Thalidomide-PEG2-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology[1].
7-O-Demethyl rapamycin, a derivative rapamycin (HY-10219), has antifungal activity and also immunosuppressant properties. 7-O-Demethyl rapamycin has useful tumor cell growth-inhibiting activity[1].
FGTI-2734 is a RAS C-terminal mimetic dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT) inhibitor with IC50s of 250 nM and 520 nM for FT and GGT, respectively. FGTI-2734 can prevent membrane localization of KRAS, hence solving KRAS resistance problem and thwarting mutant KRAS patient-derived pancreatic tumors[1].
LMP7-IN-2 is a LMP7 inhibitor. LMP7-IN-2 can be used for associated inflammatory diseases and disorders[1].
Regaloside H, a phenylpropanoid glycerol glucoside, is a gluconeogenesis inhibitor. Regaloside H can reduce glucose production in Hepatocytes[1].
Bendroflumethiazide is an orally active diuretic. Bendroflumethiazide is an antihypertensive agent. Bendroflumethiazide has the potential for the research of arterial hypertensive disease[1].
N-(2-Benzoylmercaptopropionyl)glycine ethyl ester-d3 is the deuterium labeled N-(2-Benzoylmercaptopropionyl)glycine ethyl ester[1].
Nolatrexed dihydrochloride (AG 337) is a non-competitive lipophilic inhibitor of thymidylate synthase, interacts at the folate cofactor binding site of the enzyme, with a Ki of 11 nM for human thymidylate synthase[1]. Nolatrexed dihydrochloride (AG 337) has anti-cancer activity, induces cell cycle arrest in S phase of cancer cells[2].
Antibacterial agent 96 (compound 4k) is a potent antibacterial agent. Antibacterial agent 96 shows antitubercular activity against drug-susceptible and multidrug-resistantMycobacterium tuberculosis (M. tuberculosis) strains. Antibacterial agent 96 shows toxicity to HepG2 and Vero cells[1].
Dabigatran(BIB-953; BIBR 953ZW) is a reversible and selective, direct thrombin inhibitor (DTI) with Ki value of 4.5 nM.IC50 Value: 4.5 nM (Ki); 10 nM(Thrombin-induced platelet aggregation) [1]Target: thrombinin vitro: Dabigatran selectively and reversibly inhibited human thrombin(Ki: 4.5 nM) as well as thrombin-induced platelet aggregation (IC(50): 10 nM), while showing no inhibitory effect on other platelet-stimulating agents.Thrombin generation in platelet-poor plasma (PPP), measured as the endogenous thrombin potential (ETP) was inhibited concentration-dependently (IC(50): 0.56 microM). Dabigatran demonstrated concentration-dependent anticoagulant effects in various species in vitro, doubling the activated partial thromboplastin time (aPTT), prothrombin time (PT) and ecarin clotting time (ECT) in human PPP at concentrations of 0.23, 0.83 and 0.18 microM, respectively [1]. in vivo: Dabigatran prolonged the aPTT dose-dependently after intravenous administration in rats (0.3, 1 and 3 mg/kg) and rhesus monkeys (0.15, 0.3 and 0.6 mg/kg). Dose- and time-dependent anticoagulant effects were observed with dabigatran etexilate administered orally to conscious rats (10, 20 and 50 mg/kg) or rhesus monkeys (1, 2.5 or 5 mg/kg), with maximum effects observed between 30 and 120 min after administration, respectively [1]. Patients treated with dabigatran etexilate experienced fewer ischaemic strokes (3.74 dabigatran etexilate vs 3.97 warfarin) and fewer combined intracranial haemorrhages and haemorrhagic strokes (0.43 dabigatran etexilate vs 0.99 warfarin) per 100 patient-years [2].Clinical trial: An Evaluation of the Pharmacokinetics and Pharmacodynamics of Oral Dabigatran Etexilate in Hemodialysis Patients . Phase1
Virgaureagenin F is a saponin that can be extracted from the rhizoma bolbostemmae[1].
SB-743921 free base is a potent selective inhibitor of the mitotic kinesin KSP (Eg5), with a Ki of 0.1 nM. SB-743921 free base can induce mitotic arrest, block cell cycle progression, induce apoptosis, and can be used in the research of myeloma, leukemia and other diseases[1][2].
Metachromins X is a sesquiterpene quinone that arrests the cell cycle progression of HeLa/Fucci2 cells at S/G2/M phase[1].
(-)-Camphoric acid is the less active enantiomer of Camphoric acid. Camphoric acid stimulates osteoblast differentiation and induces glutamate receptor expression. Camphoric acid also significantly induced the activation of NF-κB and AP-1[1].
LDN-57444 is a reversible, competitive and site-directed inhibitor of ubiquitin C-terminal hydrolase L1 (UCH-L1), with an IC50 of 0.88 μM and a Ki of 0.40 μM; LDN-57444 also suppresses UCH-L3 activity, with an IC50 of 25 μM.
DiBoc-Vidarabine-Ribose(diBoc)-2-cyanoethyl-diisopropylphosphoramidite (compound 2) is used for protein modification[1].
DM8966 exhibits potent antibacterial activity against gram-positive and -negative bacteria.
Neryl acetate is a chemical compound isolated from citrus oils[1].
Cibacron Blue 3G-A is an anthraquinone dye, inhibits the R46 β-lactamase with a Ki value of 1.2 uM[1].
CADD522 is a potent inhibitor of runt-related transcription factor-2 (RUNX2)-DNA binding with an IC50 of 10 nM. CADD522 exhibits antitumor activity[1].
BMS-214662 is a potent and selective farnesyl transferase inhibitor with potent antitumor activity with an IC50 of 1.35 nM.
(S)-6-Amino-2-((S)-2-amino-4-(methylthio)butanamido)hexanoic acid compound with formic acid (1:1) is a lysine derivative[1].
Fmoc-Phe(2-Cl)-OH is a phenylalanine derivative[1].
Antifungal agent 73 (compound A32) is an antifungal agent for azole-resistant candidiasis. Antifungal agent 73 disrupts the fungal cell wall and cell membrane. Antifungal agent 73 shows potent in vivo antifungal activity against pathogenic fungi and fluconazole-resistant strains[1].
Feprazone (DA2370; Prenazone), an analogue of Phenylbutazone (HY-B0230), is a nonsteroidal anti-inflammatory agent with analgesic and antipyretic activities. Feprazone acts by inhibiting the activity of cyclooxygenase (COX)-2. Feprazone ameliorates free fatty acid (FFA)-induced oxidative stress by reducing the production of mitochondrial reactive oxygen species (ROS). Feprazone can decrease the expression of MMP-2 and MMP-9. Besides, Feprazone can suppress adipogenesis and increase lipolysis in differentiating 3 T3-L1 cells. Feprazone also can be used to research atherosclerosis and obesity[1][2][3].
Ac-Tyr-Val-Lys-Asp-aldehyde is a caspase-1 inhibitor, can be used for disease research including anemia-associated to chronic diseases, chemotherapy-induced anemia and Diamond-Blackfan anemia[1].
Onilcamotide is a C-terminal peptide of RhoC protein. Onilcamotide is a cancer vaccine and has potential immunomodulating and antineoplastic activities[1].
Exatecan-amide-cyclopropanol (compound 1) is a anticancer agent. Exatecan-amide-cyclopropanol shows anti-proliferation activity against SK-BR-3 and U87 cells, with IC50 values of 0.12 and 0.23 nM, respectively[1].
12-O-Methylcarnosic acid (12-Methoxycarnosic acid), a diterpene carnosic acid isolated from the acetone extract of Salvia microphylla, is an active constituent of 5α-reductase inhibition with an IC50 value of 61.7 μM. 12-O-Methylcarnosic acid inhibits proliferation in LNCaP cells. 12-O-Methylcarnosic acid has antioxidant, anti-cancer and antimicrobial activity[1][2].
WDR5-0102 is an inhibitor targeting WDR5-MLL1 interface (Kdis=7 μM, Kd=4 μM). WDR5-0102 suppresses MLL1 HMT activity, but not human H3K4 methyltransferase SETD7 and six other HMTs: G9a, EHMT1, SUV39H2, SETD8, PRMT3, and PRMT5[1][2].