(1S,2R)-Alicapistat ((1S,2R)-ABT-957) is an orally active selective inhibitor of human calpains 1 and 2 for the potential application of Alzheimer's disease (AD)[1]. (1S,2R)-Alicapistat mitigates the metabolic liability of carbonyl reduction and inhibits calpain 1 with an IC50 value of 395 nM[2].
TMP780 is an inverse agonist of RORγt with an IC50 of 13 nM. RORγt is a tractable drug target for the treatment of cutaneous inflammatory disorders[1].
Dihydrolanosterol-d7 is deuterium labeled Dihydrolanosterol. Dihydrolanosterol is a subtrate of CYP51 and a cholesterol biosynthesis inhibitor[1].
6-Methoxytricin (Compound 6) is an flavonoid isolated from Artemisia iwayomogi. 6-Methoxytricin (Compound 6) is an inhibitor on aldose reductase (AR) and advanced glycation endproduct (AGE) formation activities with IC50 values of 30.29 μM and 134.88 μM, respectively. 6-Methoxytricin (Compound 6) has potential as an anti-diabetic complications agent[1].
PF-06840003 is a highly selective orally bioavailable IDO-1 inhibitor.
hCAII-IN-2 (Compound 11f) is a cytosolic human carbonic anhydrase (hCA) inhibitor with Ki values of 261.4, 3.8, 19.6 and 45.2 nM against hCA I, hCA II, hCA IX and hCA XII, respectively[1].
Viscumneoside III, a dihydroflavone O-glycoside, is a potent tyrosinase inhibitor with an IC50 of 0.5 mM. Viscumneoside III has anti-angina pectoris[1].
Palmitic acid-d4-1 is the deuterium labeled Palmitic acid. Palmitic acid is a long-chain saturated fatty acid commonly found in both animals and plants. PA can induce the expression of glucose-regulated protein 78 (GRP78) and CCAAT/enhancer binding protein homologous protein (CHOP) in in mouse granulosa cells[1][2][3].
TLK117, the active metabolite of TLK199, selective inhibits Glutathione S-transferase P1–1 (GSTP1-1) with a Ki of 0.4 μM for GSTP. TLK117 also competitively inhibits glyoxalase I with a Ki of 0.56 μM.
BC-11 hydrobromide is a selective TMPRSS2 inhibitor (TMPRSS2 is a key host cellular factor for viral entry and SARS-CoV-2 pathogenesis), and a selective urokinase (uPA) inhibitor (IC50=8.2 μM). BC-11 hydrobromide is cytotoxic to triple-negative MDA-MB231 breast cancer cells. BC-11 hydrobromide is used in research on viral infections and cancer[1][2][3].
Aderamastat (FP-025) is an orally active matrix metalloproteinase 12 (MMP-12) inhibitor. Aderamastat can be used for the research of asthma, chronic obstructive pulmonary disease (COPD), and pulmonary fibrosis[1].
Isopedicin potently and concentration-dependently inhibits superoxide anion (O2 U?) production in formyl-L-methionyl-L-leucyl-L-phenylalanine (FMLP)-activated cells. Isopedicin increases cAMP formation and PKA activity in FMLP-activated cells by inhibiting phosphodiesterase (PDE) activity[1].
MY33-3 is a small-molecule inhibitor of RPTPβ/ζ (PTPRZ1) with IC50 of 0.1 uM, significantly increases the phosphorylation of key tyrosine residues of RPTPβ/ζ substrates involved in neuronal survival and differentiation; blocks ethanol conditioned place preference, shows limited effects on ethanol-induced ataxia, and potentiates the sedative effects of ethanol in mice; increases levels of phosphorylated ALK and TrkA in neuroblastoma cells, modulates signaling pathways activated by alcohol.
PF-05180999 is a phosphodiesterase 2A (PDE2A) inhibitor, with an IC50 of 1.6 nM.
BCI-215 (BCI215) is a potent, tumor cell-selective dual specificity MAPK phosphatase (DUSP-MKP) inhibitor; restores defective MAPK activity caused by overexpression of DUSP1 and DUSP6 in mammalian cells; inhibits cell motility, causes apoptosis but not primary necrosis, and sensitizes cells to lymphokine-activated killer cell activity in MDA-MB-231 human breast cancer cells; induces rapid and sustained phosphorylation of ERK, p38 and JNK, also hyperactivates MKK4/SEK1; causes selective cancer cell cytotoxicity in part through non-redox-mediated activation of MAPK signaling.
AQX-435 is a potent SHIP1 activator. AQX-435 reduces PI3K activation downstream of the B-cell receptor (BCR) and induces apoptosis of malignant B cells, and reduces lymphoma growth[1].
ENOblock(AP-III-a4) is a novel small molecule which is the first, nonsubstrate analogue that directly binds to enolase and inhibits its activity (IC50=0.576 uM); inhibit cancer cell metastasis in vivo.IC50 value: 0.576 uM [1]Target: enolaseEnolase is a component of the glycolysis pathway and a “moonlighting” protein, with important roles in diverse cellular processes that are not related to its function in glycolysis. However, small molecule tools to probe enolase function have been restricted to crystallography or enzymology. In this study, we report the discovery of the small molecule “ENOblock”, which is the first, nonsubstrate analogue that directly binds to enolase and inhibits its activity. ENOblock was isolated by small molecule screening in a cancer cell assay to detect cytotoxic agents that function in hypoxic conditions, which has previously been shown to induce drug resistance. Further analysis revealed that ENOblock can inhibit cancer cell metastasis in vivo. Moreover, an unexpected role for enolase in glucose homeostasis was revealed by in vivo analysis. Thus, ENOblock is the first reported enolase inhibitor that is suitable for biological assays. This new chemical tool may also be suitable for further study as a cancer and diabetes drug candidate.A Unique Small Molecule Inhibitor of Enolase Clarifies Its Role in Fundamental Biological ProcessesBy Jung, Da-Woon; Kim, Woong-Hee; Park, Si-Hwan; Lee, Jinho; Kim, Jinmi; Su, Dongdong; Ha, Hyung-Ho; Chang, Young-Tae; Williams, Darren R. From ACS Chemical Biology (2013), 8(6), 1271-1282.
Argatroban is a direct, selective thrombin inhibitor.Target: ThrombinArgatroban may have a complementary effect for preventing thrombus formation without aggravating bleeding tendency because of its monotarget specificity to thrombin. Administration (0.5 to 2 micrograms/kg/min) of argatroban is a safe anticoagulant for left heart bypass in repairs of traumatic aortic rupture associated with multiple organ injuries [1]. Argatroban, as compared with heparin, appears to enhance reperfusion with TPA in patients with AMI, particularly in those patients with delayed presentation. The incidences of major bleeding and adverse clinical outcome were lower in the patients receiving argatroban [2].
Odanacatib (MK-0822) is a potent and selective inhibitor of cathepsin K, with an IC50 of 0.2 nM for human cathepsin K.
TMP778 is a potent and selevtive RORγt inverse agonist, with an IC50 of 7 nM in FRET assay.
Imidapril (TA-6366 free base) is an orally active angiotensin-converting enzyme (ACE) and MMP-9 inhibitor. Imidapril suppresses the conversion of angiotensin I to angiotensin II and thereby reduces total peripheral resistance and systemic blood pressure. Imidapril can be used for hypertension, type 1 diabetic, nephropathy and chronic heart failure research[1][2].
GSK 650394 is a novel SGK inhibitor with IC50 of 62 nM and 103 nM for SGK1 and SGK2 in the SPA assay respectively.
KPT-9274 is an orally bioavailable, dual PAK4/Nicotinamide phosphoribosyltransferase (Nampt) inhibitor, with IC50s less than 100 and 120 nM, respectively.
MMP13-IN-4 (compound 13) is a potent and selective inhibitor of MMP-13 (IC50=14.6 μM)，involved in osteoarthritis (OA)[1].
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].
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].
RHC 80267 (U-57908) is a potent and selective inhibitor of diacylglycerol lipase (DAGL) (with IC50 of 4 μM in canine platelets). RHC-80267 inhibits cholinesterase activity with an IC50 of 4 μM, thereby enhancing the relaxation evoked by acetylcholine. RHC 80267 also inhibits COX and the hydrolysis of phosphatidylcholine (PC)[1][2][3][4].
5-Feruloylquinic acid (5-FQA) possesses antioxidative effects and tyrosinase inhibitory activities[1].
Lactacystin, an antibiotic Streptomyces spp. metabolite, is a potent and selective proteasome inhibitor with an IC50 of 4.8 μM for 20S proteasome. Lactacystin also inhibits the lysosomal enzyme cathepsin A[1]. Lactacystin inhibits cell growth and induces neurite outgrowth[2].
Hesperetin 7-O-glucoside is produced by the enzymatic conversion of Hesperidin. Hesperetin 7-O-glucoside is a potent human HMG-CoA reductase inhibitor and also effectively inhibits the growth of Helicobacter pylori. Antihypertensive effect[1][2].