Cbl-b-IN-8 (Compound 293) is a casitas B-lineage lymphoma-b (Cbl-b) and c-Cbl inhibitor with IC50s of 5.5 nM and 7.8 nM, respectively[1].
HIV-1 protease-IN-5 (Compound 13c) is a HIV-1 protease inhibitor with an IC50 of 1.64 nM. HIV-1 protease-IN-5 shows remarkable activity against wild-type and DRV-resistant HIV-1 variants[1].
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.
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].
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].
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].
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].
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].
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].
Vonafexor (EYP001) is a selective FXR agonist with anti-HBV effects[1][2].
Glycolic Acid is an inhibitor of tyrosinase, suppressing melanin formation and lead to a lightening of skin colour.
SZL P1-41 is Skp2 inhibitor, selectively suppresses Skp2 E3 ligase activity, but not activity of other SCF complexes.target: Skp2In vitro: SZL P1-41 also phenocopies the effects observed upon genetic Skp2 deficiency, such as suppressing survival, Akt-mediated glycolysis as well as triggering p53-independent cellular senescence. SZL P1-41 prevent Skp2-Skp1 interactions and Skp2 SCF E3 ligase activity. The reference concentration is 5 uM. SZL P1-41 restricts cancer cell survival through triggering p53-independent cellular senescence and inhibiting aerobic glycolysis.In vivo: SZL P1-41 exhibits potent anti-tumor activities in multiple animal models and cooperates with chemotherapeutic agents to reduce cancer cell survival.
MIV-247 is a selective cathepsin S inhibitor with Kis of 2.1, 4.2 and 7.5 nM for human, mouse and cynomolgus monkey cathepsin S, respectively.
Lepirudin is a potent irreversible thrombin inhibitor. Lepirudin also is a recombinant hirudin. Lepirudin has anticoagulation in heparin-induced thrombocytopenia (HIT)[1].
hCAI/II-IN-6 is a human carbonic anhydrase(CA) inhibitor. hCAI/II-IN-6 selectively inhibits hCA II and hCA VII isoforms with Ki values of 220, 4.9, 6.5 and ＞50000 nM for hCA I, hCA II , hCA VII and hCA XII respectively. hCAI/II-IN-6 shows anticonvulsant activity and anti maximal electroshock (MES) activity in vivo. hCAI/II-IN-6 can be used for the research of epilepsy[1].
PDE4B-IN-2 is an orally active and selective PDE4B inhibitor (IC50=15 nM) and exhibits >100-fold selectivity for PDE4B over 4D. PDE4B-IN-2 regulates cAMP in inflammatory cells and inhibits LPS-induced TNF-α production and neutrophil accumulation in mouse lungs. PDE4B-IN-2 reduces microglial and neutrophil activation, and improves behavioral deficits in a traumatic brain injury model in vivo. PDE4B-IN-2 also exhibits antidepressant-like effects.
LP117 is a novel and potent inhibitor of 5-Lipoxygenase (5-LO) product synthesis with an IC50 of 1.1 μM.
CYP4A11/CYP4F2-IN-2 is a potent and orally active dual inhibitor of cytochrome P450 (CYP) 4A11 and CYP4F2, with IC50s of 140 nM and 40 nM, respectively. CYP4A11/CYP4F2-IN-2 has potential for the research of renal diseases[1].
ATX inhibitor 21 (compound 8) is a potent ATX (autotaxin) inhibitor, with an IC50 of 3490 nM[1].
TAO Kinase inhibitor 2 (Example 49) is a TAO Kinase inhibitor (IC50=between 50 and 500 nM). TAO Kinase inhibitor 2 also inhibits KIAA1361 and JIK with IC50s of 50-500 nM[1].
Cerulenin, the best known natural inhibitor of fatty acid synthase (FAS), is an epoxide produced by the fungus Cephalosporium caeruleus.
RS4317 is a topically effective 5-lipoxygenase (5-LO) inhibitor.
PDE IV-IN-1 is an inhibitor of phosphodiesterase IV, used for the research of asthma, COPD or other inflammatory diseases.
NG-497 is a selective human adipose triglyceride lipase (ATGL) inhibitor that targets the enzymatically active patatin-like domain of human ATGL. NG-497 has potential value for tumor research[1].
NSC232003 is a highly potent and cell-permeable UHRF1 inhibitor, which inhibits DNA methylation in vitro and disrupts DNMT1/UHRF1 interactions at a cellular level.
Proteasome β2c/i-IN-1 (compound 37) is a subunit-selective human proteasome β2c and β2i inhibitor[1].
ML228 analog is an analog of ML228 (HY-12754). ML228 is a potent activator of HIF[1].
Veliflapon (BAY X 1005; DG-031) is an orally active inhibitor of the synthesis of the leukotrienes B4 and C4[1]. Veliflapon is shown to be a selective inhibitor of the formation of 5-lipoxygenase-derived metabolites in vitro, without effects on other routes of arachidonic acid metabolism[2].