Tricaprilin (Trioctanoin) is used in study for patients with mild to moderate Alzheimer's disease and has a role as an anticonvulsant and a plant metabolite[1][2].
hPGDS-IN-1 is a hPGDS inhibitor ,with IC50 of 12 nM in the Fluorescence Polarization Assay or the EIA assay.IC50 value: 12 nMTarget: hPGDSThe detailed information please refer to WO2011044307A1 and WO2010080563A2
UMP-morpholidate is an intermediate of pharmaceutical synthesis by coupling[1].
MK-4256 is a potent and selective SSTR3 antagonist with IC50s of 0.66 nM and 0.36 nM in human and mouse receptor binding assays, respectively.
4-Ethoxycoumarin is an antimicrobial[1].
SNDX-5613 is a potent and specific Menin-MLL inhibitor with a binding Ki of 0.149 nM and a cell based IC50 of 10-20 nM. SNDX-5613 can be used for the research of MLL-rearranged (MLL-r) acute leukemias, including acute lymphoblastic leukemia (ALL) and acute myeloid leukemia (AML)[1].
Tyk2-IN-5 (compound 6) is a highly potent, selective and orally active Tyk2 inhibitor and targets the JH2 domain, with a Ki of 0.086 nM for Tyk2 JH2 and an IC50 of 25 nM for IFNα. Highly effective in inhibiting IFNγ production in a rat pharmacodynamics model and fully efficacious in a rat adjuvant arthritis model[1].
Donepezil-d5 is deuterium labeled Donepezil. Donepezil (E2020 free base) is a specific and potent AChE inhibitor with IC50s of 8.12 nM and 11.6 nM for bovine AChE and human AChE, respectively[1].
Oxalic Acid-13C2 (disodium) is the 13C labeled Oxalic Acid disodium[1].
UBP618 is a GluN1/GluN2 receptors pan-inhibitor.
D-(-)-Norleucine is a leucine derivative[1].
(R)-(-)-α-Methylhistamine dihydrobromide is a potent and selective H3 histamine receptor agonist with a Kd of 50.3 nM[1][2]. (R)-(-)-α-Methylhistamine dihydrobromide can cross the blood-brain barrier, and can enhance memory retention, attenuates memory impairment in rats[3][4][5].
Maropitant is a neurokinin (NK1) receptor antagonist. IC50 value:Target: NK1 receptorMaropitant is the first NK1 receptor antagonist developed to treat and prevent emesis in dogs. Treatment with 1 mg/kg Maropitant citrate, significantly reduced the size of ulcerative dermatitis (UD) lesions in mice. Intravenous Maropitant decreased (p < 0.05) MAC by 16% (1.74 ± 0.17%). In contrast, epidural administration of either saline or Maropitant did not change (p > 0.05) the MAC (2.17 ± 0.34% and 1.92 ± 0.12%, respectively).
Propargyl-PEG3-phosphonic acid diethyl ester is a PEG-based PROTAC linker can be used in the synthesis of PROTACs[1].
2-(2-Ethoxyphenoxy)acetic acid-d5 is the deuterium labeled 2-(2-Ethoxyphenoxy)acetic acid[1].
GS87 is a highly specific and potent GSK3 inhibitor with IC50s of 415nM and 521nM for GSK3α and GSK3β, respectively. GS87 induces differentiation of acute myeloid leukemia (AML) cell lines by effectively activating GSK3-dependent signaling components including MAPK signaling. GS87 modulates key GSK3 target proteins involved in cell proliferation and differentiation more effectively than Lithium and SB415285 (SB). GS87 has the potential for acting as a differentiation agent for non-promyelocytic AML research[1].
Oxidopamine hydrobromide is a selective catecholaminergic neurotoxin, depletes brain catecholamine levels via uptake and accumulation by a transport mechanism specific to these neurons. In vitro: Oxidopamine hydrobromide-induced apoptosis of PC12 cells was initiated by superoxide generation followed by caspase cascade activation, which was associated with the suppressed Akt phosphorylation and increased p38 phosphorylation. It is likely that pCPT-cAMP prevented the Oxidopamine hydrobromide-induced apoptosis via activation of the PI3-kinase/Akt pathway without any effect on superoxide generation or mitochondrial membrane depolarization. [1]In vivo the presence of sulfhydryl antioxidants protected against neuronal degeneration in the striatum, which was particularly remarkable in the case of CySH and was attributed to its capacity to remove the H2O2 produced in the autoxidation of Oxidopamine hydrobromide.
5'-ODMT cEt m5U Phosphoramidite Amidite is a locked nucleic acid (LNA) analog. 5'-ODMT cEt m5U Phosphoramidite Amidite shows excellent safety and antisense activity[1][2].
Azido-PEG4-propargyl is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
4-Fluorophenoxyacetic acid (4FPA) induces parthenocarpy. 4-Fluorophenoxyacetic acid (4FPA) protects cereals from piercing-sucking insects and thereby increases rice yield in the field[1][2].
Tyrosinase-IN-17 (Compound 5b) is a lipophilic, skin-permeable, and non-cytotoxic Tyrosinase inhibitor (pIC50=4.99). Tyrosinase-IN-17 can be used for research on melanin-related diseases, such as melanoma, melanogenesis, etc[1].
2-Aminopurine-9-beta-D-(3’,5’-di-O-benzoyl-2’-deoxy-2’-fluoro)arabinoriboside 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].
o-Toluic acid (2-Methylbenzoic acid) is a benzoic acid substituted by a methyl group at position 2. O-Toluic acid plays a role as a xenobiotic metabolite.
Flucloxacillin sodium is a highly active antibiotic against Gram-positive and Gram-negative bacteria.
Y-9738 is a hypolipidemic agent.
Isogermafurenolide is a cytotoxic Terpenoids from the Wood of Vepris punctata from the Madagascar Rainforest[1].
Taniborbactam is a potent inhibitor of β-lactamase, with IC50s of <100 nM for SHV-5, KPC-2, VIM-2, and AmpC β-lactamase, and 0.1 to 1 μM for OXA-1 β-lactamase, used in the research of bacterial infections[1].
Raphin1 is an orally bioavailable, selective inhibitor of the regulatory phosphatase PPP1R15B (R15B). Raphin1 binds strongly to the R15B-PP1c holophosphatase (Kd=33 nM), and shows ~30-fold selective in binding R15B-PP1c over R15A-PP1c. Raphin1 crosses the blood-brain barrier, and reduces organismal and molecular deficits in a mouse model of a protein misfolding disease[1].
(Des-Ala3)-GHRP-2 is a biologically active peptide.
L-Threonolactone ((3R,4S)-3,4-Dihydroxyoxolan-2-one) 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].