HCV-IN-37 (Compound 3d) is a potent inhibitor of HCV. HCV-IN-37 is orally available and long-lasting in rat plasma after oral administration to rats by a single dose of 15 mg/kg. The high potency of active derivative HCV-IN-37 is primarily driven by the inhibitory effect on the virus entry stage[1].
Tubastatin A is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in a cell-free assay, and is selective (1000-fold more) against all other isozymes except HDAC8 (57-fold more).
Mycophenolate Mofetil is a non-competitive, selective and reversible inhibitor of inosine monophosphate dehydrogenase (IMPDH) with IC50s of 39 nM and 27 nM, respectively.
4-Phenylbutyric acid-d5 is the deuterium labeled 4-Phenylbutyric acid[1]. 4-Phenylbutyric acid (4-PBA) is an inhibitor of HDAC and endoplasmic reticulum (ER) stress, used in cancer and infection research[2][3][4].
Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition[1][2][3].
RGB-286147 is a selective and ATP-competitive CDK and CDK-related kinases (CRK) inhibitor with 50 values ranging from 9-839 nM. RGB-286147 shows less active against other non-CDK/CRK kinases. RGB-286147 induces cell apoptosis, and exhibits anti-tumor activity[1].
Siramesine(Lu 28-179) Hcl is a selective sigma-2 receptor agonist, which has been shown to trigger cell death of cancer cells and to exhibit a potent anticancer activity in vivo. IC50 value:Target: sigma-2 receptor; lysosome-destabilizing agentsiramesine can induce rapid cell death in a number of cell lines at concentrations above 20 μM. In HaCaT cells, cell death was accompanied by caspase activation, rapid loss of mitochondrial membrane potential (MMP), cytochrome c release, cardiolipin peroxidation and typical apoptotic morphology, whereas in U-87MG cells most apoptotic hallmarks were not notable, although MMP was rapidly lost [1]. Siramesine, a sigma-2 receptor agonist originally developed as an anti-depressant, can induce cell death in transformed cells through a mechanism involving lysosomal destabilization [2].in vivo: SA4503 or siramesine given jointly with MEM (as well as with AMA) decreased the immobility time in rats. The effect of SA4503 and AMA co-administration was antagonized by progesterone, a sigma1 receptor antagonistic neurosteroid. Combined treatment with siramesine and AMA was modified by neither progesterone nor BD1047 (a novel sigma antagonist with preferential affinity for sigma1 sites) [3]
Thalidomide-propargyl is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide-propargyl can be connected to the ligand for protein by a linker to form the IMiD containing PROTACs[1].
Cy-FBP/SBPase-IN-1 (compound S5) is a Cy-FBP/SBPase inhibitor, which is an important regulatory enzyme in cyanobacterial photosynthesis. Thus Cy-FBP/SBPase-IN-1 inhibits Calvin cycle and photosystem, and decreases photosynthetic efficiency in cyanobacterial photosynthesis. Cy-FBP/SBPase-IN-1 potently inhibits the growth of cyanobacteria, as well as Synechocystis sp.PCC6803. Cy-FBP/SBPase-IN-1 shows safety profile in human-derived cells and zebrafish models[1].
AMG131 (INT131), a potent and highly selective PPARγ partial agonist, binds to PPARγ and displaces Rosiglitazone with a Ki of ~10 nM. AMG131 can be used for research of type-2 diabetes mellitus (T2DM)[1][2].
BKT140 4-fluorobenzoyl is a novel CXCR4 antagonist with an IC50 vakue of ～1 nM. Sequence: 4F-Benzoyl-Arg-Arg-{2-Naph-Ala}-Cys-Tyr-{Cit}-Lys-Lys-Pro-Tyr-Arg-{Cit}-Cys-Arg-NH2(Disulfide bridge: Cys4-Cys13).
MCL0020 is a potent and selective melanocortin MC4 receptor antagonist, with an IC50 of 11.63 nM. MCL0020 dose-dependently and significantly attenuates restraint stress-induced anorexia without affecting food intake[1].
Carindacillin (Carbenicillin indanyl) sodium is an orally active and broad-spectrum antimicrobial agent. Carindacillin sodium can be hydrolyzed to Carbenicillin in vivo. Carindacillin sodium can be used for the research of urinary-tract infection[1][2].
Clematomandshurica saponins B shows significant inhibitory activity on cyclooxygenase-2 (IC50=2.58 mM)[1].
8-Phenyl-2,6-diethyl-BODIPY 505/515 is a derivative of BODIPY 505/515 (Ex=525 nm，Em=544 nm)[1].
ODN D-SL03 is a C class CpG oligonucleotides, can induce stimulate PBMCs to produce high level of IFN-α. ODN D-SL03 can activate human B cells, NK cells and mononuclear cells and up-regulate expression of CD80, CD86 and HLA-DR on the surface of subsets in human PBMCs. ODN D-SL03 also can inhibit the growth of the tumor. ODN D-SL03 sequence: 5'-tcgcgaacgttcgccgcgttcgaacgcgg-3'[1].
(+)-Epieudesmin is an antineoplastic agent. (+)-Epieudesmin has marginal cancer cell line inhibitory activities. (+)-Epieudesmin inhibits the growth of Gram-negative pathogen[1].
N-Heptyl 4-hydroxybenzoate-d4 is the deuterium labeled N-Heptyl 4-hydroxybenzoate[1].
TRPV4 antagonist 4 is a potent TRPV4 antagonist with an IC50 value of 22.65 nM. TRPV4 antagonist 4 inhibits TRPV4 current. TRPV4 antagonist 4 shows protective effects on acute lung injury[1].
1,2,3,6-Tetragalloylglucose is a potent UDP glucuronosyltransferase 1 family, polypeptide A1 (UGT1A1) inhibitor, with a Ki of 1.68 μM[1].
(D-His2)-Goserelin is a derivative of Goserelin, a decapeptide analog of gonadotropin-releasing hormone (GnRH/LHRH)[1].
Amino-PEG4-CH2COOH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1]. Amino-PEG4-CH2COOH is also a non-cleavable 4 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[2].
Utomilumab (PF 05082566) is a fully human IgG2 mAb agonist of the T-cell costimulatory receptor 4-1BB/CD137. Utomilumab can be used for the research of relapsed/refractory follicular lymphoma (FL) and other CD20+ non-Hodgkin lymphomas (NHL)[1][2].
Ridogrel (R 68070) is an orally active combined thromboxane A2 synthetase inhibitor and thromboxane A2/prostaglandin endoperoxide receptor blocker. Ridogrel is potent antiplatelet agent. Anti-inflammatory activities[1][2][3].
FKKSFKL-NH2 is a protein kinase C-selective peptide. FKKSFKL-NH2 can be used for the research of various biochemical[1].
Adenosine 5'-monophosphate monohydrate is an adenosine A1 receptor agonist.
4-Acetylsulfanilamide-13C6 is the 13C6 labeled 4-Acetylsulfanilamide.
27-p-Coumaroyloxyursolic acid (compound 6) is a kind of ulmoidol. 27-p-Coumaroyloxyursolic acid can be isolated from Ilex kudincha. 27-p-Coumaroyloxyursolic acid is an inhibitor of Acyl CoA Cholesteryl Acyl Transferase (ACAT) with an IC50 value of 0.73 μM[1].
ZK756326 is a nonpeptide chemokine receptor agonist for the CC chemokine receptor CCR8.
Azido-PEG5-azide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].