MA242 is a dual inhibitor of murine double minute 2 (MDM2) and nuclear factor of activated T cells 1 (NFAT1) for Pancreatic Cancer Therapy[1].
Macrostemonoside I is a furostanol saponin that can be isolated from Allium macrostemon[1].
2-Amino-2′-O-(2-methoxy-2-oxoethyl)adenosine is an adenosine analogue. Adenosine analogs mostly act as smooth muscle vasodilators and have also been shown to inhibit cancer progression. The popular products in this series are adenosine phosphate, Acadesine (HY-13417), Clofarabine (HY-A0005), Fludarabine phosphate (HY-B0028) and Vidarabine (HY-B0277)[1].
MK2-IN-5 is a Mk2 pseudosubstrate (Ki= 8 μM). MK2-IN-5 targets the protein interaction domain in the MAPK pathway. MK2-IN-5 inhibits HSP25 and HSP27 phosphorylation[1][2][3].
1-Oxo Ibuprofen (Ibuprofen EP impurity J) is a degradation product and a potential impurity in preparations of Ibuprofen. Ibuprofen is an anti-inflammatory inhibitor targeting COX-1 and COX-2 with IC50s of 13 μM and 370 μM, respectively[1][2].
Propargyl-PEG4-tetra-Ac-beta-D-galactose is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
CSF1R-IN-2 (compound 5) is an oral-active inhibitor of SRC, MET and c-FMS, with IC50 values of 0.12 nM, 0.14 nM and 0.76 nM for SRC, MET and c-FMS respectively[1].
Flibanserin is a novel multifunctional serotonin agonist and antagonist (MSAA) that improves sexual functioning in premenopausal women who suffer from reduced sexual interest and desire.IC50 value:Target: serotoninin vivo: The multifunctional serotonergic agent Flibanserin is both a serotonin 1A agonist and a serotonin 2A antagonist. Flibanserin theoretically improves sexual functioning by enhancing downstream release of dopamine and norepinephrine while reducing serotonin release in the brain circuits that mediate symptoms of reduced sexual interest and desire. Flibanserin, a new molecular entity for the treatment of hypoactive sexual desire disorder (HSDD) in premenopausal women. Flibanserin improves interest in and desire for sex by hypothetically targeting these circuits and causing the release of dopamine and norepinephrine while also reducing the release of serotonin. Flibanserin has demonstrated clinical efficacy in premenopausal women who have reduced interest in and desire for sex and has 2 principal pharmacologic actions in microcircuits: it is a full agonist at postsynaptic serotonin 5HT1A receptors and an antagonist at postsynaptic 5HT2A receptors.
4-Nitrobenzoic acid-d4 is the deuterium labeled 1-(5-(2-fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl)-N-methylmethanamine fumarate (Vonoprazan Impurity）[1].
Hederacolchiside A1, isolated from Pulsatilla chinensis, suppresses proliferation of tumor cells by inducing apoptosis through modulating PI3K/Akt/mTOR signaling pathway[1]. Hederacolchiside A1 has antischistosomal activity, affecting parasite viability both in vivo and in vitro[2].
Dibenzylamine-d10 is the deuterium labeled Dibenzylamine[1].
SIRT1/2/3-IN-1 (compound 10) is a highly potent, selective and cell permeable inhibitor of SIRT1, SIRT2 and SIRT3, with IC50s of 0.54, 0.253, and 0.72 μM respectively. SIRT1/2/3-IN-1 (compound 10) can be used for research of cancer[1].
Val-Arg-Pro-DL-Arg-Fluoromethylketone is a potent MALT1 inhibitor. Val-Arg-Pro-DL-Arg-Fluoromethylketone inhibits cell proliferation and migration. Val-Arg-Pro-DL-Arg-Fluoromethylketone shows anticancer activity[1].
lota-conotoxin RXIA is an agonist of voltage-gatedsodium channels (Nav1.2, 1.6, 1.7). Iota-conotoxin RXIAcan induce repetitive action potential and seizure in motor axons of frogsafter intracranial injection in mice [1].
22-Dehydroclerosterol is a compound that can be found in Morinda citrifolia L.[1].
Praeruptorin E is a main bioactive constituent of Peucedanum praeruptorum (also known as Bai-Hua Qian Hu). Praeruptorin C is a calcium antagonist with pD2′ value of 5.2[1].
Milnacipran-d5 (hydrochloride) is deuterium labeled Milnacipran (hydrochloride).
5Z-7-Oxozeaenol is a natural anti-protozoan compound from fungal origin, acting as a potent irreversible and selective inhibitor of TAK1 and VEGF-R2, with IC50s of 8 nM and 52 nM, respectively.
1,2-Dipalmitoyl-3-oleoylglycerol, a major P-containing triacylglycerol, can be found in palm oil, palm stearin, cocoa butter, and lard[1].
Prednisolone tebutate is a synthetic glucocorticoid used as an antiinflammatory and immunosuppressant.
Loureiriol is a homoisoflavonoid with weak anticancer effects[1].
CDDO-Im (CDDO-imidazolide) is an activator of Nrf2 and PPAR, with Kis of 232 and 344 nM for PPARα and PPARγ.
Glycerol phenylbutyrate is a sigma-2 (σ2) receptor ligand, with a pKi of 8.02.
Mequinol (4-Methoxyphenol) is one of bioactive components in Mercurialis spp. Mequinol is used for skin depigmentation[1]
Riboflavin phosphate sodium significantly increases in corneal biomechanical stiffness
VPC13163 is a potent androgen receptor (AR) BF3 inhibitor with an IC50 of 0.31 µM. VPC13163 has anticancer effects[1].
PF-3758309 hydrochloride is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (Kd= 2.7 nM; Ki=18.7 nM). PF-3758309 hydrochloride has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation[1][2][3].
MT-7716 hydrochloride (W-212393 hydrochloride) is a selective non-peptide nociceptin receptor (NOP) agonist and promising potential treatment drug for alcohol abuse and relapse prevention[1].
Antibacterial agent 72 displays the antibacterial activities by targeting the bacterial membrane.
Pantothenate kinase-IN-1 (Compound 1) is a pantothenate kinase (PANK) modulator with an IC50 of 0.51 µM against PANK3. Pantothenate kinase-IN-1 has a reasonable ligand efficiency (LipE = 2.8)[1].