Tonapofylline (BG 9928) is an orally active and selective adenosine A1 receptor antagonist with a Ki of 7.4 nM for human adenosine A1 receptor (hA1), which displays 915-fold selectivity versus human adenosine A2A receptor and 12-fold selectivity versus human adenosine A2B receptor and is used in development for the treatment of heart failure[1][2].
Pomalidomide-C3-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a linker used in PROTAC technology[1].
AXL-IN-13 is a potent and orally active AXL inhibitor (IC50: 1.6 nM, Kd: 0.26 nM). AXL-IN-13 reverses TGF-β1-induced epithelial-mesenchymal transition (EMT), and inhibits cancer cell migration and invasion[1].
Corynoxine is an enantiomer of Corynoxine B; induces autophagy in different neuronal cell lines, including N2a and SHSY-5Y cells.IC50 value:Tareget: Autophagy inducerIn vivo, Cory promotes the formation of autophagosomes in the fat bodies of Drosophila. By inducing autophagy, Cory promotes the clearance of wild-type and A53T α-syn in inducible PC12 cells. Interestingly, different from its enantiomer Cory B, Cory induces autophagy through the Akt/mTOR pathway as evidenced by the reduction in the levels of phospho-Akt, phospho-mTOR and phospho-p70 S6 Kinase [1]. Corynoxine significantly decreased locomotor activity after oral administration to mice [2].
MurF-IN-1 (Compound 7) is a MurF inhibitor with an pIC50 of 5.19 against S. pneumoniae MurF[1].
Antitrypanosomal agent 4 (compound 19) is a potent and blood-brain barrier permeable antitrypanosomal agent. Antitrypanosomal agent 4 has good activity against Trypanosoma cruzi (T. cruzi) and Trypanosoma brucei brucei (T. b. brucei) with IC50s of 1.2 μM and 70 nM, respectively[1].
Genz-123346 (free base) is an inhibitor of GL1 synthase that blocks the conversion of ceramide to GL1; inhibits GM1 with IC50 value of 14 nM.
Sephadex G 25 is a dextran chromatography medium. Sephadex G-25 separates from 1 to 5 kD (spherical proteins) and can be used for the separation of peptides as well as for the desalting and buffer replacement of large molecule proteins[1].
(Rac)-Hesperetin-13C,d3 is the 13C- and deuterium labeled. (Rac)-Hesperetin is the racemate of Hesperetin. Hesperetin is a natural flavanone, and acts as a potent and broad-spectrum inhibitor against human UGT activity. Hesperetin induces apoptosis via p38 MAPK activation.
Momelotinib-3,3,5,5-d4 (CYT387-3,3,5,5-d4) is the deuterium labeled Momelotinib (HY-10961). Momelotinib has inhibitory activity for JAK1/JAK2[1][2].
1,5-Dihexadecyl N-(3-carboxy-1-oxopropyl)-L-glutamate is a lipid. 1,5-Dihexadecyl N-(3-carboxy-1-oxopropyl)-L-glutamate can be used for the synthesis of phospholipid vesicle and improve the encapsulation efficiency of proteins[1].
MSBN is a highly selective fluorogenic probe for thiols, selectively imaging thiols in live cells and specifically label protein thiols with a turn-on signal to determine diverse reversible protein thiol modifications.
2-Chloroinosine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
LY2183240 is a novel and highly potent blocker of anandamide uptake (IC50 = 270 pM). LY2183240 inhibits fatty acid amide hydrolase (FAAH) activity (IC50 = 12.4 nM). IC50: 270 pM (anandamide uptake); 12.4 nM (FAAH)Target: FAAH; Anandamide uptakeFollowing i.p. administration in rats, LY2183240 increases brain anandamide concentration and exerts antinociceptive effects in formalin model of pain.
Donasine, indole alkaloid, is a nature product with effect of reducing fever. Donasine can be isolated from the rhizomes of Arundo donax L[1].
3-O-Caffeoylquinic acid methyl ester is a chemical constituent of Pyrrosia calvata[1].
Boc-Tyr(PO3Me2)-OH is a tyrosine derivative[1].
3'-Deoxy-3'-fluoroadenosine is a purine nucleoside analogue. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
Azido-PEG10-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Siplizumab (MEDI-507) is a humanized IgG1 monoclonal antibody against CD2. Siplizumab depletes T cells, decreases T cell activation, inhibites T cell proliferation and enriches naïve and bona fide regulatory T cells[1].
Fabiatrin is a natural product isolated from Przewalskia tangutica[1].
NH-bis(C1-Boc)is a uncleavable linker used for antibody-drug conjugates (ADC).
Filixic acid ABA is a molluscicidal agent against B. peregrina adult snails, with an LD50 of 8.40 ppm. Filixic acid ABA shows 100% mortality of B. peregrina at 15 ppm[1].
Pseudojervine is a glycoalkaloid with a feeble inhibition activity against platelet aggregation[1].
N1-Propargylpseudouridine (see GL102032) is a purine nucleoside analogue. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
GDP366, a dual inhibitor of survivin and Op18, induces cell growth inhibition, cellular senescence and mitotic catastrophe in human cancer cells.
Mesitaldehyde is an endogenous metabolite.
VEGFR-2-IN-21 (Compound 5d) is a potent VEGFR-2 inhibitor with an IC50 of 0.10 μM. VEGFR-2-IN-21 shows anticancer activity[1].
5-Fluoromethylornithine (5-FMOrn) dihydrochloride is a specific irreversible inhibitor of L-ornithine:2-oxoacid aminotransferase (OAT). 5-Fluoromethylornithine dihydrochloride can be used in the study of gyrate atrophy of choroid and retina[1][2].
6α-Hydroxypolyporenic acid C, a lanostane triterpenoid, is a nature product that could be isolated from the sclerotium of Poria cocos. 6α-Hydroxypolyporenic acid C can be absorbed across intestinal epithelial cells[1].