T2017

U-104 (NSC-213841) is an effective carbonic anhydrase (CA) inhibitor for CA IX( Ki=45.1 nM) and CA XII(Ki=4.5 nM).

TTT20171 is an SDHC inhibitor that demonstrates nanomolar-level inhibition of CII; however, it shows limited efficacy within cellular environments. In cell assays, the most responsive cells, 22Rv1 prostate cancer cells, exhibit an IC50 of 5.4 µM, which significantly exceeds both the suggested usage concentration of 2 µM and the chemical probe quality standard of 1 µM.

Tetrahexyldecyl ascorbate (BV-OSC) is a lipophilic precursor of ascorbic acid, a more stable and permeable form of vitamin C. It is a potent anti-photo-aging and anti-hyperpigmentation antioxidant that inhibits MMP enzyme activity.

MG-T-19, a TIM-3 inhibitor (KD=0.26 μM), significantly inhibited the interaction of TIM-3 with PtdSer, CEACAM1, and Gal-9, and increased the production of TNF-α and IFN-γ in PBMCs, which reactivated the tumor-attacking ability of T cells.

VAV1 degrader-2 (Example 176) is a molecular gel degrader (DC50=4.41 nM) that targets VAV 1 for the study of inflammatory and autoimmune diseases.

MGD-4 is an orally active, Cereblon (CRBN)-dependent degrader of IKAROS proteins that demonstrates dose-dependent degradation of IKZF1 (DC50=67.2 nM), IKZF2 (DC50=918.2 nM), and IKZF3 (DC50=95.8 nM). The compound effectively inhibits the growth of multiple myeloma.

Dioleyl phosphatidylserine is a phospholipid that can activate PKC-γ (Protein Kinase C-gamma) when the Ca2+ concentration is below 0.5 μM, specifically at a concentration of 100 μM.

Ofirnoflastum (Ofirnoflast) is a selective serine/threonine-protein kinase Nek7 inhibitor that exerts potent anti-inflammatory effects by suppressing Nek7-dependent NLRP3 inflammasome activation, reducing caspase-1 cleavage, IL-1β and IL-18 secretion, and pyroptotic cell death in vitro, while significantly attenuating cytokine production and tissue injury in animal models of acute and chronic inflammation, supporting its therapeutic potential in autoimmune and inflammatory diseases.

STAT3-IN-36 (compound 11g) is a tritarget inhibitor that selectively targets LRPPRC, STAT3, and CDK1, exhibiting potent anticancer activity. This compound binds to LRPPRC, STAT3, and CDK1, demonstrating more effective anticancer effects than those of TMF or Capecitabine. Additionally, STAT3-IN-36 exhibits an IC50 value of 1.8 μM in HGC27 cells.

VU6043653 is an effective, selective, and blood-brain barrier-permeable negative allosteric modulator of the metabotropic glutamate receptor subtype 5 (mGlu5), with an IC50 value of 325 nM against h mGlu5.

SJ1008066 is a MAGE-A11 inhibitor with an IC50 of 0.13 μM. It binds to the MAGE homology domain (MHD) and disrupts the MAGE-A11:PCF11 interaction.

FGFR-IN-16 (compound 7N) is a potent inhibitor of FGFR1, FGFR2, and FGFR4, exhibiting IC50 values of 8 nM, 4 nM, and 3.8 nM respectively. It plays a crucial role in cancer research.

E3 Ligase Ligand-Linker Conjugate 135 is a critical intermediate in the synthesis of the complete PROTAC molecule pan-KRAS degrader 5, comprising a conjugate of E3 ligase ligand and linker.

Pan-KRAS degrader 4 (compound 69) is a cereblon-based PROTAC KRAS degrader exhibiting anticancer activity with a DC50 value of less than 100 nM.

Kyotorphin is a Morphine-like dipeptide.

Desmethylflunitrazepam (Norflunitrazepam) is a benzodiazepine derivative and an active metabolite of Flunitrazepam.

BTK-IN-39 (0204) is a PROTAC target protein ligand employed in the synthesis of PROTAC BTK Degrader-11.

EGF Rligand-11, a target protein ligand for EGFR, is utilized in the synthesis of PROTAC MS154.

Kyotorphin acetate is an endogenous peptide with analgesia activity and can be used as a biomarker of Alzheimer disease.

Noradrenaline tartrate is an effective adrenergic receptor agonist that activates α1, α2, and β1 receptors. It is a precursor of epinephrine and serves as the principal neurotransmitter of most postganglionic sympathetic fibers and the diffuse projection system in the brain originating from the locus coeruleus, and can be used to establish cardiomyopathy models.

AMG580 is a selective PDE10A antagonist exhibiting sub-nanomolar affinity towards PDE10A in rats, primates, and humans. It is utilized in research as a non-invasive radiotracer.

AGH-107 is a highly selective 5-HT7 receptor agonist that can cross the blood-brain barrier, featuring a Ki value of 6 nM and an EC50 value of 19 nM. Demonstrating high selectivity for central nervous system targets, AGH-107 also exhibits high metabolic stability and low toxicity in HEK-293 and HepG2 cell cultures.

PROTAC BTK Degrader-11 is a PROTAC degrader that targets and degrades BTK with a DC50 of 1.7 nM. It is utilized in oncological research.

Ionizable Lipid 4 is an ionizable cationic lipid that forms as a product of the rearrangement of cationic lipid CA-lipid 5 under hydrogen peroxide induction.