PSNCBAM-1 is a selective CB1 receptor allosteric antagonist with an EC50 of 0.1 μM. PSNCBAM-1 can be used in the researches of obesity[1].
Methyl ganoderate H is a natural product that can be isolated from Ganoderma lucidum. Methyl ganoderate H has moderate inhibitory effect to NO production[1].
E3 Ligase Ligand-Linker Conjugates 24 (TFA) incorporates an E3 ligase ligand and a linker, can be an immunomodulater for the treatment of cancer.
Lebrikizumab is an IgG4 humanized monoclonal antibody that specifically binds to interleukin-13 (IL-13) and inhibits its function. Lebrikizumab can be used for the research of asthma[1].
LIT-001 trifluoroacetate (LIT001) is the first nonpeptide Oxytocin receptor (OT-R) agonist with EC50 of 55 nM, Emax=96%; efficiently relieved social interaction deficits in Oprm1−/− mice, a mouse model of autism.
(S)-ErSO is the dextrorotatory enantiomer of ErSO. (S)-ErSO is inactive in MCF-7 cells (from patent WO2020009958A1, compound (s)-105)[1].
DOTA derivative is a benxyl derivative of the cyclic tosamide; can be nitrated directly; is more convenient to incorporate the nitro group after deprotection lithium aluminum hydride.
Oligomycin A, created by Streptomyces, acts as a mitochondrial F0F1-ATPase inhibitor, with a Ki of 1 μM; Oligomycin A shows anti-fungal activity.
Emprumapimod is a potent, orally bioavailable and selective inhibitor of p38α MAPK directly inhibits LPS-induced IL-6 production from RPMI-8226 cell (IC50=100 pM). Emprumapimod can be used for the research of dilated cardiomyopathy and acute inflammatory pain[1][2].
RTS-V5 is a dual HDAC/proteasome inhibitor with IC50s of 6.9, 18, 15, 0.27, 0.53 μM for HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, respectively.
H-8 (dihydrochloride) is a cell-permeable, reversible and ATP-competitive PKA inhibitor[1].
Shizukanolide, a sesquiterpene lactone, can be isolated from Chloranthus japonicus (Chloranthaceae). The dehydro-compound of Shizukanolide, shows moderate antifungal activity[1].
Fluxametamide is an insecticide with wide spectrum, acts as an antagonist of GABA- and glutamate-gated chloride channels, with IC50 of 1.95 nM and 225 nM for M. domestica GABACls and GluCls.
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].
Methyltetrazine-PEG5-NHS ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[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].
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.
(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.
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].
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].
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].
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.
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].