CA-5f is a potent late-stage macroautophagy/autophagy inhibitor via inhibiting autophagosome-lysosome fusion. CA-5f increases LC3B-II (a marker to monitor autophagy) and SQSTM1 protein both in A549 cells and HUVECs. Anti-tumor activity[1].
Bromocriptine mesylate is a potent dopamine D2/D3 receptor agonist, which binds D2 dopamine receptor with pKi of 8.05±0.2.
HDAC-IN-36 (compound 23 g) is an orally active and potent HDAC (histone deacetylase) inhibitor, with an IC50 of 11.68 nM (HDAC6). HDAC-IN-36 promotes apoptosis, autophagy and suppresses migration. HDAC-IN-36 shows anti-tumor and anti-metastatic activity, and can be used for breast cancer research[1].
Nordihydroguaiaretic acid is a 5-lipoxygenase (5LOX) (IC50=8±3 μM) and tyrosine kinase inhibitor.
Aloperine is an alkaloid in sophora plants such as Sophora alopecuroides L, which has shown anti-cancer, anti-inflammatory and anti-virus properties[1]. Aloperine is widely used to treat patients with allergic contact dermatitis eczema and other skin inflammation in China[2]. Aloperine induces apoptosis and autophagy in HL-60 cells[1].
Hesperadin is an ATP-competitive inhibitor of aurora B kinase with an IC50 of 250 nM.
Trimetazidine is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine is an effective antianginal agent and a cytoprotective drug, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine triggers autophagy. Trimetazidine is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor[1][2][3][4].
Kaempferide is an O-methylated flavonol, a type of chemical compound. It can be found in Kaempferia galanga (aromatic ginger). The enzyme kaempferol 4'-O-methyltransferase uses S-adenosyl-L-methionine and kaempferol to produce S-adenosyl-L-homocysteine and kaempferide. P-glycoproteins.
Pogostone is isolated from patchouli with anti-bacterial and anti-cancer activities. Pogostone inhibits both gram negative and gram positive bacteria, also show inhibitory effect on corynebacterium xerosis with a MIC value of 0.098 µg/ml [2]. Pogostone induces cell apoptosis and autophagy[2].
Veliparib (dihydrochloride) is a potent inhibitor of PARP1 and PARP2 with Kis of 5.2 nM and 2.9 nM in cell-free assays, respectively.
UNC0638 selectively inhibits G9a and GLP histone methyltransferase activity with IC50s of less than 15 nM and 19 nM, respectively.
SP600125 is a reversible and ATP-competitive JNK inhibitor with IC50s of 40, 40 and 90 nM for JNK1, JNK2 and JNK3, respectively.
Nitroxoline is an antibiotic that has proven to be very effective at combating biofilm infections. Nitroxoline functions by chelating Fe2+ and Zn2+ ions from the biofilm matrix.
Esmolol Hydrochloride is a beta adrenergic receptor blocker.Target: Adrenergic receptorEsmolol Hydrochloride is the hydrochloride salt form of Esmolol, a short and rapid-acting beta adrenergic antagonist belonging to the class II anti-arrhythmic drugs and devoid of intrinsic sympathomimetic activity. Esmolol hydrochloride competitively blocks beta-1 adrenergic receptors in cardiac muscle and reduces the contractility and cardiac rate of heart muscle, thereby decreasing cardiac output and myocardial oxygen demands. This agent also decreases sympathetic output centrally and blocks renin secretion. At higher doses, Esmolol hydrochloride also blocks beta-2 receptors located in bronchial and vascular smooth muscle, thereby leading to smooth muscle relaxation.
Lapatinib-d4-1 is deuterium labeled Lapatinib. Lapatinib (GW572016) is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively[1].
Tolbutamide is a first generation potassium channel blocker, sulfonylurea oral hypoglycemic drug.Target: Potassium ChannelTolbutamide is an oral antihyperglycemic agent used for the treatment of non-insulin-dependent diabetes mellitus (NIDDM). Tolbutamide act by stimulating β cells of the pancreas to release insulin. Sulfonylureas increase both basal insulin secretion and meal-stimulated insulin release. Tolbutamide belongs to a class of medications called sulfonylureas. Tolbutamide inhibits both the basal and the cyclic AMP-stimulated protein kinase activities and the IC50 of Tolbutamide is 4 mM. Similar Tolbutamide concentrations are required for half maximal inhibition of in vitro lipolysis induced by hormones (norepinephrine and ACTH) or by dibutyryl cyclic AMP plus theophylline. Tolbutamide also inhibits both soluble and membrane-bound protein kinase from canine heart. The Tolbutamide inhibition of adipose tissue cyclic AMP-dependent protein kinase is one possible explanation for the antilipolytic effects of this drug [1]. Tolbutamide inhibits C6-glioma cell proliferation by increasing Cx43, which correlates with a reduction in pRb phosphorylation due to the up-regulation of the Cdk inhibitors p21 and p27 [2].
Indomethacin sodium hydrate (Indometacin sodium hydrate) is a potent, blood-brain permeable and nonselective inhibitor of COX1 and COX2, with IC50s of 18 nM and 26 nM for human COX-1 and COX-2, respectively, in CHO cells[1]. Indomethacin sodium hydrate disrupts autophagic flux by disturbing the normal functioning of lysosomes[2].
Resveratrol analog 1 is an analog of Resveratrol (HY-16561), compound 48. Resveratrol is a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties.
Sitagliptin phosphate is a potent inhibitor of DPP4 with IC50 of 19 nM in Caco-2 cell extracts
Peiminine(Verticinone; Raddeanine) is a natural compound with anti-inflammatory activity.IC50 value:Target:Peiminine and DXS significantly reduced alveolar inflammation and pulmonary interstitial inflammation in rats with bleomycin-induced lung injury. peiminine inhibits lung inflammation and pulmonary fibrosis in a rat model of bleomycin-induced lung injury, by reducing circulating IFN-γ levels and inhibiting signal transduction pathways involving TGF-β, CTGF, ERK1/2, NF-κB and FasL.
Tigecycline hydrate is a broad spectrum glycylcycline antibiotic. Tigecycline hydrate is bacteriostatic, that inhibits protein synthesis by binding to the 30S ribosomal subunit of bacteria and thereby blocking entry of Aminoacyl-tRNA into the A site of the ribosome during prokaryotic translation. Tigecycline hydrate is active against resistant strains of Gram-positive and Gram-negative bacteria.
Ulipristal acetate-d6 is deuterium labeled Ulipristal acetate. Ulipristal acetate (CDB-2914) is an orally active, selective progesterone receptor modulator (SPRM). Ulipristal acetate stimulates the autophagic response selectively in leiomyoma cells. Ulipristal acetate has the potential for benign gynecological conditions treatment, such as uterine myoma[1][2].
Theophylline is a nonselective phosphodiesterase (PDE) inhibitor, adenosine receptor blocker, and histone deacetylase (HDAC) activator.
5-Aminolevulinic acid-d2 (hydrochloride) is deuterium labeled 5-Aminolevulinic acid (hydrochloride).
Honokiol is a bioactive, biphenolic phytochemical that possesses potent antioxidative, anti-inflammatory, antiangiogenic, and anticancer activities by targeting a variety of signaling molecules. It inhibits the activation of Akt and enhances the phosphorylation of ERK1/ERK2.
Sunitinib-d4 (SU 11248-d4) is the deuterium labeled Sunitinib. Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively[1]. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation[2].
Acetyl-coenzyme A (Acetyl-CoA) lithium is a membrane-impermeant central metabolic intermediate, participates in the TCA cycle and oxidative phosphorylation metabolism. Acetyl-coenzyme A lithium, regulates various cellular mechanisms by providing (sole donor) acetyl groups to target amino acid residues for post-translational acetylation reactions of proteins. Acetyl Coenzyme A lithium is also a key precursor of lipid synthesis[1][2][3][4].
Pregnenolone monosulfate-d4 (sodium) is the deuterium labeled Pregnenolone monosulfate. Pregnenolone monosulfate sodium (3β-Hydroxy-5-pregnen-20-one monosulfate sodium) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone monosulfate sodium acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone monosulfate sodium can protect the brain from cannabis intoxication[1][2]. Pregnenolone monosulfate sodium is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels[3].
Apogossypolone (ApoG2) is an orally active Bcl-2 family proteins inhibitor with Ki values of 35, 25 and 660 nM for Bcl-2, Mcl-1 and Bcl-XL, respectively. Apogossypolone shows antitumor activities, induces cell apoptosis[1] and autophagy[2]. Apogossypolone also has antifungal activity[3].
(3R,5R)-Rosuvastatin is the (3R,5R)-enantiomer of Rosuvastatin. Rosuvastatin is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM[1]. Rosuvastatin potently blocks human ether-a-go-go related gene (hERG) current with an IC50 of 195 nM[2]. Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin is very effective in lowering low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels[3].