Deoxycholic acid sodium salt is specifically responsible for activating the G protein-coupled bile acid receptor TGR5 that stimulates brown adipose tissue (BAT) thermogenic activity.
(S,R,S)-AHPC-Me-decanedioic acid is an E3 ligase ligand-linker conjugate that can be used in the synthesis of PROTACs.
Methyl (R)-2-amino-3-(o-tolyl)propanoate is a phenylalanine derivative[1].
Ganoderic acid T is a natural product that can be found in ganoderma lucidum[1].
7-(2-Deoxy-β-D-erythro-pentofuranosyl)-7H-pyrrolo[2,3-d]pyrimidine 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].
Sulfo-NHS-Biotin (sodium) stongly label single SDS-2ME soluble cuticular protein[1].
Euphol is a tetracyclic triterpene alcohol isolated from the sap of Euphorbia tirucalli with anti-mutagenic, anti-inflammatory and immunomodulatory effects, orally active. Euphol inhibits the monoacylglycerol lipase (MGL) activity via a reversible mechanism (IC50=315 nM). MGL inhibition in the periphery modulates the endocannabinoid system to block the development of inflammatory pain[1].
C13-112-tri-tail is a cationic lipid-like compound containing a polar amino alcohol head group, three hydrophobic carbon-13 tails, and a PEG2 linker. C13-112-tri-tail can be formulated into a lipid nanoparticle (LNP).
RB-OPD (NO-red) is a o-phenylenediamine (OPD)-locked rhodamine nitric oxide (NO) fluorescent probe with great sensitivity and selectivity (λex=550 nm, λem=590 nm)[1].
Capmatinib (INC280; INCB28060) dihydrochloride hydrate is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC50=0.13 nM). Capmatinib dihydrochloride hydrate can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib dihydrochloride hydrate potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib dihydrochloride hydrate is largely metabolized by CYP3A4 and aldehyde oxidase[1][2][3].
Kemptide, 5-FAM labeled is a biological active peptide. (Kemptide is a phosphate acceptor peptide that serves as a synthetic substrate for PKA (Km = 16 μM). The corresponding fluorescent and biotinylated peptides are also proven to be good substrates for PKA. 5-FAM labeled HY-P0248)
Roflumilast N-oxide is a PDE type 4 inhibitor.
Cap-dependent endonuclease-IN-1 is an orally active cap-dependent endonuclease inhibitor with high potency. Cap-dependent endonuclease-IN-1 can be used for the research of influenza[1][2].
Renin substrate, angiotensinogen (1-14), rat is a biological active peptide. (This peptide is derived from rat angiotensinogen amino acid residues 1-14. It is a synthetic renin substrate.)
Garenoxacin-d4 (BMS284756-d4) is the deuterium labeled Garenoxacin. Garenoxacin (BMS284756) is a quinolone antibiotic for the treatment of Gram-positive and Gram-negative bacterial infections[1][2].
Calmodulin Binding Peptide 1 is a high affinity (pM) CaM-binding peptide derived from smooth muscle myosin light-chain kinase (MLCK peptide), which strongly inhibits IP3-induced Ca2+ release [1].
MC1742 is a potent HDAC inhibitor, with IC50s of 0.1 μM, 0.11 μM, 0.02 μM, 0.007 μM, 0.61 μM, 0.04 μM and 0.1 μM for HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, HDAC10 and HDAC11, respectively. MC1742 can increase acetyl-H3 and acetyl-tubulin levels and inhibits cancer stem cells growth. MC1742 can induce growth arrest, apoptosis, and differentiation in sarcoma CSC[1].
Heparan sulfate, a complex and linear polysaccharide, exists as part of glycoproteins named heparan sulfate proteoglycans, which are expressed abundantly on the cell surface and in the extracellular matrix.
2’-Deoxy-N6-cyclopentyladenosine 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].
Mal-amido-PEG12-NHS ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
HER2-IN-8 is a HER-2 inhibitor extracted from patent WO2021179274A1 compound 107. HER2-IN-8 can be used for the research of cancer and inflammation[1].
BRM/BRG1 ATP Inhibitor-4 is a BRG1/BRM inhibitor. BRM/BRG1 ATP Inhibitor-4 can be used for the research of cancers and BAF complex-related disorders[1].
Gefapixant is an orally active P2X3 receptor (P2X3R) antagonist with IC 50s of ~30 nM versus recombinant hP2X3 homotrimers and 100-250 nM at hP2X2/3 heterotrimeric receptors.
Secalonic acid D is a toxic compound against tumor cells. Secalonic acid D can be isolated from the metabolites of Aspergillus aculeatus. Secalonic acid D activates GSK3-β, and degrades β-catenin. Thus, Secalonic acid D down-regulates c-Myc expression, arrests cell cycle at G1 phase, induces cell apoptosis[1][2].
Pradefovir mesylate is a good substrate for liver CYP3A4. Pradefovir is converted to 9-(2-phosphonylmethoxyethyl)adenine (PMEA) in human liver microsomes with a Km of 60 μM.
LY3027788 hydrochloride, a diester analog of LY3020371 which is an mGlu2/3 receptor antagonist, is a potent and orally active prodrug of LY3020371. LY3027788 hydrochloride has antidepressant efficacy[1][2].
(E)-2-Decenoic acid is an interesting fatty acid isolated from royal jelly secretions of honey bees.
Teriparatide is a PHT agonist, with an IC50 of 2 nM in HEK293 cells. Sequence: Ser-Val-Ser-Glu-Ile-Gln-Leu-Met-His-Asn-Leu-Gly-Lys-His-Leu-Asn-Ser-Met-Glu-Arg-Val-Glu-Trp-Leu-Arg-Lys-Lys-Leu-Gln-Asp-Val-His-Asn-Phe.
Arabelline is a natural glycoside that can be isolated from Haplophyllum suaveolens[1].
Alniditan (Alnitidan) dihydrochloride is a potent 5-HT1B and 5-HT1D receptors agonist, with IC50s of 1.7 nM and 1.3 nM for h5-HT1B and h5-HT1D receptors in HEK 293 cells, respectively. Alniditan dihydrochloride has migraine-preventive effects[1][2].