>98%,Standard References

>98%,Standard References

>98%,Standard References

>98%,Standard References

>98%,Standard References

(±)-Bisoprolol hemifumarate is a selective β1-AR adrenergic antagonist. Possesses β1/β2 selectivity of approximately 100-fold and a Kd of 2-3 nM at the β1-AR (β1 receptor).

α-Amyloid Precursor Protein Modulator is a cell-permeable benzolactam derived PKC activator (Ki = 11.9 nM for PKCα) that efficiently enhances non-amyloidogenic α-processing of amyloid precursor protein (APP) even at 100 nM in human fibroblast AG06848.

VPS34 inhibitor 1 (Compound 19, PIK-III analogue) is a potent and selective inhibitor of VPS34 with an IC50 of 15 nM.

TAPI-2 inhibits ADAM8, 10, 12, and TACE with Ki values of 10, 3, 100, and 0.12 µM, respectively.

SW076956 is a small molecule that selectively disrupt Beclin 1/Bcl-2 binding as compared to Bax/Bcl-2 and Bim/Bcl-2 binding and induces autophagic flux at concentrations with minimal cytotoxicity.

PF-04447943 is a brain-permeable phosphodiesterase (PDE) inhibitor that is selective for PDE9A (IC50 = 12 nM) over other PDEs (IC50s = >940 nM) in enzymatic assays of second messenger hydrolysis.

Benzbromarone is a highly effective and well tolerated non-competitive inhibitor of xanthine oxidase, used as an uricosuric agent, used in the treatment of gout.

A potent, specific, orally active pan-PKD (protein kinase D) inhibitor with biochemical IC50 of 1, 2.5 and 2 nM for PKD1, 2, and 3 respectively.

Pradefovir mesylate is a good substrate for liver CYP3A4. Pradefovir is converted to 9-(2-phosphonylmethoxyethyl)adenine (PMEA) in human liver microsomes with a Km of 60 μM.

NRC-2694 is an epidermal growth factor receptor (EGFR) antagonist potentially for the treatment of solid tumors.

MLN8054 is a potent and selective inhibitor of Aurora A with IC50 of 4 nM; exhibits more than 40-fold selective for Aurora A than Aurora B.

ZLDI-8 (IAC-8) is a novel Notch signaling pathway inhibitor for Notch activating/cleaving enzyme ADAM-17, significantly decreases the level of NICD and accumulation of NICD in the nucleus; exhibits cytotoxic acitviity against MHCC97-H cells with IC50 of 5.32 uM, reduces the expression of pro-survival/anti-apoptosis regulators, Survivin and cIAP1/2, also increases the expression of epithelial marker E-Cadherin and reduces mesenchymal markers N-Cadherin and Vimentin in HCC cells; significantly disrupted the activity of Notch pathway in HCC cells and inhibits the epithelial-mesenchymal transition (EMT) process of HCC cells; ZLDI-8 treatment enhances the susceptibility of HCC cells to Sorafenib, Etoposide, and Paclitaxel both in vitro and in vivo.

Etanercept is a soluble TNF receptor fusion protein and acts as a TNF inhibitor.

Dulaglutide is a long-acting glucagon-like peptide 1 (GLP-1) receptor agonist that augments glucose-dependent insulin secretion for type 2 diabetes treatment.

Aflibercept (VEGF-Trap) is a recombinant chimeric soluble receptor containing structural elements from VEGF-R1 and VEGF-R2, and therefore it can scavenge VEGF-A and PlGF.

KDM5-C70 is the cell-permeable derivative of KDM5-C49, potent, selective and cell permeable KDM5 inhibitor with IC50 of 0.3, 0.3 and 0.58 uM for KDM5A, B and C, respectively.

TCH-165 is a specific small molecule modulator of proteasome assembly, regulates the dynamic equilibrium between the 20S and 26S proteasome complexes, favoring 20S-mediated protein degradation.

KDM5-IN-1 is a potent, selective and orally bioavailable KDM5 inhibitor with an IC50 of 15.1 nM.

AKI-603 is a novel small molecule Aurora A kinase inhibitor with IC50 of 12.3 nM, also inhibits Aurora B kinase activity to a less extent; disrupts normal spindle structure, and induces cell-cycle arrest; t; suppresses stem cell properties in breast cancer cells, and also suppresses the expression of self-renewal genes (β-catenin, c-Myc, Sox2, and Oct4); reduces xenograft tumor growth after intragastric administration.

Maribavir(GW257406X; BW1263W94; 1263W94) inhibits HCMV replication is by inhibition of an HCMV encoded protein kinase enzyme called UL97 or pUL97.

NVP-BHG712 is a specific EphB4 inhibitor with ED50 of 25 nM that discriminates between VEGFR and EphB4 inhibition; also shows activity against c-Raf, c-Src and c-Abl with IC50 of 0.395 μM, 1.266 μM and 1.667 μM, respectively.

U18666A, a cell permeable drug, is a cholesterol synthesis and transport inhibitor.

VPS34-IN1 is a potent and highly selective Vps34 inhibitor with IC50 of 25 nM invitro,which does not significantly inhibit the isoforms of class I as well as class II PI3Ks.

PT2399(PT=2399) is a novel HIF2α Antagonist.

Sulopenem, also known as CP-70429, is a potent beta-lactamase inhibitor.Sulopenem showed potent antibacterial activity against gram-positive and gram-negative bacteria except Pseudomonas aeruginosa and Xanthomonas maltophilia. CP-70,429 was stable to various types of beta-lactamases except for the enzyme from X. maltophilia and was 16- to 128-fold more active than the other compounds against beta-lactamase-producing strains of Enterobacter cloacae and Citrobacter freundii.