Prodrug of MRS4738, dramatically reducing lung inflammation in a mouse asthma model

Negative control for MRK-740

Negative control for MLi-2

Negative control for MF-094

TH10785 is a small-molecule activator that binds to the active site of 8-oxo guanine DNA glycosylase 1 (OGG1) and enables the protein to completely cleave the damaged DNA strand, which results in an overall increased repair of oxidative DNA damage.

NCDM-32B is a novel potent and selective KDM4 inhibitor, impairing viability and transforming phenotypes of basal breast cancer.

Iclepertin (BI-425809) is a potent, selective and orally active glycine transporter 1 (GlyT1) inhibitor. Iclepertin is inactive against GlyT2. Iclepertin can be used for Alzheimer disease and schizophrenia research.

Tryptolinamide (TLAM) is a small-molecule compound that activates mitochondrial respiration in cybrids generated from patient-derived mitochondria and fibroblasts from patient-derived iPSCs, inhibits phosphofructokinase-1 (PFK1) with an ATP-uncompetitive

VX-984 (M 9831) is a potent, selective inhibitor of DNA-PK with IC50 of 88±64 nM for inhibition of DNA-PKcs autophosphorylation (Ser2056) in A549 lung cancer cells, with good selectivity versus other PI3K family members..

AZD5305 is a potent, selective and oral active PARP inhibitor. AZD5305 is a highly potent inhibitor of PARP1, with significant PARP1-DNA trapping activity, no PARP2-activity, nor binding activity to any other members of the PARP family. AZD5305 has excellent secondary pharmacology and physicochemical properties as well as high oral bioavailability in preclinical species.

γ-AA peptide P6 (Cyclic γ-AA P6) is a potent activator of E6 associated protein (E6AP). γ-AA peptide P6 can stimulate the self-ubiquitination of E6AP and E6AP-catalyzed substrate ubiquitination in reconstituted reactions in vitro. γ-AA peptide P6 can also enhance the ubiquitination of E6AP substrates in the cell and accelerate their degradation by the proteasome.

MCC7840 sodium, a sulfonylurea, is a potent and selective inhibitor of NLRP3 inflammasome, with an IC50 of <100 nM. MCC7840 sodium can be used for the research of inflammatory diseases.

F7H is a Frizzled receptor FZD7 antagonist (IC50: 1.25 μM). Frizzled receptors (FZDs) influence Wnt signaling, mediating embryonic development and tissue homeostasis. F7H is a potent ligand for the FZD7 transmembrane domain (TMD).

YM-344031 is a potent, selective, brain-penetrable CCR3 antagonist with binding IC50 of 3.0 nM, inhibits ligand-induced Ca(2+) flux with IC50 of 5.4 nM.

cyclo-CRVLIR is a cyclic peptide that binds selectively to p110α RAS binding domain (p110α-RBD) with ITC Kd of 3 uM, blocks p110α/RAS interaction in vitro and KRAS cancer cell lines.

Novel RBP4 antagonist with good in vitro potency and selectivity and optimal rodent pharmacokinetic (PK) and pharmacodynamic (PD) characteristics

6-Diazo-5-oxo-L-nor-Leucine (DON) is a glutamine analog that inhibits glutaminases (Ki = 6 µM) and other glutamine-utilizing enzymes, including cytidine triphosphate synthase (CTPS), which uses glutamine in the synthesis of CTP.1,2,3 DON is commonly used in cells or tissues but its use in whole animals is limited by its teratogenicity.

IK930 (compound I-32) is a potent and orally active TEAD inhibitor with an EC50 value of <0.1 µM.

PLX5622 is the HCl salt form of PLX-5622, which has better water solubility.PLX-5622 is a highly selective brain-penetrant CSF1R inhibitor (IC50=0.016 µM; Ki=5.9 nM) allowing for extended and specific microglial elimination, preceding and during pathology development.

PLX-5622 hemifumarate is a highly selective brain penetrant and orally active CSF1R inhibitor (IC50=0.016 µM; Ki=5.9 nM). PLX5622 hemifumarate allows for extended and specific microglial elimination, preceding and during pathology development. PLX5622 hemifumarate demonstrates desirable PK properties in varies animals.

TT-10 is a novel multifaceted fluorinated compound with promising features of CM proliferative, antioxidant, and antiapoptotic activities in vitro.

CI-976 (PD 128042) is a potent, selective, orally bioavailable inhibitor of ACAT-1 (Acetyl-CoA acetyltransferase 1) with IC50 of 73 nM.

PCC0208017 is a microtubule affinity regulating kinases (MARK3/MARK4) inhibitor with IC50s of 1.8 and 2.01 nM, respectively. PCC0208017 has much lower inhibitory activity against MARK1 and MARK2, with IC50s of 31.4 and 33.7 nM, respectively. PCC0208017 suppresses glioma progression in vitro and in vivo. PCC0208017 disrupts microtubule dynamics and induces G2/M phase cell cycle arrest and cell apoptosis. PCC0208017 demonstrates robust antitumor activity in vivo and displays good BBB permeability.

tert-butyl (8-aminooctyl)carbamate can be used as a PROTAC linker in the synthesis of PROTACs. tert-butyl (8-aminooctyl)carbamate is an alkane chain with terminal amine and Boc-protected amino groups. Amine group is reactive with carboxylic acids, activated NHS esters, carbonyls (ketone, aldehyde) etc. The Boc group can be deprotected under mild acidic conditions to form the free amine.

Isolithocholic acid (β-Lithocholic acid) is an isomer of Lithocholic acid. Isolithocholic acid, a bile acid, is formed by microbial metabolism of Lithocholic acid or Lithocholic acid 3α-sulfate.

A sphingosine 1-phosphate (S1PR) receptor agonist

GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. GSK778 phenocopies the effects of pan-BET inhibitors in cancer models.

BTA-EG4, acts as an amyloid-binding small molecule that promotes dendritic spine density and cognitive function in wild-type mice.

Shield-1 is a cell-permeable FKBP ligand that is designed to protect an otherwise unstable protein domain from degradation; binds tightly to FKBP, induces rapid and processive degradation of the LID domain.

Nrf2-Activator is a potent Nrf-2 activator.