Thalidomide-NH-(CH2)2-NH-Boc is a Boc-modified Thalidomide (HY-14658) that acts as a Cereblon ligand to recruit CRBN protein. The Boc protecting group at the end of Thalidomide-NH-(CH2)2-NH-Boc can be removed under acidic conditions to participate in the synthesis of PROTAC molecules. Thalidomide-NH-(CH2)2-NH-Boc is a key intermediate in the synthesis of CRBN-based PROTAC molecules.
As-358 (hydrochloride) has inhibitory effects against Ebola virus and Marburg virus with IC50s of 9.1 μM and 18.1 μM, as well as exhibits good in vivo safety[1].
TRAF-STOP inhibitor 6877002, is a selective inhibitor of CD40-TRAF6 interaction, compound VII, shows inhibition of NF-κB activation in RAW cells, extracted from patent WO2014033122A1[1]. TRAF-STOP 6877002 prevents the progression of established atherosclerosis in mice, reduces leukocyte recruitment and reduces macrophage activation; reduces macrophage proliferation in atherosclerotic plaques[2].
BMS-819881 is a melaninconcentrating hormone receptor 1 (MCHR1) antagonist, which binds rat MCHR1 with a Ki of 7 nM. BMS-819881 also is selective and potent for CYP3A4 activity with an EC50 of 13 μM.
COX-2-IN-23 (compound A10) is a potent both AChE and HDAC inhibitor with IC50 values of 0.12 and 0.23 nM. COX-2-IN-23 exhibits antioxidant activity and metal chelating properties. COX-2-IN-23 can be used in alzheimer's disease research[1].
Oleoyl coenzyme A (Oleoyl-CoA) lithium is a thioester of oleic acid and coenzyme A. Oleoyl coenzyme A lithium has a role as an Escherichia coli metabolite and a mouse metabolite[1][2].
Galloylalbiflorin (6′-O-Galloylalbiflorin) is an androgen receptor (AR) antagonist (IC50=53.3 μM) and can be found in the roots of Paeonia lactiflora. Galloylalbiflorin shows anti-androgens activity[1].
Lp-PLA2-IN-9 (compound 17), a tetracyclic pyrimidinone compound, is a potent Lp-PLA2 inhibitor with a pIC50 of 10.1 for rhLp-PLA2. Lp-PLA2-IN-9 has the potential for neurodegenerative related diseases research[1].
Propargyl-PEG1-SS-alcohol is a cleavable 1 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
Secologanate is a natural secoiridoid glucoside found in Lonicerae Japonicae Caulis[1].
N-methyl-N'-methyl-O-(m-PEG4)-O'-(propargyl-PEG4)-Cy3 is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
ATN-224 is an oral Cu2+/Zn2+-superoxide dismutase 1 (SOD1) inhibitor. ATN-224 inhibits SOD1 activity in endothelial cells, an effect that is dose dependent with an IC50 of 17.5±3.7 nM.
Polygodial (Poligodial) is an antifungal potentiator[1]. Polygodial is a sesquiterpene with anti-hyperalgesic properties[2].
NMS-P715 analog is an inhibitor of MPS1, with an IC50 of 84 nM.
4',5-Dihydroxyflavone is a soybean LOX-1 and yeast α-Glucosidase inhibitor, with an Ki of 102.6 μM for soybean LOX-1 and an IC50 of 66 μM for yeast α-glucosidase.
Cbz-NH-PEG6-C2-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
FMK is a an irreversible RSK2 kinase inhibitor, that covalently modifies the C-terminal kinase domain of RSK.
LH-RH (7-10) is a tetrapeptide, one of major degradation products of luteinising-hormone releasing hormone (LHRH) via pituitary and hypothalamus. LH-RH (7-10) produced in macrophages, type I-like and type II pneumocytes[3].
Dibenzothiophene-d8 is the deuterium labeled Dibenzothiophene[1].
Vincristine sulfate is an antitumor vinca alkaloid which inhibits microtubule formation in mitotic spindle, resulting in an arrest of dividing cells at the metaphase stage. It binds to microtubule with a Ki of 85 nM.
IDH889 is an orally available, brain penetrant, allosteric and mutant specific inhibitor of isocitrate dehydrogenase 1 (IDH1). IDH889 has potent selectivity for IDH1 R132* mutations, with IC50s of 0.02 μM, 0.072 μM and 1.38 μM for IDH1R132H, IDH1R132C and IDH1wt, respectively. IDH889 shows potent cellular inhibition of R-2-hydroxyglutarate (2-HG) production with an IC50 of 0.014 μM[1].
CM03 is a G-quadruplex-binding compound that potently inhibits cell growth in PDAC cell lines (MIA PaCa-2 IC50=19 nM); CM03 shows >20-fold selectivity for MIA PaCa-2 compared to MCF-7 cells, also shows greater selectivity than MM41 relative to the non-oncogenic control fibroblasts; demonstrates anticancer activity in PDAC models, with a superior profile compared to gemcitabine.
9-Hydroxycalabaxanthone (Xanthone I) is a known xanthone isolated from Garcinia mangostana Linn. 9-Hydroxycalabaxanthone has quorum-sensing inhibitory, anti-microbial, and anti-malarial activities (IC50=1.2-1.5 µM)[1].
11-Azidoundecanoic acid is a click chemistry reagent containing an azide group. 11-Azidoundecanoic acid acts as a hydrophobic bioconjugation linker that can be further modified at the azido-position using Staudinger ligation or Click-chemistry. 11-Azidoundecanoic acid is substrate of lipoic acid ligase (LpIA) for labeling[1][2].
Propargyl-PEG5-amine is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Propargyl-PEG5-amine is a PEG-based PROTAC linker can be used in the synthesis of PROTACs[1].
NMI 8739 is a dopamine D2 autoreceptor agonist, which is an amine conjugate of the DHA carrier and the neurotransmitter dopamine.
Cyclodrine hydrochloride is a cholinergic (muscarinic, nicotinic) (mAChR and nAChR) receptor antagonist.
BMS-1166 is a potent PD-1/PD-L1 interaction inhibitor with an IC50 of 1.4 nM.
LY-3381916 is a potent, selective and brain penetrated inhibitor of IDO1 activity, binds to apo-IDO1 lacking heme rather than mature heme-bound IDO1[1].
Skullcapflavone I can be isolated from A. nallamalayana. Skullcapflavone I inhibits collagenase and elastase enzyme with IC50s of 106.74 μM and 186.70 μM. Skullcapflavone I has anticancer activities by down-regulating miR-23a[1].