Boc-α-allyl-DL-Pro-OH is a proline derivative[1].
VH032-NH-CO-CH2-NHBoc is a Boc-modified VH032 (HY-120217) that acts as a ligand for VHL to recruit von Hippel-Lindau (VHL) proteins. VH032-NH-CO-CH2-NHBoc will remove the Boc protection under acidic conditions, and connect with the target protein ligand through a linker to form a PROTAC molecule, which is a key intermediate for the synthesis of PROTAC based on VHL ligand.
Ac-Gly-Ala-Lys(Ac)-AMC is a fluorogenic substrate for the determination of protease activity. Ac-Gly-Ala-Lys(Ac)-AMC undergoes hydrolysis and releases the fluorescent product 7-amino-4-methylcoumarin (AMC). AMC is fluorescent under UV light and can emit a fluorescent signal[1].
Methylamino-PEG1-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Flavipin is an aryl hydrocarbon receptor (Ahr) agonist that induces the expression of Ahr downstream genes in mouse CD4+ T cells and CD11b+ macrophages. Flavipin inhibits the stabilizing function of Arid5a on Il23a 3′UTR, a newly identified target mRNA[1]. Flavipin exhibits the DPPH free radical scavenging ability with IC50 value of 7.2 μM, and has potent α-glucosidase inhibition with IC50 value of 33.8 μM[2].
Lewis a trisaccharide (Lewis a) is a trisaccharide that has been found to be present in the glycan structures of spermatozoa. Lewis a trisaccharide also is a major component of the glycan structures on the surface of HL-60 cells[1].
2’-O-Acetyl-5’-O-(p-toluoyl)-3’-deoxy-3’-fluoro-5-methyluridine 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].
ERK-IN-3 is a potent and oral inhibitor of ERK. ERK-IN-3 inhibits ERK1/2 with low single-digit nM IC50 values. ERK-IN-3 has the potential to be used to study cancers driven by RAS mutations.[1].
PI3K/mTOR Inhibitor-1 is a potent, orally bioavailable dual PI3K/mTOR inhibitor with IC50s of 20/376/204/46 nM and 186 nM for PI3Kα/PI3Kβ/PI3Kγ/PI3Kδ and mTOR, respectively[1]. Antitumor activity[1].
MK-2295 (NGD-8243) is a TRPV1 antagonist. MK-2295 is an analgesic agent, and can be used for research of pain[1][2].
3-Cyanoumbelliferone is a coumarin derivative, acting as molecular probe and fluorescent dye. 3-Cyanoumbelliferone is also a macrophage migration inhibitory factor (MIF) tautomerase inhibitor with a Ki of 2.9 μM[1].
YH-306 is a candidate drug in preventing growth and metastasis of colorectal cancer by modulating FAK signalling pathway.
Leptomerine, an alkaloid from stems of Esenbeckia leiocarpa Engl. (Rutaceae) as potential treatment for Alzheimer Disease. Leptomerine inhibits acetyl cholinesterase (AChE) with an IC50 of 2.5 μM. Anticholinesterasic activity[1].
N6-Dimethylamino methylidene-2’-deoxyisoguanosine 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].
(R)-Zunsemetinib is the inactive isomer of Zunsemetinib (HY-139553), and can be used as an experimental control. Zunsemetinib (CDD-450) is an orally active and selective p38α mitogen-activated protein kinase-activated protein kinase 2 (MK2) pathway inhibitor. Zunsemetinib can be used for the research of immuno-inflammatory diseases[1].
Lugdunin is an antibiotic peptide. Lugdunin inhibits bacteria by dissipating their membrane potential. Lugdunin is active against Gram-positive bacteria, such as S. aureus, and reduces S. aureus skin and nasal colonization. Lugdunin induces LL-37 and CXCL8/MIP-2 in human keratinocytes and mouse skin[1].
ZSTK474 is an ATP-competitive pan-class I PI3K inhibitor with IC50s of16 nM, 44 nM, 4.6 nM and 49 nM for PΙ3Κα, PI3Kβ, PI3Kδ and PI3Kγ, respectively.
EP2 receptor antagonist-1 (compound 1) is a potent, reversible, and agonist dependent allosteric prostaglandin EP2 receptor antagonist. EP2 receptor antagonist-1 shows anti-inflammatory effects[1].
L-Biotin-NH-5MP is a biotin-conjugated 5-Methylene pyrrolone (5MP). 5-Methylene pyrrolones (5MPs) are thiol-specific, reversible bioconjugation reagents for cysteine-specific protein modification, that are commonly used for protein bioconjugation[1].
Kushenol W is a prenylated flavonoid that can be isolated from the root of Sophora flavescens. Kushenol W has antimicrobial effect, with a MIC of 10 μg/mL for Staphylococcus aureus[1].
(R)-N-Fmoc-2-(4'-pentenyl)glycine is a derivative of glycine, can be used for synthesis of compounds.
MUC1, mucin core is the region of the MUC1 mucin core. MUC1 is a type I transmembrane glycoprotein, and is overexpressed and aberrantly glycosylated in carcinoma cells. MUC1, mucin core protein binds to domain 1 of ICAM-1[1].
1,2-Dimyristoyl-sn-glycero-3-phospho-(1'-rac-glycerol)-d54 (sodium) is deuterium labeled 1,2-Dimyristoyl-sn-glycero-3-phospho-(1'-rac-glycerol) (sodium).
3,3’,5,5’-Tetramethylbenzidine(TMB) is a chromogenic substrate used in staining procedures in immunohistochemistry as well as being a visualising reagent used in enzyme-linked immunosorbent assays (ELISA).
A novel potent and selective TGF-βRI (ALK5) inhibitor with IC50 of 4.83 nM, dispalys >300-fold selectivity over p38α; decreases phosphorylated Smad2 levels and the nuclear translocation of Smad2 increased by TGF-β1, inhibits TGF-β1-induced epithelial-to-mesenchymal transition (EMT) and wound healing of NMuMG cells; inhibits metastasis to lung from breast tumours in xenografted mice.
SR10067 is a potent, selective and brain penetrant Rev-Erbα/β agonist, with IC50 values are 160 and 170 nM for Rev-Erbβ and Rev-Erbα, respectively. SR10067 has anxiolytic activity[1][2].
Eniluracil (5-Ethynyluracil), a uracil analogue and a mechanism-based irreversible inhibitor of dihydropyrimidine dehydrogenase (DPD), increases the oral bioavailability of 5-fluorouracil (5-FU) to 100%, facilitating uniform absorption and predictable toxicity[1].
4-Methylumbelliferyl butyrate (4-MUB) is a coumarin-based fluorogenic substrate used for the identification of M. catarrhalis C4- esterase. 4-Methylumbelliferyl butyrate can converse to the blue-emissive 4-methylumbelliferone (4-MU; HY-N0187)[1].
2-Undecanone is a volatile organic compound, which inhibits the DnaKJE-ClpB bichaperone dependent refolding of heat-inactivated bacterial luciferases. 2-Undecanone inhibits lung tumorigenesis[1][2].
Boc-bipiperidine-ethynylbenzoic acid is an Alkyl/ether-based PROTAC linker can be used in the synthesis of ARD-61[1].