NAcM-OPT is an orally bioavailable cullin neddylation 1 (DCN1) inhibitor, which potently inhibits the DCN1-UBE2M interaction[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].
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.
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
Tetrahydrocurcumin D6 (HZIV 81-2 D6) is a deuterium labeled Tetrahydrocurcumin. Tetrahydrocurcumin is a Curcuminoid which displays inhibitory activity for CYP2C9 and CYP3A4[1].
YM-53601 free base is a squalene synthetase inhibitor which suppresses lipogenic biosynthesis and lipid secretion in rodents.
Dyphylline acts as an adenosine receptor antagonist and phosphodiesterase inhibitor, which is used in the treatment of respiratory disorders.Target: Adenosine Receptor; PDEDyphylline (trade names Dilor, Lufyllin), also known as diprophylline, is a xanthine derivative with bronchodilator and vasodilator effects. It is used in the treatment of respiratory disorders like asthma, cardiac dyspnea, and bronchitis. It acts as an adenosine receptor antagonist and phosphodiesterase inhibitor.
Pectolinarigenin, isolated from Cirsium chanroenicum, is a dual inhibitor of COX-2/5-LOX. Anti-inflammatory activity[1]. Pectolinarigenin has potent inhibitory activities on melanogenesis[2].
PF-06795071 is a potent and selective covalent MAGL inhibitor with an IC50 of 3 nM[1].
Azo-resveratrol, an Azo compound, inhibits Mushroom tyrosinase (IC50=36.28 μM).
Bay 60-7550 is a potent and selective PDE2 inhibitor with a Ki of 3.8 nM.
Dual FAAH/sEH-IN-1 (compound 3) is a high affinity dual sEH (soluble epoxide hydrolase) and FAAH (fatty acid amide hydrolase) inhibitor, with IC50 values of 9.6 and 7 nM, respectively. Dual FAAH/sEH-IN-1 shows antinociception against the inflammatory phase[1].
27-Hydroxycholesterol is a selective estrogen receptor modulator and an agonist of the liver X receptor.
Liarozole dihydrochloride (R75251; R85246) is a cytochrome P450 (CYP450) dependent inhibitor, orally active, it also a potent inhibitor of estrogen (via inhibition of aromatase) and testicular androgen synthesis (inhibition of 17 ,20-lyase). Liarozole dihydrochloride prevents the catabolism of retinoic acid via inhibition of 4-hydroxylase and exhibits retinoid sparing and retinoid-mimetic effects in vivo. Liarozole dihydrochloride is an imidazole derivative; it is being investigated as a non-hormonal agent in prostate cancer and in the treatment of various other cancers and skin disorders[1].
LG100754 (UVI 2112) is a RXR dimers modulater. LG100754 acts as a RXR:RXR homodimer antagonist, but functions as a agonist towards RXR:PPARα and RXR:PPARγ heterodimers. LG100754 is an insulin sensitizer that functions through RXR[1].
A novel small molecule inhibitor of PDE6δ/KRas interaction with Kd of 203 pM; inhibits PDE6δ/KRas interaction in cells with Kd of 85 nM, selectively inhibits growth of KRas mutated and -dependent cells.
MLS000544460 is a highly selective and reversible Eya2 phosphatase inhibitor with a Kd of 2.0 μM and an IC50 of 4 μM. MLS000544460 inhibit Eya2 phosphatase mediated cell migration and has anti-cancer activity[1].
BI-6C9 is a BH3 interacting domain (Bid) inhibitor, which prevents mitochondrial outer membrane potential (MOMP) and mitochondrial fission, and protects the cells from cell death[1].
Raphin1 acetate is an orally bioavailable, selective inhibitor of the regulatory phosphatase PPP1R15B (R15B). Raphin1 acetate binds strongly to the R15B-PP1c holophosphatase (Kd=33 nM), and shows ~30-fold selective in binding R15B-PP1c over R15A-PP1c. Raphin1 acetate crosses the blood-brain barrier, and reduces organismal and molecular deficits in a mouse model of a protein misfolding disease[1].
Quinidine hydrobromide is an antiarrhythmic agent. Quinidine is a potent, orally active, selective cytochrome P450db inhibitor. Quinidine hydrobromide is also a K+ channel blocker with an IC50 of 19.9 μM. Quinidine hydrobromide can be used for malaria research[1][2][3].
Cholesterol 24-hydroxylase-IN-2 is an inhibitor of cholesterol 24-hydroxylase (CH24H or CYP46A1), with the IC50 of 5.4 nM. Cholesterol 24-hydroxylase-IN-2 can be used in imaging of cholesterol 24-hydroxylase in mammals[1].
U66858 is a potent inhibitor of LTB4 production in human whole blood. U66858 also exhibits significant inhibition of lipoxygenase and TXB2 release.
Obtusifoliol is a specific CYP51 inhibitor, Obtusifoliol shows the affinity with Kd values of 1.2 µM and 1.4 µM for Trypanosoma brucei (TB) and human CYP51, respectively[1].
TPN729 is a novel potent, selective phosphodiesterase type 5 (PDE5) inhibitor with IC50 of 2.28 nM, shows better selectivity profile 2.5 times higher than sildenafil against PDE6 and 500 times higher than tadalafil against PDE11; selectively inhibits PDE5 and blocks the degradation of cyclic guanosine monophosphate, and is a promising PDE5 inhibitor providing fewer side effects and better compliance.
Asp-AMS, an analogue of aspartyl-adenylate, is an aspartyl-tRNA synthetase inhibitor and also a strong competitive inhibitor of the mitochondrial enzyme.
Lopinavir Metabolite M-1, an active metabolite of Lopinavir, inhibits HIV protease with a Ki of 0.7 pM. Lopinavir Metabolite M-1 has antiviral activities in vitro[1][2].
DCN1-UBC12-IN-1 is potent and selective DCN1-UBC12 inhibitor with an IC50 of 2.86 nM. Anticardiac fibrotic effect[1].
p-Aminophenylmercuric acetate is an organomercurial activator of matrix metalloproteinases (MMP). P-Aminophenylmercuric acetate participates in the activation and inhibition of MMP-8 by attacking protein sulfhydryl or inducing cysteine switching reaction. p-Aminophenylmercuric acetate promotes the shedding of betacellulin precursor (pro-BTC). p-Aminophenylmercuric acetate influences the binding of agonists and antagonists to the opiate receptor[1][2][3].
Mca-Pro-Leu-Ala-Cys(Mob)-Trp-Ala-Arg-Dap(Dnp)-NH2 is a fluorogenic substrate for matrix metalloproteinase-14 (MMP-14).