UK-371804 is a urokinase-type plasminogen activator (uPA) inhibitor with a Ki of 10 nM.
Z-Phe-Tyr(tBu)-diazomethylketone is a potent cathepsin L inhibitor. Z-Phe-Tyr(tBu)-diazomethylketone mediates reovirus disassembly. Z-Phe-Tyr(tBu)-diazomethylketone decreases viral detection[1][2].
EA4, a derivative of quinone, is an inhibitor for both rPLA and cPLA. EA4 can inhibit rPLA2 with a Ki value of 130 μM. EA4 can be used for the research of hemostasis, thrombosis, and erythropoiesis[1].
Azaleatin is an O-methylated flavonol isolated from Rhododendron species. Azaleatin is a dipeptidyl peptidase-IV inhibitor. Azaleatin can be used for the research of type-2 diabetes and obesity[1][2].
Doxycycline (hyclate) is a tetracycline antibiotic and broad-spectrum metalloproteinase (MMP) inhibitor.
Andolast is an anti-allergic agent for the treatment of bronchial asthma, chronic obstructive pulmonary disease (COPD). Andolast inhibits dose dependently guinea-pig lung cAMP-phosphodiesterase with an IC50 of 50 mM.
UK-101 is a potent and selective immunoproteasome β1i (LMP2) inhibitor with an IC50 value of 104 nM, displays 144- and 10-fold selectivity over β1c (IC50=15 μM) and β5 subunit (IC50=1 μM), respectivey[1]. UK-101 induces cell apoptosis and can be used for the study of prostate cancer[2].
D-3 is a selective PSC eliminating agent, inducing toxicity in cultured iPSCs and ESCs after 1 h of incubation, via an alkaline phosphatase-dependent mechanism.
LMP7-IN-1, a Boronic acid derivative, is a potent and selective immunoproteasome subunit LMP7 (β5i) inhibitor with an IC50 of 1.83 nM (WO2021143923A1; compound 20)[1].
L 691816 is a potent, selective and orally active inhibitors of 5-lipoxygenase. L 691816 can be used for the research of allergies and asthma[1].
PTP1B-IN-14 is a selective PTP1B inhibitor (IC50 = 0.72 μM) targeting the allosteric site.
Braylin, a coumarin, is a potent phosphodiesterase-4 (PDE4) inhibitor and is involved in anti-inflammatory and immunomodulation, which may serve as a potential target for the study of immunoinflammatory diseases[1].
Relacatib (SB-462795) is a novel, potent, and orally active inhibitor of human cathepsins K, L, and V with Ki values of 41 pM, 68 pM, and 53 pM, respectively. Relacatib inhibits endogenous cathepsin K in situ in human osteoclasts and human osteoclast-mediated bone resorption with IC50 values of 45 nM and 70 nM, respectively. Relacatib inhibits bone resorption in vitro in human tissue as well as in cynomolgus monkeys in vivo[1][2].
CMI-392 is a dual 5-lipoxygenese inhibitor and platelet-activating factor (PAF) receptor antagonist with IC50s of 100 and 10 nM, respectively.
NCT-58 is a potent inhibitor of C-terminal HSP90. NCT-58 does not induce the heat shock response (HSR) due to its targeting of the C-terminal region and elicits anti-tumor activity via the simultaneous downregulation of HER family members as well as inhibition of Akt phosphorylation. NCT-58 kills Trastuzumab-resistant breast cancer stem-like cells. NCT-58 induces apoptosis in HER2-positive breast cancer cells[1].
DD1, a proteasome inhibitor, targets Bax activation and P70S6K degradation during acute myeloid leukemia (AML) apoptosis. DD1 induces apoptosis in the caspase-dependent manner. DD1 induces mitochondrial membrane depolarization and Bad dephosphorylation[1].
MAGLi 432 is a non-covalent, potent, highly selective, and reversible MAGL inhibitor. MAGLi 432 binds with high affinity to the MAGL active site, with IC50 values of 4.2 nM (human enzyme) and 3.1 nM (mouse enzyme). MAGLi 432 can be used in the research of chronic inflammation, blood–brain barrier dysfunction, neurological disorders such as multiple sclerosis, Alzheimer’s disease and Parkinson’s disease[1].
Acetyl tetrapeptide-5 inhibits glycosylation and ACE-1 activity. Acetyl tetrapeptide-5 reduces edema and relieves vascular pressure by improving the vascular system and strengthening the skin under the eyes. Acetyl tetrapeptide-5 can be used in the research of Antioxidant, anti-aging skin care[1][2][3].
ATX inhibitor 5 is a potent and orally active autotaxin (ATX) inhibitor, with an IC50 of 15.3 nM. ATX inhibitor 5 has anti-hepatofibrosis effect, and reduces CCl4-induced hepatic fibrosis level prominently[1].
SMAP-2 (DT-1154) is an orally bioavailable phosphatase 2A (PP2A) activator which binds to the PP2A Aα scaffold subunit to drive conformational changes in PP2A. SMAP-2 (DT-1154) inhibits the growth of KRAS-mutant lung cancers [1].
GW 4064 is a potent FXR agonist with EC50 of 65 nM.
PC945 is a novel broad spectrum antifungal agent that potently inhibits Aspergillus fumigatus sterol 14α-demethylase (CYP51A and CYP51B) with IC50 of 0.23 and 0.22 uM, respectively; shows MIC values 0.032 to >8 ug/ml against 96 clinically isolated A. fumigatus strains, demonstrates activity against itraconazole-susceptible and -resistant A. fumigatus growth with IC50 of 0.0012 to 0.034 ug/ml; PC945 is a broad spectrum of pathogenic fungi with MIC 0.0078 to 2 ug/ml, and exhibits activity in vivo. Fungal Infection Phase 1 Clinical
CAY10502 is a potent, calcium-dependent cytosolic phospholipase A2 α (cPLA2α) inhibitor with an IC50 of 4.3 nM for isolated enzyme. CAY10502 can be used in the research of retinopathy and inflammatory diseases[1][2][3].
XY018 is a potent ROR-γ-selective antagonist. XY018 inhibits ROR-γ constitutive activity in 293T cells with high potency (EC50, 190 nM). XY018 binds to the ROR-γ hydrophobic ligand binding domain (LBD)[1].
CP-609754 (LNK-754) is a potent and reversible farnesyltransferase inhibitor with potential anticancer activity.The IC50 for inhibiting farnesylation of recombinant human H-Ras is 0.57 ng/mL and recombinant K-Ras is 46 ng/mL[1].
Pepstatin (Pepstatin A) acetate is a specific, orally active aspartic protease inhibitor produced by actinomycetes, with IC50s of 4.5 nM, 6.2 nM, 150 nM, 290 nM, 520 nM and 260 nM for hemoglobin-pepsin, hemoglobin-proctase, casein-pepsin, casein-proctase, casein-acid protease and hemoglobin-acid protease, respectively. Pepstatin acetate also inhibits HIV protease[1][2].
Aliskiren fumarate is an orally active, highly potent and selective renin inhibitor, with IC50 of 1.5 nM. Aliskiren fumarate can be used for the research of hypertension, cardiovascular diseases and cancer cachexia[1][2][3].
Cathepsin inhibitor 1 (compound 25) is a potent and selective inhibitor of Cathepsin, with pIC50s of 7.9, 6.7, 6.0, 5.5 and 5.2 for CatL, CatL2, CatS, CatK, and CatB, respectively[1].
NVP-DPP728 dihydrochloride is a potent, selective and orally active dipeptidyl peptidase IV (DPP-IV) inhibitor with a Ki of 11 nM. NVP-DPP728 dihydrochloride can be used for the research of diabetes mellitus[1][2].
Asunaprevir is a potent hepatitis C virus (HCV) NS3 protease inhibitor, with IC50 of 0.2 nM-3.5 nM.