Hydroxycitric acid tripotassium hydrate (Potassium citrate monohydrate) is the major active ingredient of Garcinia cambogia and a derivative of citric acid. Hydroxycitric acid tripotassium hydrate competitively inhibits ATP citrate lyase with weight loss benefits. Hydroxycitric acid tripotassium hydrate effective inhibits stones formation and also inhibits HIF, and has antioxidation, anti-inflammation and anti-tumor effects[1][2][3][4].
2,7-Dihydrohomoerysotrine is an alkaloid that can be found in Dysoxylum[1].
DSPE-PEG(2000)-Amine is used in the synthesis of solid lipid and thermosensitive liposomal nanoparticles for the delivery of anticancer agents[1][2][3].
Betamethasone disodium phosphate (Betamethasone 21-phosphate disodium salt) is a kind of corticosteroid, which is commonly used in the intralesional research of keloids[1].
UC-112 is a novel potent IAP(Inhibitor of apoptosis) inhibitor; potently inhibit cell growth in two human melanoma (A375 and M14) and two human prostate (PC-3 and DU145) cancer cell lines(IC50=0.7-3.4 uM).IC50 value: 0.7-3.4 uM (Cell assay) [1]Target: IAP inhibitorin vitro: UC-112 also potently inhibits the growth of P-glycoprotein (P-gp)-overexpressed multidrug-resistant cancer cells, strongly activates caspase-3/7 and caspase-9 activities, and selectively downregulates survivin level at a concentration as low as 1 μM. Coincubation of UC-112 with a known proteasome inhibitor Z-Leu-Leu-Leu-CHO (MG-132) rescued survivin inhibition, consistent with the anticipated mechanism of action for UC-112 [1].in vivo: As a single agent, UC-112 strongly inhibits tumor growth and reduces both X chromosome-linked IAP and survivin levels in an A375 human melanoma xenograft model in vivo [1].
PI4K-IN-1 (compound 44) is a potent PI4KIII inhibitor, with pIC50 values of 9.0 and 6.6 for PI4KIIIα and PI4KIIIβ, respectively. PI4K-IN-1 also inhibits PI3Kα/β/γ/δ, with pIC50 values of 4.0/<3.7/5.0/<4.1, respectively[1].
TD-165 is a cereblon (CRBN) degrader. TD-165comprises a cereblon (CRBN) ligand binding group, a linker and an von Hippel-Landau (VHL) binding group[1].
DNA Gyrase-IN-3 (Compound 28) is a bacterial DNA gyrase B inhibitor with IC50s of 5.41-15.64 µM for E. coli DNA gyrase. Anti-tubercular and antibacterial activity[1].
Desacetyl bisacodyl is the active metabolite of the laxative bisacodyl. Desacetyl bisacodyl induces epithelial Cl(-) secretion in rat colon and rectum. Desacetyl bisacodyl evokes several effects at the colon or rectum, including increased mucus and chloride secretion[1].
Schineolignin B is a Lignan that can be isolated from the fruit of schisandra chinensis. schisandra chinensis has antihepatitis, antitumor, and anti-HIV-1 activities[1].
SKI-II is a synthetic inhibitor of sphingosine kinase (SK) activity with IC50 of 78 μM for SK1 and 45 μM for SK2.IC50 value: 78/45 μM (SK1/2) [2]Target: SKin vitro: SKI II inhibits cell proliferation by suppressing the Wnt/β-catenin signaling pathway. SKI II also reduces the expression of c-Myc and cyclin D1, the downstream target genes of the Wnt signaling pathway. SKI II inhibits cell proliferation by suppressing the Wnt/β-catenin signaling pathway. SKI II promotes the degradation of β-catenin by enhancing Wnt5A. SKI II inhibits the proliferation of HepG2 cells by blocking the Wnt/β-catenin signaling pathway. [1]in vivo: SKI-II causes an irreversible inhibition of SK1 by inducing its lysosomal and/or proteasomal degradation. In the present study, SKI-II was administered 3-weekly i.p. to LDL-R-/- mice for 16 weeks at a dose previously demonstrated to reduce tumor growth in mice. Preliminary experiments revealed that a single administration of SKI-II produces a significant reduction of plasma S1P with the maximum (40%) observed 12 h after injection. [2]
(23E)-5b,19-epoxycucurbita-6,23,25(26)-triene-3b-ol is a cucurbitane triterpenoid. (23E)-5b,19-epoxycucurbita-6,23,25(26)-triene-3b-ol can be isolated from the seeds of Momordica charantia L[1].
Nevirapine is a non-nucleoside inhibitor of HIV-1 reverse transcriptase used to treat and prevent HIV/AIDS; with a Ki of 270 μM.
Wulignan A1 is isolated from the stems of Schisandra henryi. Wulignan A1 exhibits anti-influenza virus H1N1 and H1N1-TR (a Tamiflu drug resistant virus strain) activities[1].
HDAC6-IN-11 (Compound 9) is a selective HDAC6 inhibitor with the IC50 value of 20.7 nM. HDAC6-IN-11 has more than 300-fold selectivity over HDAC other isoforms. HDAC6-IN-11 shows anti-proliferative activities against cancer cells[1].
TAK-024 is a platelet inhibitor with IC50s of 31, 79 and 51 nM in human, monkey and guinea pig, respectively.
Mal-C2-cyclohexylcarboxyl-hydrazide hydrochloride is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Nikkomycin Z, a nucleoside-peptide, is a selective competitive chitin synthesis inhibitor. Nikkomycin Z has antifungal effects and acts as a competitive analogue of the chitin synthase substrate UDP-N-acetylglucosamine[1].
Xylan represents the main hemicellulose component in the secondary plant cell walls of flowering plants. Xylan is a polysaccharide made from units of xylose and contains predominantly β-D-xylose units linked as in cellulose.
Prostaglandin E1-d4 (Alprostadil-d4) is the deuterium labeled Prostaglandin E1. Prostaglandin E1 (Alprostadil) is a prostanoid receptor ligand, with Kis of 1.1 nM, 2.1 nM, 10 nM, 33 nM and 36 nM for mouse EP3, EP4, EP2, IP and EP1, respectively. Prostaglandin E1 induces vasodilation and inhibits platelet aggregation. Prostaglandin E1 can be used as a vasodilator for the research of peripheral vascular diseases[1][2][3].
Tau Peptide (295-309) is a polypeptide that can be found by peptide screening. Peptide screening is a research tool that pools active peptides primarily by immunoassay. Peptide screening can be used for protein interaction, functional analysis, epitope screening, especially in the field of agent research and development[1].
Cefotaxime, a third-generation cephalosporin antibiotic, possesses broad-spectrum antibiotic activity against numerous Gram-positive and Gram-negative bacteria[1][2][3][4].
Glp-His-Pro-Gly-NH2 (pGlu-His-Pro-Gly-NH2) is a peptide containing 4 amino acids. Glp-His-Pro-Gly-NH2 stimulates gonadotrophin, luteinizing hormone (LH) and follicle stimulating hormone (FSH) release[1][2].
Linifanib (ABT-869) is a multi-targeted inhibitor of VEGF and PDGFR receptor family with IC50s of 3, 4, 66, 4 nM for KDR, Flt-1, PDGFRβ and FLT3, respectively.
SHP2 protein degrader-2 (SHP2-D26) is a SHP2 protein PROTAC degrader. SHP2 protein degrader-2 reduces expression level of SHP2 in various cancer cells[1].
Tilomisole (Wy 18251) is a benzimidazothiazole experimental drug with anti-inflammatory activity. Tilomisole causes less agranulocytosis than levamisole, but retains immunomodulating capabilities. Tilomisole is orally active. Tilomisole has the potential for the research of cancer and inflammation[1][2].
2,4-D Methyl ester-d3-1 is the deuterium labeled 2,4-D methyl ester[1].
Phenylalanylalanine (H-Phe-Ala-OH) is a dipeptide composed of phenylalanine and alanine. Phenylalanylalanine is an incomplete breakdown product of protein digestion or protein catabolism[1].
Scabronine M is a novel inhibitor of NGF-induced neurite outgrowth from PC12 cells.
Ecliptasaponin D is a triterpenoid glucoside isolated from Eclipta alba (L.) Hassk which is the aerial part of Eclipta prostrate. Eclipta prostrate is considered as a nourishing herbal medicine with pleiotropic effects, including anti-inflammatory, hepatoprotective, antioxidant and immunomodulatory[1,2].