Murraol (CM-c2), a coumarin, can be isolated from the leaves of Madagascar pine cork (Apiaceae). Murraol has cyclooxygenase (COX) and lipoxygenase inhibitory properties and has an inhibitory effect on the growth of cancer cells[1].
SB-705498 is a potent, selective and orally bioavailable transient receptor potential vanilloid 1 (TRPV1) receptor antagonist with a pIC50 of 7.1.
Celite can be used as an excipient, such as filter media, adsorbent. Pharmaceutical excipients, or pharmaceutical auxiliaries, refer to other chemical substances used in the pharmaceutical process other than pharmaceutical ingredients. Pharmaceutical excipients generally refer to inactive ingredients in pharmaceutical preparations, which can improve the stability, solubility and processability of pharmaceutical preparations. Pharmaceutical excipients also affect the absorption, distribution, metabolism, and elimination (ADME) processes of co-administered drugs[1].
Radotinib-d6 is deuterium labeled Radotinib.
Dipentyl phthalate is an endocrine-disrupting phthalate plasticizer. Dipentyl phthalate increases AMPK phosphorylation and decreases AKT1 phosphorylation and SIRT1 levels. Dipentyl phthalate reduces adrenocorticotropic hormone levels. Dipentyl phthalate is a testicular toxicant[1].
JCN037 (JGK037) is non-covalent and BBB-penetrant EGFR tyrosine kinase inhibitor, with IC50 values of 2.49 nM, 3.95 nM, 4.48 nM for EGFR, p-wtEGFR and pEGFRvⅢ, respectively[1].
BAM-12P, an endogenous opioid peptide, is a novel pro-Met-enkephalin. BAM-12P can activate human κ-opioid receptor (hKOR) with an EC50 of 101 nM and a pEC50 of 6.99. BAM-12P is a ligand for CXCR7 with an EC50 of 175 nM[1][2][3].
PIPES (1,4-Piperazinediethanesulfonic acid) disodium is an important component of PIPES buffer agent used in biochemistry[1].
EC-17 (disodium salt) is a folate receptor alpha (FRα) targeting contrast agent with fluorescent properties in the visible light spectrum. The peak excitation and emission wavelengths of EC-17 are 470/520 nm.
5-HT3 antagonist 2 is a 5-HT3 receptor antagonist.
Mahanimbidine is a terpenoid alkaloid. Mahanimbidine can be isolated from the leaves and stem skins of the Murraya koenigii Spreng[1][2].
AZA1 is a potent dual inhibitor of Rac1 and Cdc42. AZA1 induces prostate cancer cells apoptosis and inhibits prostate cancer cells proliferation, migration and invasion[1][2].
SCH900776 is a potent, selective and oral inhibitor of checkpoint kinase1 (Chk1) with an IC50 of 3 nM. It shows 50- and 500-fold selectivity over CDK2 andChk2, respectively.
Fluorescein-6-isothiocyanate is a fluorescent isomeric haptenic probes with Kds of 8.74, 2.72 and 1.88 for N-Acetyl-L-Lysine, normal mouse IgG and 4-4-20, respectively[1].
FR260010 free base is a selective 5-HT2C receptor antagonist, with a Ki value of 1.1 nM[1].
Ro 04-6790 is a potent, competitive and selective 5-HT6 receptor antagonist with pKi values of 7.26, 7.35 for rat and human 5-HT6 receptors, respectively. Ro 04-6790 has no affinity at other receptors[1].
SP 600125, negative control (SPM1) is an alkyl derivative of pyrazoloanthrone, which can be used as a negative control for SP600125 (HY-12041)[1].
Procyanidin C2 is a phenol glycoside derived from Fagopyrum dibotrys (D. Don) Hara[1].
Echinatin is a chalcone isolated from the Chinese herbal medicine Gancao with hepatoprotective and anti-inflammatory effects. Echinatin may undergo an electron transfer (ET) and a proton transfer (PT) to cause the antioxidant action in aqueous solution[1]. Echinatin can be quickly absorbed and eliminated and extensively distributed with an absolute bioavailability of approximately 6.81% in Rat[2].
Leojaponin (compound 2 ) is a labdane diterpene. Leojaponin can be isolated from the EtOH extract of the herb Leonurus japonicus[1].
RN-1734 is selective antagonist of the TRPV4 channel, completely antagonizes 4αPDD-mediated activation of TRPV4 with comparable, low micromolar IC50values for all three species (hTRPV4: IC50 = 2.3 μM, mTRPV4: IC50 = 5.9 μM, rTRPV4: IC50 = 3.2 μM).IC50 value: 2.3 μM (hTRPV4), 5.9 μM (mTRPV4), IC50 = 3.2 μM (rTRPV4) Target: TRPV4in vitro: RN-1734 completely inhibits both ligand- and hypotonicity-activated TRPV4. In addition, RN-1734 is selective for TRPV4 in a TRP selectivity panel including TRPV1, TRPV3 and TRPM8, and could thus be a valuable pharmacological probe for TRPV4 studies. [1]
An E3 ligase ligand-linker conjugate for PROTAC.
Hematoporphyrin (Hematoporphyrin IX) is a substrate for affinity chromatography of heme-binding proteins.
N-Acryloyl-1-pyrenebutylamine is a potent fluorescent derivatization agent. N-Acryloyl-1-pyrenebutylamine combines with an alkyl-acrylamide side-chain to give fluorescence function on the polymer.[1][2].
Neochamaejasmine A is a biflavonoid that can be isolated from the roots of Stellera chamaejasme L.. Neochamaejasmine A inhibits proliferation, induces cell cycle arrest and Apoptosis in tumor cells. Neochamaejasmine A can be used in the research of cancers such as prostate cancer, hepatoma cancer[1][2].
Metronidazole is a nitroimidazole antibiotic medication used particularly for anaerobic bacteria and protozoa.Target: Antibacterial; AntiparasiticMetronidazole is a nitroimidazole antibiotic medication used particularly for anaerobic bacteria and protozoa. Metronidazole is an antibiotic, amebicide, and antiprotozoal.[1] It is the drug of choice for first episodes of mild-to-moderate Clostridium difficile infection [2]. Metronidazole, taken up by diffusion, is selectively absorbed by anaerobic bacteria and sensitive protozoa. Once taken up by anaerobes, it is non-enzymatically reduced by reacting with reduced ferredoxin, which is generated by pyruvate oxido-reductase. Many of the reduced nitroso intermediates will form sulfinamides and thioether linkages with cysteine-bearing enzymes, thereby deactivating these critical enzymes. As many as 150 separate enzymes are affected.In addition or alternatively, the metronidazole metabolites are taken up into bacterial DNA, and form unstable molecules. This function only occurs when metronidazole is partially reduced, and because this reduction usually happens only in anaerobic cells, it has relatively little effect upon human cells or aerobic bacteria.[3]
CDK5-IN-3 (compound 11) is a potent and selective CDK5 inhibitor, with IC50s of 0.6 nM and 18 nM for CDK5/p25 and CDK2/CycA, respectively. CDK5-IN-3 can be used for the research of autosomal dominant polycystic kidney disease (ADPKD)[1].
(±)-1-Hexadecanoyl-3-chloropropane-dd5-diol is the deuterium labeled (±)-1-Hexadecanoyl-3-chloropropane-diol[1].
Mal-C6-amine (TFA) is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Zilpaterol-d7 is a deuterium labeled Zilpaterol. Zilpaterol is a β-adrenergic receptor agonist that putatively, through activation of protein kinase A, increases protein synthesis in skeletal muscle fibers as well as reduces lipogenesis and increases lipolysis in adipose tissues. Formulations containing Zilpaterol have been used to increase lean body weight and improve feed efficiency in commercial beef cattle.