11β-HSD1-IN-7 (compound c10a) is a 11β‑HSD1 inhibitor with an IC50 value of 1.9 μM for human 11β‑HSD1. 11β-HSD1-IN-7 can be used for the research of diabetes and cognitive decline[1].
10-Gingerol is a major pungent constituent in the ginger oleoresin from fresh rhizome, with anti-inflammatory, antioxidant and anti-proliferative activities. 10-Gingerol inhibits the proliferation of MDA-MB-231 tumor cell line with an IC50 of 12.1 μM[1][2].
PROTAC FKBP Degrader-3 is a PROTAC that comprises a FKBP ligand binding group, a linker and an VHL binding group. PROTAC FKBP Degrader-3 is a potent FKBP degrader[1].
BS-181 dihydrochloride is a potent and selective CDK7 inhibitor (IC50=21 nM) than Seliciclib (HY-30237). BS-181 is also against CDK2, CDK5 and CDK9 with IC50 values of 880 nM, 3000 nM and 4200 nM, respectively (fails to block CDK1, 4 and 6). BS-181 dihydrochloride inhibits a panel of cancer cells growth (IC50=11.5 μM-37.3 μM) and induces cell apoptosis. BS-181 dihydrochloride has the potential for the research of cancer therapy[1][2].
Uridine triacetate (Tri-O-acetyl uridine) is an orally active prodrug of Uridine. Uridine triacetate (Tri-O-acetyl uridine) is lipophilic, is quickly absorbed in the gut, and is rapidly deacetylated in the circulation to yield free uridine. Uridine triacetate (Tri-O-acetyl uridine) is uesd for the prevention and treatment of life-threatening 5-fluorouracil and capecitabine toxicity. Uridine triacetate (Tri-O-acetyl uridine) delivers high concentrations of uridine, which competes with toxic 5-FU metabolites[1][2].
Sibiricose A5 is an oligosaccharide ester isolated from Polygalae Radix with potent antioxidant activity[1][2].
Coprine is a mycotoxin isolated from Coprinopsis atramentaria. Coprine is an acetaldehyde dehydrogenase inhibitor that causes the buildup of acetaldehyde, causing the alcohol flushing reaction[1].
Cyclorasin 9A5 is an 11-residue cell-permeable cyclic peptide that orthosterically inhibits the Ras-Raf protein interaction with an IC50 of 120 nM[1].
A potent, selective, brain permeable, orally available glycine transporter-1 (GlyT1) inhibitor with IC50 of 92 nM (rat GlyT1), 50-fold selectivity over GlyT2; shows minimal affinity for many other receptors except for μ-opioid receptors (IC50=1.83 uM); inhibits ex vivo [(3)H]-glycine uptake in mouse cortical homogenate, improves cognition in animal models of cognitive impairment in schizophrenia and Alzheimer's disease. Schizophrenia Phase 1 Discontinued
trans-2-Undecenoic acid ((E)-2-Undecenoic acid) is an α,β-unsaturated carboxylic acid and is characterized by acid dimers. The corresponding dimers are connected via intermolecular hydrogen bonds of the carboxylic groups C=O···H-O[1].
Fradafiban is a nonpeptide platelet glycoprotein IIb/IIIa antagonist, which binds to the human platelet GP IIb/IIIa complex with a Kd value of 148 nM.
CGP-53153 is a steroidal inhibitor of 5 alpha reductase with IC50s of 36 and 262 nM in rat and human prostatic tissue, respectively.
[Gln8]-C517 (LH-RH), chicken is an avian hypothalamic peptide, which stimulates release of gonadotropins from anterior pituitary, thus regulating reproductive functions.
SU3327 is a potent, selective and substrate-competitive JNK inhibitor with an IC50 of 0.7 μM. SU3327 also inhibits protein-protein interactions between JNK and JNK Interacting Protein (JIP) with an IC50 of 239 nM. SU3327 shows less active against p38α and Akt kinase[1][2].
Linalool oxide is a secondary metabolite in elongating wheat plants with antinociceptive and anticonvulsant effects. Linalool oxide shows anxiolytic activity[1][2][3].
Elamipretide TFA (MTP-131 TFA; RX-31 TFA; SS-31 TFA) is a cardiolipin peroxidase inhibitor and mitochondria-targeting peptide[1].
BRK inhibitor P21d hydrochloride is a potent breast tumor kinase (BRK/PTK6) inhibitor with an IC50 of 30 nM. BRK inhibitor P21d hydrochloride inhibits p-SAM68 with an IC50 of 52 nM. BRK inhibitor P21d hydrochloride can be used to evaluate the in vivo activity of BRK inhibitors in xenograft breast tumor models[1].
Alectinib-d6 is deuterium labeled Alectinib. Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively[1]. Alectinib demonstrates effective central nervous system (CNS) penetration[2].
Dehydro-α-lapachone can be isolated from the methanol extract of stems of Catalpa ovata G Don. Dehydro-α-lapachone inhibits mycelial growth of Botrytis cinerea with IC50 value 0.41 mg/L[1].
(S)-(-)-Citronellal ((-)-Citronellal) is a monoterpenoid compound found in Corymbia citriodora and Cymbopogon nardus essential oils[1][2].
Malacidin B is a macrocyclic lipopeptide antibiotic that shows antibacterial activity in a calcium-dependent manner[1][2].
GB-6 is a short linear peptide that targets the gastrin releasing peptide receptor (GRPR). GRPR is overexpressed in pancreatic cancer. Based on the tumor selectivity and tumor-specific accumulation properties of GB-6, GB-6 labeled with near infrared (NIR) fluorescent dyes or radionuclide netium-99m (99mTc) can be used as a high-contrast imaging probe. GB-6 has excellent in vivo stability, with tumor to pancreatic and intestinal fluorescence signal ratios of 5.2 and 6.3, respectively, in SW199 0 subcutaneous xenograft models. GB-6 can rapidly target tumors and accurately delineate tumor boundaries, which has broad application prospects[1].
N-Benzyl-2-methylpropan-2-amine-d9 is the deuterium labeled N-Benzyl-2-methylpropan-2-amine[1].
TVB-3664 is an orally available, reversible, potent, selective and highly bioavailable fatty acid synthase (FASN) inhibitor, with IC50 values of 18 nM and 12 nM for human and mouse cell palmitate synthesis, respectively. TVB-3664 significantly reduces tubulin palmitoylation and mRNA expression[1][2].
Amyloid β-Protein (1-12) is a biologically active peptide.
Fmoc-Asn(Trt)-Ser(psi(Me,Me)pro)-OH is a dipeptide.
Diacetamide-d7 is the deuterium labeled Diacetamide[1].
Cinperene is an atropine-like drug which can block pilocarpine-induced lacrimation and salivation.
Dihydrodehydrodiconiferyl alcohol 9-Oglucoside can be extracted from G. mangostana L[1].
BMS-753426 is a potent and orally bioavailable antagonist of CCR2.