6-Methyl-5-azacytidine is a potent DNMT inhibitor.
Biotin-PEG2-NHS ester is a biotin-labeled, PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
GPVI antagonist 2 (Compound 1) is a potential antagonist of Glycoprotein VI (GPVI). IC50 values of GPVI antagonist 2 are, respectively, 0.35 μM for collagen, 0.80 μM for CRP, 195.2 μM for convulxin and 81.38 μM for thrombin. Glycoprotein VI (GPVI) is a platelet major collagen receptor and a target for potent and safe antithrombotic research. GPVI antagonist 2 is a promising antiplatelet agent[1].
Dorsomorphin dihydrochloride (BML-275 dihydrochloride) is a potent, selective and ATP-competitive AMPK inhibitor, with a Ki of 109±16 nM.
Atractyloside A(126054-77-1) is a natural TCM reference compound.
Calcimycin (A-23187) hemimagnesium is an antibiotic and a unique divalent cation ionophore (like calcium and magnesium). Calcimycin hemimagnesium induces Ca2+-dependent cell death by increasing intracellular calcium concentration. Calcimycin hemimagnesium inhibits the growth of Gram-positive bacteria and some fungi. Calcimycin hemimagnesium also inhibits the activity of ATPase and uncouples oxidative phosphorylation of mammalian cells. Calcimycin hemimagnesium induces apoptosis[1][2][3][4].
AZD-7762 is a potent ATP-competitive checkpoint kinase (Chk) inhibitor in with an IC50 of 5 nM for Chk1.
(Rac)-Normetanephrine-d3 is the deuterium labeled (Rac)-Normetanephrine[1].
Onartuzumab (MetMAb) is a unique, humanized and affinity-matured monovalent (one-armed) monoclonal antibody against the MET receptor. Onartuzumab potently inhibits HGF binding and receptor phosphorylation and signaling. Onartuzumab has antibody-like pharmacokinetics and antitumor activity[1].
Diayangambin (Syringaresinol dimethyl ether; Lirioresinol C dimethyl ether) is a cell proliferation inhibitor with an IC50 value of 1.5 μM against human monocytes. Diayangambin also has immunosuppressive and anti-inflammatory effects[1].
BTK-IN-5 is a covalent BTK inhibitor for treating medical conditions such as cardiovascular diseases, respiratory diseases, inflammation, and diabetes.
NCT-503 is a phosphoglycerate dehydrogenase (PHGDH) inhibitor with an IC50 of 2.5 µM.
FIN56 is a specific inducer of ferroptosis.
Oregovomab (Alt-2 monoclonal antibody) is a murine mAb targeting CA125. Oregovomab induces cytotoxic immune response against CA125 expressing tumor cells[1][2].
N6-Carbobenzoxy-L-lysine benzyl ester hydrochloride is a lysine derivative[1].
Embelin is a cell-permeable benzoquinone compound that exhibits antitumor properties. Specifically antagonizes XIAP-mediated inhibition of caspase-9 activation by directly targeting the Smac and caspase-9 binding domain BIR3 (IC50 = 4.1 uM in a competitive binding assay with Smac peptide).IC50 value: 4.1 uM [1]Target: XIAPin vitro: Embelin induced activation of caspase-9 and embelin-induced apoptosis was prevented by caspase inhibitors [2]. Treatment with subtoxic doses of Embelin broadly sensitized malignant glioma cells to TRAIL-mediated apoptosis. Notably, human astrocytes were not significantly affected by the combined treatment consisting of Embelin and TRAIL. Combined treatment with Embelin and TRAIL augmented the activation of initiator caspases-8/-9 and effector caspases-3/-7, respectively [3]. in vivo: Embelin inhibited topical edema in the mouse ear, leading to substantial reductions in skin thickness and tissue weight, inflammatory cytokine production, neutrophil-mediated myeloperoxidase activity, and various histopathological indicators. Furthermore, embelin was effective at reducing inflammatory damage induced by chronic TPA exposure [4]. Embelin (10, 30 or 50mg/kg body weight) was administrated daily per oral route for 7days. Embelin significantly attenuated DSS-induced DAI scores and tissue MPO accumulation, which implied that it suppressed weight loss, diarrhea, gross bleeding, and the infiltrations of immune cells. Embelin administration also effectively and dose-dependently prevented shortening of colon length and enlargement of spleen size [5].
H-Glu-Tyr-OH is adipeptide.
Syncytial Virus Inhibitor-1 is a potent, orally bioavailable respiratory syncytial virus (RSV) fusion inhibitor with EC50s of 0.002 μM, 0.004 μM, and 0.002 μM for RSV Long, RSV A2, and RSV B strains, respectively[1].
TIC10 isomer is the isomer of TIC10. TIC10 isomer does not possess the reported biological activity of inducing TRIAL expression.
Orthocaine is a local anesthetic agent (extracted from patent WO2002089849A1)[1].
Agrimol B is a polyphenol derived from Agrimonia pilosa Ledeb, suppresses adipogenesis via inducing SIRT1 translocation and expression, and reducing PPARγ expression[1].
AD57 hydrochloride is an orally active multikinase inhibitor, inhibits RET, BRAF, S6K and Src[1].
VU6004909 is a mGlu5 receptor positive allosteric modulator (pEC50: 7.59). VU6004909 shows antipsychotic-like effects. VU6004909 can reverse MK801-induced cortical hyperactivity and cognitive deficits[1][2].
16β-Hydroperoxyalisol B 23-acetate is a natural product that can be isolated from Alisma orientale[1].
Cupressuflavone is a natural product that can be found in Cupressus macrocarpa. Cupressuflavone exhibits anti-inflammatory and antiulcerogenic activities. Cupressuflavone also show protective effects against CCl4-induced hepato- and nephrotoxicity in mice[1][2][3].
NCX899 is a NO-releasing derivative of enalapril, and shows inhibitory activity against angiotensin-converting enzyme (ACE) activity.
Fludroxycortide is a synthetic topical steroid and is used as an anti-inflammatory treatment for use on skin irritations.
3-Acetoxy-11-ursen-28,13-olide (11,12-dehydroursolic lactone acetate) is a reduction product of 11-ketoursolic acid[1].
XL 188 is a potent and selective USP7 inhibitor with IC50 values of 90 nM and 193 nM for USP7 full-length and catalytic domain enzyme, respectively. XL 188 can be used in research of cancer[1].
TET 830 modified/T-helper epitope from tetanus toxoid is a modified T-helper epitope from tetanus toxoid. TET 830 modified/T-helper epitope from tetanus toxoid induces T-cells responses and is used as a helper peptide in vaccinations[1].