ML349 is a potent and specific acyl protein thioesterase 2 (APT-2) inhibitor with a Ki of 120 nM. ML349 is also an inhibitor of LYPLA2 with an IC50 of 144 nM.
CC0651 is an allosteric inhibitor of the human Cdc34 ubiquitin-conjugating enzyme. CC0651 potently (IC50=1.72 μM) inhibits the ubiquitination of p27Kip1, as confirmed by dose-response analysis.
TC-F2 is a reversible non-covalent binding inhibitor of fatty acid amide hydrolase (FAAH) with an IC50 of 28 nM. FAAH is involved in many human diseases, particularly cancer, pain and inflammation as well as neurological, metabolic and cardiovascular disorders[1].
Win 58237 is a cyclic nucleotide phosphodiesterase (PDE) inhibitor, with Ki of 170 nM for PDE V, possessing vasorelaxant activity.
RO5461111 a highly specific and orally active antagonist of Cathepsin S with IC50s of 0.4 nM (human Cathepsin S) and 0.5 nM (murine Cathepsin S), respectively. RO5461111 can effectively inhibit the activation of antigen-specific T cells and B cells. RO5461111 can improve pulmonary inflammation and lupus nephritis[1][2].
MMP13-IN-4 (compound 13) is a potent and selective inhibitor of MMP-13 (IC50=14.6 μM)，involved in osteoarthritis (OA)[1].
SBI-425 is a potent, selective and oral bioavailable tissue-nonspecific alkaline phosphatase (TNAP) inhibitor[1]. Long-term administration of SBI-425 effectively reaches and inhibits TNAP in the vasculature, improving cardiovascular parameters and survival at a dose that does not cause a detectable change in bone[2].
Mirodenafil-d7 (SK-3530-d7) dihydrochloride is the deuterium labeled Mirodenafil dihydrochloride. Mirodenafil dihydrochloride (SK3530 dihydrochloride) is a phosphodiesterase type 5 (PDE-5) inhibitor developed for the treatment of erectile dysfunction[1][2].
hCAIX-IN-7 (compound 6c) is a potent and selective hCAIX inhibitor with KIs of >10000, >10000, 43.0, 410.6 nM for hCAI, hCAII, hCAIV, hCAIX, respectively[1].
Glucocorticoid receptor-IN-1 (Compound WX002) is a selective glucocorticoid receptor (GR) modulator with anti-inflammatory effect. Glucocorticoid receptor-IN-1 exhibits very good transcriptional repressive activity with an IC50 of 2.11 nM against hMMP1, and transcriptional activation activity with an EC50 of 5.59 nM against MMTV[1].
Aurantiamide benzoate is a nature product that could be isolated from two tropical medicinal plants, Cunila spicata and Hyptis fasciculata. Aurantiamide benzoate is a potent xanthine oxidase inhiobitor with an IC50 value of 70 μM[1].
SBI-797812 is structurally similar to active-site directed NAMPT inhibitors and blocks binding of these inhibitors to NAMPT with EC50 of 0.37 μM. SBI-797812 shifts the NAMPT reaction equilibrium towards NMN formation, increases NAMPT affinity for ATP, stabilizes phosphorylated NAMPT at His247, promotes consumption of the pyrophosphate by-product, and blunts feedback inhibition by NAD+. Treatment of cultured cells with SBI-797812 increases intracellular NMN and NAD+. Dosing of mice with SBI-797812 elevates liver NAD+[1].
Boc-Gln-Ala-Arg-AMC hydrochloride is a fluorogenic substrate for trypsin. Boc-Gln-Ala-Arg-AMC hydrochloride can also be used for measuring the proteolytic activity of TMPRSS2[1][2].
Aloe-emodin-8-O-β-D-glucopyranoside, a compound isolated from Saussrurea lappa, is a moderate inhibitor of human protein tyrosine phosphatase 1B (hPTP1B) with an IC50 of 26.6 μM[1].
Atecegatran metoxil is a oral anticoagulant, which inhibits thrombin factor II and is used in thromboembolic disorders. In vivo, Atecegatran metoxil is converted to AR-H067637, a selective and reversible direct thrombin inhibitor.
Mersalyl (Salirgan) is a potent vascular endothelial growth factor (VEGF) and hypoxia-inducible factor 1 (HIF-1) inducer. Mersalyl induces VEGF and ENO1 mRNA expression. Mersalyl shows diuresis effects[1][2][3].
Tropifexor is a novel and highly potent agonist of FXR with an EC50 of 0.2 nM.
PF-8380 is a potent autotaxin inhibitor with an IC50 of 2.8 nM in isolated enzyme assay and 101 nM in human whole blood.
CYP1B1-IN-1 (Compound 9e) is a selective cytochrome P450 1B1 (CYP1B1) inhibitor with an IC50 of 0.49 nM[1].
Paeoniflorin is a herbal constituent extracted from the root of Paeonia albiflora Pall.Target: OthersPaeoniflorin (PF) is the principal bioactive component of Radix Paeo- niae alba, which is widely used in Traditional Chinese Medicine for the treatment of neurodegenerative disorders such as Parkinson's disease(PD) [1]. Paeoniflorin, a compound found in white peony that inhibited the production of testosterone and promoted the activity of aromatase, which converts testosterone into estrogen [2]. Treatment of cells with paeoniflorin but not glycyrrhizin resulted in enhanced phosphorylation and acquisition of the deoxyribonucleic acid-binding ability of heat shock transcription factor 1 (HSF1), as well as the formation of characteristic HSF1 granules in the nucleus, suggesting that the induction of HSPs by paeoniflorin is mediated by the activation of HSF1. Also, thermotolerance was induced by treatment with paeoniflorin but not glycyrrhizin. Paeoniflorin had no toxic effect at concentrations as high as 80 microg/ mL (166.4 microM). To our knowledge, this is the first report on the induction of HSPs by herbal medicines [3].
Razaxaban hydrochloride (BMS 561389 hydrochloride) is a highly potent, selective and orally active factor Xa inhibitor with a Ki of 0.19 nM. Razaxaban hydrochloride exhibits excellent selectivity (>5000-fold) for factor Xa over other related serine proteases. Razaxaban hydrochloride is also a potent thrombin inhibitor with a Ki of 540 nM. Razaxaban hydrochloride has strongly antithrombotic activity[1].
Retagliptin Phosphate is pharmaceutical composition of DPP-4 inhibitor for treating type-2 diabetes.
Nampt-IN-7 (compound GF8) is a potent NAMPT inhibitor, with an IC50 of 7.31 μM. Nampt-IN-7 also displays cytotoxic activity against human HepG2 hepatocellular carcinoma cell line with an IC50 of 24.28 μM[1].
Mulberroside F is one of the main bioactive constituents in mulberry (Morus alba L.)[1]. Mulberroside F shows inhibitory effects on tyrosinase activity and on the melanin formation. Mulberroside F also exhibits superoxide scavenging activity that is involved in the protection against auto-oxidation[2].
HCV-IN-4 is a potent and orally active HCV NS5A inhibitor, shows great potency against GT1a, GT2b, GT3a, GT1a Y93H and GT1a L31V, with EC90s of 3 pM, 0.3 nM, 0.01 nM, 0.5 nM and 0.02 nM, respectively[1].
Choline Fenofibrate (ABT-335) is the choline salt of fenofibric acid under clinical development as a combination therapy with rosuvastatin for the management of dyslipidemia. IC50 value:Target:Several clinical trials have been developed with Choline Fenofibrate on Reverse Cholesterol Transport, Macular Edema and Hypertriglyceridemia.
Z-LLNle-CHO (Z-Leu-Leu-Nle-CHO) is a γ-secretase inhibitor I. Z-LLNle-CHO induces caspase and ROS-dependent apoptosis by blocking the Akt-mediated pro-survival pathway. Z-LLNle-CHO can be used in cancer research, such as breast cancer and leukaemia[1][2].
2,3-Dihydroisoginkgetin, a biflavonoid, is a inhibitor of Tyrosinase, with 36.84% inhibition at 0.1 mM. 2,3-Dihydroisoginkgetin shows less toxicity in HEMn (human epidermal melanocytes) cells, with an IC50 of 86.16 μM[1].
Vonafexor (EYP001) is a selective FXR agonist with anti-HBV effects[1][2].
Proteasome inhibitor IX (PS-IX; AM114) is a Chalcone derivative and a chymotrypsin-like activity of the 20S proteasome inhibitor with an IC50 value of ~1 μM. Proteasome inhibitor IX exhibits HCT116 p53+/+ cells growth inhibitory activity with an IC50 value of 1.49 μM. Proteasome inhibitor IX has potent anticancer activity[1][2].