Novel Enrichable and MS-Cleavable Cross-linker to Define Protein-Protein Interactions by Mass Spectrometry

Snail/HDAC-IN-1 is a potent Snail/HDAC dual target inhibitor. Snail/HDAC-IN-1 displays potent inhibitory activity against HDAC1 with an IC50 of 0.405 μM and potent inhibition against Snail with a Kd of 0.18 μM. Snail/HDAC-IN-1 increases histone H4 acetylation in HCT-116 cells and decreases the expression of Snail protein to induce cell apoptosis.

YE-120 is an agonist of G protein-coupled receptor 35 (GPR35).

FiVe1 is a vimentin binding small molecule that promotes vimentin disorganization and phosphorylation during metaphase, causes mitotic catastrophe, multinucleation, and the loss of stemness in cancer cells.

Senexin C is a novel potent, selective and orally bioavailable CDK8/19 inhibitor with Kd of 1.4 and 2.9 nM for CDK8/CycC and CDK19/CycC, respectively.Senexin C inhibits CDK8/CycC with IC50 of 3.6 nM, shows high selectivity against other HDAC isoforms.Senexin C is more metabolically stable and provides a more sustained inhibition of CDK8/19-dependent cellular gene expression when compared with the prototype inhibitor Senexin B.Senexin C inhibits MV4-11 leukemia growth in a systemic in vivo model with good tolerability.

Diclofensine(Ro-8-4650) is a potent inhibitor of monoamine reuptake, blocking the uptake of dopamine, noradrenaline, and serotonin by rat brain synaptosomes with IC50 values of 0.74, 2.3, and 3.7 nM, respectively.

Blue fluorescent amino acid, exhibiting blue fluorescence (λ max ~ 405 nm) with a high quantum yield and long lifetime

RO6806051 (compound12) is a potent dual fatty acid binding protein 4 and 5 (FABP4 and FABP5) inhibitor with good selectivity and absorption, distribution, metabolism and excretion (eADME) properties.

Aurachin D is an antibiotic. Aurachin D inhibits Gram-positive bacteria and a few funguses. Aurachin D blocks NADH oxidation in beef heart submitochondrial particles.

PAFAH inhibitor P11 (P11) is a potent, selective platelet-activating factor acetylhydrolases PAFAH1b2 and PAFAH1b3 inhibitor with IC50 of 40 nM and 900 nM respectively.

Inflachromene (ICM) is a microglial inhibitor with anti-inflammatory effects, directly binds high mobility group protein 1 (HMGB1) and HMGB2 and reduces their cytoplasmic accumulation in microglial cells.

Befiradol (F13640, NLX 112) is a highly potent, selective 5-HT1A receptor agonist with Ki of 2.7 nM.

GSK1059865 is a potent orexin 1 receptor antagonist.

ZINC20451377 is a small molecule that binds to hepatitis B surface antigen (HBsAg) with high affinity (Kd=65.3 nM), reduces HBsAg levels and HBV virion secretion in cell culture model for HBV.

Sultopride hydrochloride (LIN-1418 hydrochloride) is a selective antagonist of dopamine D2 receptor.

TL4-12 is a potent MAP4K2 (GCK) inhibitor that inhibits IL-1 and TGFβ-induced p38 MAPK phosphorylation, in vitro.

TZ9 is a novel inhibitor of Rad6 ubiquitin conjugating enzyme(E2 enzyme); inhibits MDA-MB-231 cell proliferation with IC50 of ~6 uM.

Dibenzo[a,i]pyrene is a polycyclic aromatic hydrocarbon (PAH) with potent carcinogenic activity. Dibenzo[a,i]pyrene was shown to induce DNA adduction, tumorigenicity as well as Ki-ras oncogene mutations in strain A/J mouse lung. Dibenzo[a,i]pyrene has been shown to be present in cigarette smoke condensate and in automobile exhaust gas in small quantities.

R121919 is a potent small-molecule CRF1 receptor antagonist with a Ki of 2 to 5 nM for the CRF1 receptor and over 1000-fold weaker activity at the CRF2 receptor, CRF-binding protein, or 70 other receptor types.

Rilmenidine hemifumarate, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine hemifumarate is an alpha 2-adrenoceptor agonist. Rilmenidine hemifumarate induces autophagy. Rilmenidine hemifumarate acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na+/H+ antiport. Rilmenidine hemifumarate modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells .

Novel enhancer of endothelial NO synthase (eNOS)

HuR inhibitor KH-3 is a small molecule, selective inhibitior of HuR function with Ki of 0.83 and 0.72 uM in FP and AlphaLISA assays, respectively.KH-3 potently inhibits breast cancer cell growth in vitro and in vivo.KH-3 inhibits breast cancer cell invasion in vitro as well as delays initiation of lung colonies and improves mouse survival in an experimental metastasis model in vivo.KH-3 suppresses breast cancer cell invasion by disrupting HuR-FOXQ1 mRNA interaction.Inhibition of HuR with KH-3 yielded a significant reduced in the progression of pathological cardiac hypertrophy in a transverse aortic constriction model.

ML353 (VU0478006) is a highly potent, selective, MPEP-site silent allosteric modulator of mGlu5 receptor with with sub-100 nM affinity.

K145 is a selective, substrate-competitive and orally active sphingosine kinase-2 (SphK2) inhibitor with an IC50 of 4.3 µM and a Ki of 6.4 µM in biochemical assays.

4-APC hydrobromide is a highly sensitive and selective derivatization agent for aldehydes. 4-APC hydrobromide possesses an aniline moiety for a fast selective reaction with aliphatic aldehydes as well as a quaternary ammonium group for improved MS sensitivity. 4-APC hydrobromide allows highly sensitive and selective MS detection of aldehydes.

Avexitide (Exendin (9-39)) is a specific and competitive antagonist of glucagon-like peptide-1 (GLP-1) receptor.

20-O-Acetylingenol-3-angelate is a diterpene ester that has been found in E. peplus and a derivative of ingenol-3-angelate

AP1510 is a potent cell-permeable ligand for human FKBP12. AP1510 regulates protein-protein interactions through dimerization.

L557-0155 is a small molecule inhibitor of VSIG-8, prevents VSIG-8 binding to VISTA, promotes cytokine production and cell proliferation in PBMCs and suppresses melanoma growth.

Tivozanib (AV-951, KRN-951) is a potent and selective VEGFR inhibitor for VEGFR1/2/3 with IC50 of 0.21 nM/0.16 nM/0.24 nM, and also inhibits PDGFR and c-Kit, low activity observed against FGFR-1, Flt3, c-Met EGFR and IGF-1R.