WWL70 is a selective alpha/beta hydrolase domain 6 (ABHD6) inhibitor with an IC50 of 70 nM.
Brimonidine (UK 14304) is a full α2-adrenergic receptor (α2-AR) agonist.
4-Nitrophenyl 2-O-(β-L-Fucopyranosyl)-β-D-Galactopyranoside is a synthetic chromogenic substrate and can be used in the assay of α-fucosidases which hydrolyze the glycosidic linkage Fuc α1-2Gal. The assay is based on the sequential action of α-fucosidase and an exogenously added exo-β-d-galactosidase to release the easily measurable p-nitrophenol moiety[1].
β-Secretase Inhibitor II is a β-Secretase inhibitor. β-Secretase Inhibitor II is a simple tripeptide aldehyde (IC50=700 nM for inhibition of total Aβ and IC50=2.5 μM for Aβ1–42). β-Secretase Inhibitor II can be used for the research of Alzheimer's disease[1].
Stearoyl-L-carnitine chloride is an endogenous long-chain acylcarnitine. Stearoyl-L-carnitine chloride is a less potent inhibitor of GlyT2. Stearoyl-L-carnitine chloride inhibits glycine responses by 16.8% at concentrations up 3 μM[1][2].
JF646, SE (JF646, NHS), a red fluorescent dye, is supplied as an NHS ester for coupling to primary amine groups. JF646, SE is suitable for confocal fluorescent imaging, super resolution microscopy (SRM) techniques such as dSTORM (live and fixed cells) and STED imaging. JF646, SE is also suitable for flow cytometry.
Sanshool is a major component in Zanthoxylum bungeanum. Sanshool improves UVB-induced skin photodamage by targeting JAK2/STAT3-dependent autophagy[1].
Nω-Propyl-L-arginine hydrochloride (N-omega-Propyl-L-arginine hydrochloride) is a potent, competitive, and highly selective inhibitor of neuronal nitric oxide synthase (nNOS), with a Ki of 57 nM. Nω-Propyl-L-arginine hydrochloride displays a 149-fold selectivity for nNOS over endothelial NOS (eNOS)[1][2].
Ascr#2 is an ascaroside isolated from Caenorhabditis elegans, potently promotes dauer formation, and also acts as a potent male attractant combined with ascr#3 at low concentration[1].
Z-Glu-OtBu is a glutamic acid derivative[1].
Bis-PEG13-NHS ester is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
Datelliptium chloride is a DNA-intercalating agent derived from ellipticine, with anti-tumor activities.
Lanuginosine (Compound 12) is an AChE inhibitor (IC50: 10.9 μM). Lanuginosine inhibits Aβ aggregation. Lanuginosine can be used for research of Alzheimer’s disease[1].
Isocupressic acid ((+)-Isocupressic acid) is an abortifacient compound[1].
MNK1/2-IN-5 is a potent and selective MNK1/2 inhibitor as a therapeutic agent.
Elbasvir (MK-8742) is a hepatitis C virus nonstructural protein 5A (HCV NS5A) inhibitor with EC50s of 4, 3 and 3 nM against genotype 1a, 1b, and 2a, respectively.
P62-mediated mitophagy inducer is a mitophagy regulator which activates mitophagy without recruiting Parkin or collapsing ΔΨm and retains activity in cells devoid of a fully functional PINK1/Parkin pathway[1].
Cyprodime hydrochloride is a highly selective μ-opioid receptor antagonist with Ki values of 5.4 nM, 244.6 nM and 2187 nM for μ-, δ- and κ-opioid receptors, respectively. Cyprodime hydrochloride has anti-depressant-like effect[1][2].
Gestrinone (R2323) is a synthetic steroid hormone used to treat endometriosis. It inhibits leiomyoma cells with an IC50 of 43.67 μM.
Gly-Pro-AMC is a biological active peptide. (This is a fluorescent dipeptidylaminopeptidase IV substrate, Abs/Em=353/442 nm.)
Streptozocin is a potent DNA-methylating agent, with IC50s of 11.7, 904 and 1024 μg/mL in HL60, K562 and C1498 cells respectively.
ML243 is a selective small-molecule inhibitor of breast cancer stem cells. ML243 has 32-fold greater selective inhibition in the breast CSC-like cell line HMLE_shECad than the control cell line HMLE_shGFP[1].
Mal-NH-ethyl-SS-propionic acid is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
LX2343 is a BACE1 enzyme inhibitor with an IC50 value of 11.43±0.36 μM. LX2343 acts as a non-ATP competitive PI3K inhibitor with an IC50 of 15.99±3.23 μM. LX2343 stimulates autophagy in its promotion of Aβ clearance.
VAL-083 is an alkylating agent that creates N7 methylation on DNA, with antitumor activity.
(2-pyridyldithio)-PEG1-hydrazine is a cleavable 1 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
Rehmapicrogenin, isolated from the root of Rehmannia glutinosa, exhibits potent anti-inflammatory effect by inhibiting iNOS, COX-2 and IL-6[1].
CPI-637 is a potent and selective CBP/EP300 bromodomains inhibitor with IC50 of 0.03±0.01μM and 11.0±0.6 μM for CBP/EP300 and BRD4, respectively.IC50:0.03±0.01μM (CBP/EP300)[1]IC50:11.0±0.6 μM(BRD4)[1]CPI-637, which demonstrated substantial biochemical potency that was confirmed by isothermal titration calorimetry. A cocrystal structure of CPI-637 in the CBP bromodomain indicated that the compound recapitulated the key hydrogen bonding interactions observed with the parent compound, with the substituted indazole filling space above Pro1110 and the Pro/Arg cleft . As expected, CPI-637 was also potent against EP300, and its opposite enantiomer displayed a >200-fold loss in potency. The biochemical potency of CPI-637 translated well into cells (CBP BRET EC50 = 0.3 μM), and the compound demonstrated a >700-fold selectivity over the BET family of bromodomains (BRD4 IC50 = 11.0 ± 0.6 μM).CPI-637 was also highly selective against other bromodomains (detailed list in the Supporting Information), displaying substantial biochemical activity only against BRD9, which is acceptable, since inhibition of the BRD9 bromodomain has not been shown to produce a pronounced cellular phenotype . In a cellular assay, CPI-637 inhibits the expression of MYC, a transcription factor widely expressed in human cancer,with an EC50 of 0.60 μM, providing an orthogonal measure of the target engagement of the compound .The inactive enantiomer of CPI-637 displayed an EC50 in the same assay of >10 μM.[1]
2-Chloro-N6-methyl-2’-deoxyadenosine 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].
Volixibat (SHP626) is a highly selective, minimally absorbed, and competitive apical sodium-dependent bile acid transporter (ASBT) inhibitor. Volixibat has potential for treatment for non-alcoholic steatohepatitis (NASH)[1][2].