LEI-401 is a first-in-class, selective, and CNS-active NAPE-PLD (N-acylphosphatidylethanolamine phospholipase D) inhibitor, with an IC50 of 27 nM. LEI-401 modulates emotional behavior in mice[1].
Abiraterone N-oxide is a metabolite of Abiraterone (HY-148377). Abiraterone is a potent and irreversible CYP17A1 inhibitor with antiandrogen activity[1].
CKI-7 is a potent and ATP-competitive casein kinase 1 (CK1) inhibitor with an IC50 of 6 μM and a Ki of 8.5 μM. CKI-7 is a selective Cdc7 kinase inhibitor. CKI-7 also inhibits SGK, ribosomal S6 kinase-1 (S6K1) and mitogen- and stress-activated protein kinase-1 (MSK1). CKI-7 has a much weaker effect on casein kinase II and other protein kinases[1][2][3][4].
Dagrocorat (PF-00251802) hydrochloride is an orally active and selective high-affinity partial agonist of the glucocorticoid receptor. Dagrocorat hydrochloride is also a time-dependent reversible inhibitor of CYP3A (IC50=1.3 μM in human liver microsomes) and CYP2D6 (Ki=0.57 μM in human liver microsomes). Dagrocorat hydrochloride can be used for the research of rheumatoid arthritis[1].
Carbonic anhydrase inhibitor 13 (compound 7) is a potent carbonic anhydrase (CA) inhibitor, which features 3-methylthiazolo[3,2-a]benzimidazole moiety (as a tail) connected to the zinc anchoring benzenesulfonamide moiety via ureido linker[1].
Amprenavir (Agenerase) is a HIV protease inhibitor(Ki=0.6 nM) used to treat HIV infection.IC50 Value: 0.6 nM (Ki); Against wild-type clinical HIV isolates:14.6 +/- 12.5 ng/mL (mean +/- SD) [1].Target: HIV proteasein vitro: Amprenavir has an enzyme inhibition constant (Ki = 0.6 nM) that falls within the Ki range of the other protease inhibitors. Amprenavir's in vitro 50% inhibitory concentration (IC50) against wild-type clinical HIV isolates is 14.6 +/- 12.5 ng/mL (mean +/- SD) [1]. Amprenavir had direct inhibitory effects on invasion of Huh-7 hepatocarcinoma cell lines, inhibiting MMP proteolytic activation [2].in vivo: Amprenavir was able to promote regression of hepatocarcinoma growth in vivo by anti-angiogenetic and overall anti-tumor activities, independently by PI3K/AKT related pathways that at today is one of the more suggestive hypothesis to explain the anti-tumor effects of the different protease inhibitors [2]. Amprenavir efficiently activated PXR and induced PXR target gene expression in vitro and in vivo. Short-term exposure to amprenavirsignificantly increased plasma total cholesterol and atherogenic low-density lipoprotein cholesterol levels in wild-type mice, but not in PXR-deficient mice [3]. Amprenavir has been approved for adults and children; the recommended capsule doses are 1200 mg twice daily for adults and 20 mg/kg twice daily or 15 mg/kg 3 times daily for children < 13 years of age or adolescents < 50 kg [1].Clinical trial: A Study to Compare Three Doses of T-20 When Given in Combination With Abacavir, Amprenavir, Ritonavir, and Efavirenz to HIV-Infected Adults. Phase 2
FG-2216 is a potent HIF-prolyl hydroxylase inhibitor with IC50 of 3.9 uM for PDH2 enzyme; orally bioavailable and induced significant and reversible Epo induction in vivo.IC50 value: 3.9 uM [1]Target: PDH inhibitorFG-2216 was orally bioavailable and induced significant and reversible Epo induction in vivo (82- to 309-fold at 60 mg/kg). Chronic oral dosing in male rhesus macaques was well tolerated, significantly increased erythropoiesis, and prevented anemia induced by weekly phlebotomy. Furthermore, modest increases in HbF-containing red cells and reticulocytes were demonstrated by flow cytometry, though significant increases in HbF were not demonstrated by high-pressure liquid chromatography (HPLC) [2].
Cecropin B has high level of antimicrobial activity and is considered as a valuable peptide antibiotic. Sequence: Lys-Trp-Lys-Val-Phe-Lys-Lys-Ile-Glu-Lys-Met-Gly-Arg-Asn-Ile-Arg-Asn-Gly-Ile-Val-Lys-Ala-Gly-Pro-Ala-Ile-Ala-Val-Leu-Gly-Glu-Ala-Lys-Ala-Leu-NH2.
DT-061 is an orally bioavailable activator of protein phosphatase 2A (PP2A) and could be applied in the therapy of KRAS-mutant and MYC-driven tumorigenesis[1].
MY10 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.
Palmitic acid-d2-1 is the deuterium labeled Palmitic acid. Palmitic acid is a long-chain saturated fatty acid commonly found in both animals and plants. Palmitic acid 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].
AZD-7295 is a HCV NS5A protein inhibitor, with an EC50 of 7 nM for GT-1b replicon[1][2].
NAcM-OPT is an orally bioavailable cullin neddylation 1 (DCN1) inhibitor, which potently inhibits the DCN1-UBE2M interaction[1].
BMS-764459 is a CRF1 antagonist. BMS-764459 can be used for the research of neurological disorders such as depression and anxiety. BMS-764459 is also an atypical CYP1A1 inducer[1][2].
PDE5-IN-2 is a potent, highly selective, and orally active PDE5 inhibitor, with an IC50 of 0.31 nM, less potently inhibits PDE2A, PDE10A, PDE4D2, and PDE6C, with IC50s of 106, 46, 43, 1.2 nM, respectively. Anti-pulmonary arterial hypertension activity[1].
TP0463518 is a potent hypoxia-inducible factor prolyl hydroxylases (PHDs) inhibitor with a Ki value of 5.3 nM for human PHD2. TP0463518 also inhibits human PHD1/PHD3 with IC50s of 18 and 63 nM as well as monkey PHD2 with an IC50 value of 22 nM[1].
Mca-Arg-Pro-Lys-Pro-Tyr-Ala-Nva-Trp-Met-Lys(Dnp)-NH2 is a biological active peptide. (MMP substrate)
Carfilzomib-d8 is deuterium labeled Carfilzomib. Carfilzomib (PR-171) is an irreversible proteasome inhibitor with an IC50 of 5 nM in ANBL-6 and RPMI 8226 cells.
Apixaban is a highly selective, reversible inhibitor of Factor Xa with Ki of 0.08 nM and 0.17 nM in human and rabbit, respectively.
Onalespib (AT13387) is a potent inhibitor of Hsp90, with a Kd of 0.71 nM.
FABP-IN-2 is a novel FABP3 ligand. FABP-IN-2 inhibits FABP3/FABP4 with an IC50 of 1.16 μM and 4.27 μM respectively[1].
IOX2 sodium is a specific prolyl hydroxylase-2 (PHD2) inhibitor with IC50 of 22 nM. IOX2 sodium regulates platelet function and arterial thrombosis by upregulating HIF-1α expression and inhibiting ROS production. IOX2 sodium can be used in the study of thrombotic diseases[1][2].
IDH1 Inhibitor 7 (Compound 88) is an IDH1 inhibitor with an IC50 of less than 100 nM[1].
Dnp-PLAYWAR is a fluorogenic substrate for matrix metalloproteinase-8 (MMP-8) and MMP-26.The activity of MMP-8 and MMP-26 can be quantified by measuring tryptophan fluorescence that is unquenched upon peptide hydrolysis that removes the N-terminal dinitro
Dim16 is a dual PCSK9/HMG-CoAR inhibitor, with an IC50 value of 19 nM for PCSK9. Dim16 inhibits PCSK9-LDLR binding with an IC50 value of 0.8 nM. Dim16 increases LDL uptake in HepG2 cells[1].
Tetrahydrocurcumin D6 (HZIV 81-2 D6) is a deuterium labeled Tetrahydrocurcumin. Tetrahydrocurcumin is a Curcuminoid which displays inhibitory activity for CYP2C9 and CYP3A4[1].
WH-15 is a fluorogenic PLC reporter with Km value of 49; 30, 86.1 µM for PLC-γ1, PLC-δ1, PLC-β2, respectively. WH-15 can be cleaved in a cascade reaction to generate fluorescent 6-aminoquinoline. WH-15 can be used to respond to imaging PLC activity in live cells[1].
Isocitrate dehydrogenase (ICDH) is a citric acid or tricarboxylic acid cycle enzyme, is often used in biochemical studies. Isocitrate dehydrogenase catalyzes the oxidative decarboxylation of isocitrate to α-ketoglutarate and reduces NAD(P)+ to NAD(P)H, it plays important roles in cellular metabolism[1].
Hydrocotarnine is a Cbl inhibitor, and results in inflammasome-mediated IL-18 secretion in colitis. Hydrocotarnine increases expression of GLUT1 and cellular glucose uptake in glycolytic metabolism. Hydrocotarnine acts as an agent that provides analgesic effect in cancer research[1][2][3].
Tipranavir inhibits the enzymatic activity and dimerization of HIV-1 protease, exerts potent activity against multi-protease inhibitor (PI)-resistant HIV-1 isolates with IC50s of 66-410 nM.