Nef-IN-B9 (Nef inhibitor B9) is a small molecule that blocks Nef-dependent Hck activity with IC50 of 2.8 uM, while the activity against Hck alone is >20 uM; also showes weak activity against other Src-family members with IC50 of >20 uM for c-Src, Lck and Lyn; blocks wild-type HIV-1 replication with IC50 of 100-300 nM, and blocks Nef-mediated SFK activation in HIV-infected cells; binds directly to Nef with Kd of 1.79 nM.
Bragsin1 is a potent, selective and noncompetitive inhibitor of the ArfGEF BRAG2, inhibits Arf GTPase activation, with an IC50 of 3 μM. Bragsin1 binds to PH domain of BRAG2, and is a noncompetitive interfacial inhibitor. Bragsin1 has no effect on the Sec7 domain of human ArfGEFs. Anti-cancer activity[1].
Sifalimumab (MEDI-545) is an anti-IFNα monoclonal antibody. Sifalimumab suppresses the abnormal immune activity by binding to multiple interferon-alpha (IFNα) subtypes. Sifalimumab can be used in systemic lupus erythematosus (SLE) research[1][2].
Deferitrin (GT-56-252), a desferrithiocin (DFT) analogue, is an orally active trident iron chelator. Deferitrin is used for chronic iron overload due to transfusional therapy. Deferitrin has the potential for beta-thalassemia major[1][2].
FX-06 (Fibrin-derived peptide Bβ15-42) is a fibrin Bbeta chain-derived peptide. FX-06 binds to VE-cadherin and inhibits leukocyte transmigration and initiates VE-cadherin-mediated signaling. FX-06 can be used in the research of ischemia/reperfusion injury, Dengue shock syndrome (DSS)[1][2][4].
PF-03814735 is a potent, orally available and reversible aurora A and aurora B inhibitor with IC50s of 0.8 and 0.5 nM, respectively.
Baxdrostat is a aldosterone synthase inhibitor[1].
m7GpppGmpG, an oligonucleotide, is an M7GpppNpG trinucleotide cap analogue. m7GpppGmpG can be used as a chemical tool enabling manufacturing of RNA featuring either cap 0 or cap 1 structures[1].
HM30181 is a potent and selective inhibitor of P-glycoprotein.
5-Heptadecylresorcinol (AR-C17), a phenolic lipid component, is also an orally active mitochondrial protector. 5-Heptadecylresorcinol improves mitochondrial function via sirtuin3 signaling pathway, thus alleviates endothelial cell damage and apoptosis. 5-Heptadecylresorcinol induces sirtuin3-mediated autophagy. 5-Heptadecylresorcinol reduces the atherosclerotic plaques in the aortic root region of mice heart. 5-Heptadecylresorcinol can be used for research of atherosclerosis prevention and obesity[1][2].
FNLPLGNYKKP is a peptide fragment of brain-derived acidic fibroblast growth factor.
Isocoronarin D is a diterpene that can be isolated from rhizomes of Hedychium coronarium. Isocoronarin D can be used for the research of cancer[1].
5-Methyl-2'-O,4'-C-methylenecytidine is a cytidine nucleoside analog. Cytidine analogs have a mechanism of inhibiting DNA methyltransferases (such as Zebularine, HY-13420), and have potential anti-metabolic and anti-tumor activities[1].
Morniflumate (UP 164) is an orally active nonsteroidal anti-inflammatory agent. Morniflumate can be used in the study of inflammatory diseases such as osteoarthritis, painful musculoskeletal disorders and soft tissue inflammation.
BTM-3528 is an activator of the mitochondrial protease OMA1 and mediates excessive activation of the mitochondrial integrated stress response (ISR). BTM-3528 stimulates OMA1-dependent DELE1 and OPA1 cleavage and mitochondrial fragmentation. BTM-3528 activates eIF2α kinase HRI, inducing cell growth arrest and apoptosis. BTM-3528 has anticancer activity against multiple DLBCL cell lines and has in vivo inhibitory potency in a mouse model xenografted with human DLBCL SU-DHL-10 cells[1].
Cinnamtannin A2, a tetrameric procyanidin, can increases GLP-1 and insulin secretion in mice. Cinnamtannin A2 could upregulate the expression of corticotrophin releasing hormone. Cinnamtannin A2 exhibits antioxidant, anti-diabetic and nephroprotective effect[1][2].
Adrenorphin is a opioid octapeptide, acting as a potent agonist of μ-opioid receptor, with Ki of 12 nM.
TDCPP is a chlorinated analog of tris(2,3-dibromopropyl)phosphate (Tris) which is one of the most detected organophosphorus flame retardants (OPFRs) in the environment.
2-Methoxyestradiol-d5 is the deuterium labeled 2-Hydroxyestradiol. 2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa[1][2][3][4][5][6][7].
Levosimendan(OR1259) is a calcium sensitiser used in the management of acutely decompensated congestive heart failure.Target: OthersLevosimendan is a calcium sensitiser used in the management of acutely decompensated congestive heart failure. Levosimendan is an inodilator indicated for the short-term treatment of acutely decompensated severe chronic heart failure, and in situations where conventional therapy is not considered adequate. Levosimendan has shown preliminary positive effects in a range of conditions requiring inotropic support, including right ventricular failure, cardiogenic shock, septic shock, and Takotsubo cardiomyopathy [1]. The cardiovascular effects of levosimendan are exerted via more than an isolated drug-receptor interaction, and involve favorable energetic and neurohormonal changes that are unique in comparison to other types of inodilators [2]. Levosimendan might reduce mortality in cardiac surgery and cardiology settings of adult patients [3].
Pamapimod-d4 (Ro4402257-d4) is the deuterium labeled Pamapimod. Pamapimod (Ro4402257) is a potent, selective and orally active p38 MAPK inhibitor with IC50s of 14 nM and 480 nM and Kis of 1.3 nM and 120 nM for p38α and p38β, respectively. Pamapimod has no activity against p38δ or p38γ isoforms. Pamapimod has the potential for rheumatoid arthritis and other autoimmune diseases treatment[1][2].
Amylin (8-37), rat is a truncated analog of native Amylin that selectively inhibits insulin-related glucose uptake and glycogen deposition in muscle tissue. Amylin (8-37), rat is a weak amylin receptor (AMY) antagonist.
Neratinib is an orally available, irreversible tyrosine kinase inhibitor with IC50s of 59 nM and 92 nM for HER2 and EGFR, respectively.
N-Benzylnaltrindole hydrochloride is a potent δ2-selective opioid receptor antagonist. Benzylnaltrindole hydrochloride has a long duration of action in vivo than Naltriben (NTB). N-Benzylnaltrindole hydrochloride iserve as a useful tool in the pharmacologic characterization of δ-opioid receptor function[1].
Ethyl-L-NIO hydrochloride is a potent and competitive human dimethylarginine dimethylaminohydrolase 1 (hDDAH-1) inhibitor with an IC50 of 70 μM and a Ki of 32 μM[1].
CAXII-IN-1 (Compound 17) is a selective CA XII inhibitor with Ki values of 3.8 nM and 56.0 nM against hCA XII and hCA IX, respectively. CAXII-IN-1 shows antitumor activity[1].
Oleanolic acid-3-O-glucosyl(1-2)xylyl(1-3)glucosiduronic acid is a nature occurring triterpene saponin[1].
Cy3 NHS (Cyanine3 NHS ester) is a water-soluble and yellow emitting fluorescent dye for labeling amino-groups in biomolecules. Used to label soluble proteins, peptides, and oligonucleotides/DNA.
FITC is a derivative of fluorescein for the labeling of amines.
DOXO-EMCH is a 6-maleimidocaproyl hydrazone derivative of Doxorubicin, is an albumin binding prodrug.