concentrations that exceed those achieved at doses used to treat ET. Anagrelide is extensively metabolised in the liver and its metabolites are primarily excreted in the urine [1]. Anagrelide is an established platelet-reducing drug. Studies have also investigated the effects of anagrelide on platelets, indicating that platelet function is as important as platelet counts in ET [2].
L-669,262, a potent inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase, with an IC50 of 0.10 ng/mL for rat liver HMG-CoA[1].
SPL-334 is a potent and selective S-Nitrosoglutathione reductase (GSNOR) inhibitor. SPL-334 causes a significant reduction in the production of Th2 cytokines IL-5 and IL-13 and the levels of the chemokine CCL11 (eotaxin-1) in the airways. SPL-334 can be used in research of allergic airway inflammation[1].
Ilexsaponin B2 is a saponin isolated from the root of Ilex pubescens Hook. et Arn. Ilexsaponin B2 is a potent phosphodiesterase 5 (PDE5) and PDEI inhibitor with IC50 values of 48.8 μM and 477.5 μM, respectively[1].
Enoximone is an inotropic vasodilating agent and a selective and orally active phosphodiesterase III (PDE3) inhibitor with an IC50 of 5.9 μM. Enoximone induces vasodilatation and increases intracellular levels of cAMP by inhibiting cGMP-inhibited PDE. Enoximone also exhibits PDE4 inhibitory effect with an IC50 of 21.1 μM for myocardial PDE4A. Enoximone has the potential for congestive heart failure research and has bronchodilatory, antiasthma and anti-inflammatory effects[1][2][3].
(Rac)-Indoximod (1-Methyl-DL-tryptophan) is an indoleamine 2,3-dioxygenase (IDO) inhibitor. Co-treatment with IFN-γ and (Rac)-Indoximod markedly reduces the activity of human cardiac myofibroblasts (hCMs) expressing α-SMA and induces apoptosis through up-regulating the IRF-1, Fas, and FasL genes[1].
UK 356618 (Compound 4j) is a potent and selective inhibitor of matrix metalloprotease-3 (MMP-3) with an IC50 of 5.9 nM. UK 356618 is >140-fold less potent against MMP-1 (IC50 of 51,000 nM), MMP-2 (IC50 of 1790 nM), MMP-9 (IC50 of 840 nM) and MMP-14 (IC50 of 1900 nM) compared with MMP-3[1].
Adapalene sodium salt(CD 271; Differin), a synthetic retinoid, is a Retinoic acid receptor agonist (RAR).Target: Retinoic acid receptor agonist (RAR)Adapalene sodium salt is a third-generation topical retinoid primarily used in the treatment of mild-moderate acne and is also used (off-label) to treat keratosis pilaris as well as other skin conditions. Adapalene sodium salt is possibly more effective than tretinoin 0.025% gel in the treatment of acne vulgaris [1].Thirty-six rats of either sex were divided into six groups (two control groups, and an etodolac, indomethacin, tretinoin and adapalene sodium salt group) of six animals each. Each group was given different drugs or chemicals. The inhibitory activities of the drugs were determined on carrageenan-induced rat-paw oedema. The inhibition rate (53.48%) in the tretinoin group was found to be higher than adapalene sodium salt and controls (P < 0.05). Adapalene sodium salt was found to have an inhibition rate of 10.28%, and when compared with the other groups, was found to have no statistically significant anti-inflammatory activity [2].Clinical indications: Acne; Purpura; SunburnFDA Approved Date: 1996Toxicity: Skin redness; dryness; itching; scaling; mild burning
CC-885 is a cereblon (CRBN) modulator with potent anti-tumour activity.
Coptisine chloride is an alkaloid from Chinese goldthread, and acts as an efficient uncompetitive IDO inhibitor with a Ki value of 5.8 μM and an IC50 value of 6.3 μM.
17-AAG is a potent HSP90 inhibitor with an IC50 of 5 nM, having a 100-fold higher binding affinity for tumour cell derived HSP90 than normal cell derived HSP90.
Propentofylline is a xanthine-derivative that inhibits adenosine uptake and blocks phosphodiesterase activity. Propentofylline has neuroprotective, antiproliferative, and anti-inflammatory effects that improve cognition and dementia severity in patients with Alzheimer's disease or vascular dementia.
Febuxostat acyl glucuronide (Febuxostat acyl-β-D-glucuronide) is a metabolite of Febuxostat (HY-14268). Febuxostat is a potent, selective and non-purine xanthine oxidase (XO) inhibitor[1].
Bergapten is a natural anti-inflammatory and anti-tumor agent isolated from bergamot essential oil, other citrus essential oils and grapefruit juice. Bergapten is inhibitory towards mouse and human CYP isoforms.
HSP90-IN-14 (compound 4) is a potent Hsp90 (heat shock protein 90) inhibitor, with a Kd of 0.26 μM. HSP90-IN-14 shows anti-influenza virus activity in MDCK cells, with EC50 values of 2.6, 3.9, and 17 μM for influenza A/H3N2, A/H1N1, and B, respectively[1].
hCAII-IN-1 (compound 7f) is a potent and selective inhibitor of carbonic anhydrase (CA II/IX) with Kis of 1.2 and 113.6 nM, respectively. hCAII-IN-1 has the potential for the research of cancer diseases[1].
HIF-2α-IN-9 (compound 35r) is an inhibitor ofHIF-2α. HIF-2α-IN-9 inhibits VEGF-A (IC50=305 nM), and regulates growth-promoting genes in tumor cells, reactivates macrophage-mediated tumor immunity[1].
hCA I-IN-1 (Compound 6q) is a human carbonic anhydrase I (hCA I) inhibitor with Ki values of 38.3, 716.4, 940.1 and 192.8 nM against hCA I, hCA II, hCAIX and hCAXII, respectively[1].
Nelfinavir(AG-1341) is a potent and orally bioavailable human immunodeficiency virus HIV-1 protease inhibitor (Ki=2 nM) and is widely prescribed in combination with HIV reverse transcriptase inhibitors for the treatment of HIV infection. IC50 Valur: 2 nM (Ki for HIV-1 protease) [2]Target: HIV Proteasein vitro: In vitro exposure (72 hours) of HAECs to NEL (0.25-2 μg/mL) decreased both basal (2.5-fold) and insulin-induced NO production (4- to 5-fold). NEL suppressed insulin-induced phosphorylation of both Akt and eNOS at serine residues 473 and 1177, respectively. NEL decreased tyrosine phosphorylation of IR-β, IRS-1, and PI3K. Coexposure to troglitazone (TRO; 250 nM) ameliorated the suppressive effects of NEL on insulin signaling and NO production. Coexposure to TRO also increased eNOS expression in NEL-treated HAECs [1]. AG1343 is a potent enzyme inhibitor (Ki = 2 nM) and antiviral agent (HIV-1 ED50 = 14 nM). An X-ray cocrystal structure of the enzyme-AG1343 complex reveals how the novel thiophenyl ether and phenol-amide substituents of the inhibitor interact with the S1 and S2 subsites of HIV-1 protease, respectively [2].in vivo: In vivo studies indicate that AG1343 is well absorbed orally in a variety of species and possesses favorable pharmacokinetic properties in humans [2].
CAY10590 (GK115) is an inhibitor of secreted phospholipase A2 (sPLA2) and can be used for the research of chronic inflammatory kidney diseases[1].
XS-060 is a potent anticancer agent and RXRα antagonist. XS-060 significantly induces RXRα-dependent mitotic arrest by inhibiting pRXRα-PLK1 interaction[1].
3-Epiursolic Acid is a triterpenoid isolated from Myrtaceae, acts as a competitive inhibitor of cathepsin L (ICIC50, 6.5 μM; Ki, 19.5 μM), with no obvious effect on cathepsin B[1].
Finasteride is an orally active testosterone 5-alpha-reductase inhibitor (Ki= 10 nM). Target: 5-alpha ReductaseApproved: 1992Finasteride, a synthetic 4-azasteroid antiandrogen compound, is a specific inhibitor of steroid Type II 5α-reductase, an intracellular enzyme that converts the androgen testosterone into 5α-dihydrotestosterone (DHT). Finasteride is used in the treatment of prostate cancer, benign prostatic hyperplasia, and androgenetic alopecia (male pattern baldness). In benign prostatic hyperplasia, finasteride inhibits 5alpha-reductase activity in epithelium for Ki of 10 nM, significantly lower than in stroma (Ki = 33nM) [1].
A selective small molecule toward Tec kinase-mediated tyrosine phosphorylation of FGF2 with IC50 of 11.7 uM; inhibits Tec-FGF2 complex and blocks tyrosine phosphorylation of FGF2 in cells, also inhibit FGF2 secretion from cells.
S-2474 is an inhibitor of COX-2 and 5-lipoxygenase, with IC50s of 11 nM and 27 μM for COX-2 and COX-1 in human intact cells, and used as a nonsteroidal anti-inflammatory drug.
Alrestatin sodium is an inhibitor of aldose reductase, an enzyme involved in the pathogenesis of complications of diabetes mellitus, including diabetic neuropathy.