ds 2

Positive allosteric modulator of δ-subunit containing GABAA receptors

This peptide is a scrambled sequence of NADPH oxidase assembly peptide inhibitor gp91 ds-tat. It is used as a control peptide. It is two amino acid residues shorter at the N-terminus compared to the scrambled gp91 ds-tat.

(2S,4R)-DS89002333 is an enantiomer of DS89002333 and functions as an orally active PRKACA inhibitor, exhibiting an IC50 of 0.3 nM.

DS-2969 is a compound that has antibacterial activity.

DS21360717 is an effective oral tyrosine kinase inhibitor with anticancer activity and IC50 of 0.49 nM.

SC-26196 is an orally active inhibitor of Delta6 desaturase (D6D) with IC50 of 0.2 µM in a rat liver microsomal assay, with antiinflammatory properties.

DS28120313 is an oral inhibitor of hepcidin production (IC50: 0.093 μM).

DS-2248 is a potent Hsp90 inhbitor, currently in phase I trials.

DS20362725 is a selective estrogen-related receptor alpha (ERRα) agonist that binds to ERRα and enhances its transcriptional activity while preventing ERRα from binding to its repressor, receptor-interacting protein 140 (RIP140), commonly used in the study of metabolic disorders.

SB1-F-21 is an UCHL1 inhibitor.

KDS2010 is a potent, highly selective, and reversible MAO-B inhibitor which shows 12,500-fold selectivity over MAO-A. KDS2010 overcomes the disadvantages of the irreversible MAO-B inhibitor and significantly attenuates increased astrocytic GABA levels and astrogliosis, thereby enhancing synaptic transmission, and rescuing learning and memory impairments in APP/PS1 mice.

Tisolagiline (KDS2010) is a potent, highly selective and reversible MAO-B inhibitor with IC50=8 nM and oral activity for the treatment of Alzheimer's disease and obesity.

DS-22-inf-021, a neuraminidase (NA) inhibitor, exhibits antiviral activity against influenza viruses [1].

Valemetostat tosylate is a dual inhibitor of EZH1/2 and used in the research of relapsed/refractory peripheral T-cell lymphoma.

Valemetostat (DS-3201) is an EZH1/2 inhibitor that can be used to study relapsed/refractory peripheral T-cell lymphoma.

DS-1150b is an orally active GLUT4 activator. It exhibits the ability to activate GLUT4 transport, facilitating the translocation of GLUT4 to the cell membrane in skeletal muscle cells. In a Zucker obese rat model, DS-1150b demonstrated hypoglycemic effects and can be utilized for research in type 2 diabetes mellitus (T2DM).

Milademetan is a potent and selective MDM2 inhibitor. MDM2 inhibitor DS-3032b binds to and prevents the binding of MDM2 protein to the transcriptional activation domain of the tumor suppressor protein p53 upon oral administration. By preventing this MDM2-p53 interaction, the proteosome-mediated enzymatic degradation of p53 is inhibited and the transcriptional activity of p53 is restored. This results in the restoration of p53 signaling and leads to the p53-mediated induction of tumor cell apoptosis.

DS-7423 is a dual PI3K and mTOR inhibitor, with IC50 values of 15.6 nM and 34.9 nM for PI3Kα and mTOR, respectively, and exhibits anti-tumor activity[1][2]. It increases TP53 expression, the level of p-TP53 on Ser-46, and induces apoptosis-related TP53 target genes (TP53AIP1 and PUMA) in OCCC cells[1]. DS-7423 also inhibits other isoforms of class I PI3K with IC50 values of 1,143 nM for PI3Kβ, 249 nM for PI3Kγ, and 262 nM for PI3Kδ[2]. [1]. Katsutoshi Oda, et al. Characterization of TP53 and PI3K signaling pathways as molecular targets in gynecologic malignancies. J Obstet Gynaecol Res. 2016 Jul;42(7):757-62. [2]. Tomoko Kashiyama, et al. Antitumor activity and induction of TP53-dependent apoptosis toward ovarian clear cell adenocarcinoma by the dual PI3K/mTOR inhibitor DS-7423. PLoS One. 2014 Feb 4;9(2):e87220.

Milademetan (DS-3032) tosylate hydrate, an orally active and specific MDM2 inhibitor, is utilized in the study of acute myeloid leukemia (AML) and solid tumors. It induces G1 cell cycle arrest, senescence, and apoptosis, showcasing its therapeutic potential [1] [2].