Lethedioside A is an Enhancer of split 1 (Hes1) dimer inhibitor with an IC50 value of 9.5 μM[1].
Benzyl-PEG1-propanol is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Vorolanib (CM082; X-82) is an orally active, multikinase VEGFR/PDGFR inhibitor. Vorolanib minimizes toxicity, disrupts tumor angiogenesis and tumor cell proliferation, and induces of tumor cell death[1].
11β-HSD1-IN-1 is an inhibitor of 11β-hydroxydehydrogenase 1 (11β-HSD1), with an IC50 of 52 nM, and used for the treatment of pain.
threo-Guaiacylglycerol beta-coniferyl ether is a lignan that can inhibit NO production. threo-Guaiacylglycerol beta-coniferyl ether exhibits anti-neuroinflammatory activities[1].
Enpp-1-IN-13 (Compound 1a) is an ectonucleotide pyrophosphatase/phosphodiesterase (ENPP) inhibitor with IC50 values of 1.29 μM and 20.2 μM against ENPP1 and ENPP3, respectively. Enpp-1-IN-13 shows anticancer activity[1].
Incensole, a 14-membered diterpenoid, is isolated from both essential oils and resins of frankincense. Incensole has shown anti-inflammatory and anti-depression activities due to their ability to activate ion channels in the brain to alleviate anxiety or depression[1].
Rupestonic acid, a sesquiterpene from Artemisia rupestris L., can inhibit influenza virus[1].
Waltonitone is a ursane-type pentacyclic triterpene isolated from Gentian waltonii Burkill. Waltonitone significantly inhibits hepatocellular carcinoma cells growth and induces apoptosis in vitro and in vivo[1].
VII-31 is a potent NEDDylation pathway activator to inhibit the tumor progression in vitro and in vivo. VII-31 induces apoptosis via intrinsic and extrinsic pathways[1].
Dorsomorphin is a potent and selective AMPK inhibitor, that is competitive with ATP, with Ki=109±16 nM in the absence of AMP.
Glyurallin B is a flavonoid, that can be isolated from licorice (Glycyrrhiza inflata and Glycyrrhiza uralensis). Glyurallin B shows ABTS+ radical scavenging activity and the inhibitory activity on lipid peroxidation, with EC50 values of 11.9 ± 0.58 μM and 15.3 ± 1.26 μM, respectivley[1].
Boc-NH-PEG2-CH2COOH is a PEG-based PROTAC linker can be used in the synthesis of PROTACs[1].
Tranilast is an antiallergic agent.Target: Angiotensin ReceptorTranilast has been approved in Japan and South Korea, since 1982, for the treatment of bronchial asthma, with indications for keloids and hypertrophic scar added in 1993. Tranilast is also used to treat asthma, autoimmune diseases, atopic and fibrotic pathologies, and can also inhibit angiogenesis. The antiproliferative properties of tranilast were found that tranilast elicited an inhibitory effect on fibroblast proliferation in vitro and also suppressed collagen production both in vitro and in vivo . Tranilast also reduced the release of chemical mediators from mast cells and suppressed hypersensitivity reactions. [1]Three-week-old C57Bl/10 and mdx mice received tranilast (~300 mg/kg) in their food for 9 weeks, after which fibrosis was assessed through histological analyses, and functional properties of tibialis anterior muscles were assessed in situ and diaphragm muscle strips in vitro. Tranilast administration did not significantly alter the mass of any muscles in control or mdx mice, but it decreased fibrosis in the severely affected diaphragm muscle by 31% compared with untreated mdx mice (P<0.05) [2].
N-Benzoyl-L-arginine ethyl ester hydrochloride is an arginine derivative[1].
Chol-PEG is a nonionic surfactant vesicles and can be used for a blood-persistent drug delivery system[1][2].
EGFR Protein Tyrosine Kinase Substrate is a EGFR protein tyrosine kinase substrate.
2'-O-Me-C(Bz) Phosphoramidite is a modified phosphoramidite monomer, which can be used for the oligonucleotide synthesis.
Mitoquinone is a mitochondria-targeted antioxidant designed to accumulate within mitochondria in vivo in order to protect against oxidative damage.
Lyso-PAF C-16 is a substrate of lysoplasmalogen (LysoPls)-specific phospholipase D (LysoPLD). Lyso-PAF C-16 selective acetylates with arachidonic acid[1][2].
Tadalafil-13C,d3 is the deuterium and 13C labeled Tadalafil[1].
SB408124 is a non-peptide antagonist for OX1 receptor with Ki of 57 nM and 27 nM in both whole cell and membrane, respectively; exhibits 50-fold selectivity over OX2 receptor.IC50 Value: 57 nM(Ki)Target: OX1 Receptorin vitro: SB-408124 binds hypocretin type 1 receptor (HcrtR1) with pKi values of 7.57. Calcium mobilization studies shows that SB-408124 is a functional antagonist of the OX1 receptor with a affinity of approximately 50-fold selectivity over the OX2 receptor. A recent study indicates that pretreatment of primary cultures of rat astrocytes with SB-401824 before Orexin A administration significantly reduced the stimulatory action of Orexin A on both basal and forskolin-acivated cAMP production.in vivo: SB-408124 (30 μg/10 μL, administered intracerebroventricularly) decreases Orexin-A induced water intake in Wistar rats. Intracerebroventricularly administered Orexin-A (30 μg/10 μL) blocks the vasopressin (VP) level increase induced by either histamine or 2.5% NaCl administration, and this blocking effect is moderated by pretreatment with SB-408124. Intracerebroventricular pretreatment with SB-408124 (50 mM, 5 μL/h) prevents Bicuculline (BIC)-induced increases in endogenous glucose production (EGP).
S12 is a mutant RAS peptide containing the Gly (G) to Ser (S12) substitution. The sequence of the peptide is KLVVVGASGVGKS[1].
(1E)-3-Methoxy-8,12-epoxygermacra-1,7,10,11-tetraen-6-one (Compound 4) is a natural compound which can be derived from resins obtained from Commiphora sphaerocarpa[1].
Rubelloside B, a triterpenoid glycoside, can be isolated from the roots of Adina rubella. Rubelloside B shows Immunological Enhancement[1].
Taurodeoxychloic Acid (sodium hydrate) prevents apoptosis by blocking a calcium-mediated apoptotic pathway as well as caspase-12 activation. Taurodeoxychloic Acid (sodium hydrate) is investigated for use in several conditions such as Primary Biliary Cirrhosis (PBC), insulin resistance, amyloidosis, Cystic Fibrosis, Cholestasis, and Amyotrophic Lateral Sclerosis[1].
Aminooxy-PEG5-azide is a PEG-based PROTAC linker can be used in the synthesis of PROTACs[1].
2’,3’,5’-Tri-O-acetyl adenosine is an adenosine analog. Adenosine analogs mostly act as smooth muscle vasodilators and have also been shown to inhibit cancer progression. Its popular products are adenosine phosphate, Acadesine (HY-13417), Clofarabine (HY-A0005), Fludarabine phosphate (HY-B0028) and Vidarabine (HY-B0277)[1].
A novel reactivator of wild-type and mutant p53, shows a p53-dependent anti-proliferative activity in human wt and mut p53R280K-expressing tumor cells; enhances p53 transcriptional activity and restores wt-like DNA binding ability to mut p53R280K; inhibits the growth of wt/mut p53-expressing tumors in xenograft mice models, without apparent toxicity.
CB1/2 agonist 4 (compound 24) is a full CB1 agonist and CB2 partial agonist with EC50 values of 15.09 nM and 1.16 nM, respectively. CB1/2 agonist 4 (compound 24) has a significant antinociceptive activity, and also can activate cannabinoid and TRPV1 receptor with values of IC50 and EC50 is 0.8 μM and 0.12 μM, respectively[1].