w5

W-5 hydrochloride (N-(6-Aminohexyl)-1-naphthalenesulfonamide HCl) is a potent calmodulin antagonist.

Rac1 Inhibitor W56 acetate(1095179-01-3 free base) is a peptide comprising residues 45-60 of the guanine nucleotide exchange factor (GEF) recognition/activation site of Rac1. Rac1 Inhibitor W56 acetate(1095179-01-3 free base) selectively inhibits Rac1 interaction with Rac1-specific GEFs TrioN, GEF-H1 and Tiam1.

NVP-AEW541 (AEW541), a potent inhibitor of IGF-1R(IC50=150 nM) and InsR(IC50=140 nM), exhibits excellent efficiency and specificity for IGF-1R in a cell-based assay.

GW590735 is an effective and selective PPARα agonist with an EC50 of 4 nM on PPARα and at least 500-fold selectivity versus PPARδ and PPARγ. GW590735 can be used in dyslipidemia studies.

GW590735 is a potent and selective agonist of PPARα with an EC50 value of 4 nM for the expression a GAL4-responsive reporter gene and at least 500-fold selectivity versus PPARγ and PPARδ. GW590735 significantly increased HDL cholesterol, decreased LDL and VLDL cholesterol, and significantly reduced triglycerides. Maximal increases in HDL cholesterol were 37%, 53%, and 84% with fenofibrate, torcetrapib, and GW590735, respectively.

DW532 is one of simplified analogues of hematoxylin that has shown broad-spectrum inhibition on tyrosine kinases and in vitro anti-cancer activities. DW532 inhibited EGFR and VEGFR2 in vitro kinase activity (the IC50 values were 4.9 and 5.5 μmol/L, respectively), and suppressed their downstream signaling. DW532 dose-dependently inhibited tubulin polymerization via direct binding to tubulin, thus disrupting the mitotic spindle assembly and leading to abnormal cell division. In a panel of human cancer cells, DW532 (1 and 10 μmol/L) induced G2/M phase arrest and cell apoptosis, which subsequently resulted in cytotoxicity. Knockdown of BubR1 or Mps1, the two core proteins of the spindle assembly checkpoint dramatically decreased DW532-induced cell cycle arrest in MDA-MB-468 cells. Moreover, treatment with DW532 potently and dose-dependently suppressed angiogenesis in vitro and in vivo. ( Acta Pharmacol Sin. 2014 Jul;35(7):916-28.)

AEW541, also known as NVP-AEW541, is a novel, potent IGF-IR kinase inhibitor. NVP-AEW541 is capable of distinguishing between the IGF-IR (IC50 = 0.086 microM) and the closely related InsR (IC50 = 2.3 microM) in cells. NVP- AEW541 abrogates IGF-I-mediated survival and colony formation in soft agar at concentrations that are consistent with inhibition of IGF-IR autophosphorylation. Note: AEW541 has a Cis-configuration on the cyclobutane ring. Its CAS# is 475489-16-8. Many vendors and Sc-finder scholar made mistake - AEW541 was mistakenly listed as CAS#475488-34-7, the trans-isomer of AEW541. The correct structure of AEW541 can be confirmed from Joel Slade, et al (from Novartis), Org. Process Res. Dev. 2007, 11, 5, 825–835.

m-PEG-OH (MW5000) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

BDW568, a prodrug of BDW-OH, serves as a stimulator of interferon genes (STING) agonist. This compound effectively induces STING transcriptional activity, evidenced by a reporter assay in THP-1 cells, with an EC50 value of 7.6 µM. Furthermore, at a concentration of 50 µM, BDW568 prompts phosphorylation of TANK-binding kinase 1 (TBK1) and IFN regulatory factor 3 (IRF3) within THP-1 cells, showcasing its biochemical activity in cellular signaling pathways.

Rac1 Inhibitor W56 is a peptide consisting of residues 45-60 of the guanine nucleotide exchange factor (GEF) recognition activation site of Rac1. It selectively inhibits Rac1 interaction with Rac1-specific GEFs TrioN, GEF-H1, and Tiam1.

PW507 is a potent, blood-brain barrier penetrable, and selective sigma 1 receptor (S1R) antagonist with a Ki value of 7.5 nM against human S1R. It exhibits lower binding affinity for S2R and hERG. This compound is utilized in the study of painful diabetic neuropathy (PDN).

GW568377A is an inhibitor of Mer Kinase and EGFR.

GW549390X is a dual inhibitor targeting both Fluc and VEGFR2, with IC50 values of 0.26 μM and 1.2 μM, respectively. This compound binds to the ATP pocket of FLuc via the aniline side chain, functioning as an ATP-competitive inhibitor of Fluc. It serves as a protein kinase inhibitor across ATP-dependent and -independent luciferases, potentially affecting Fluc reporter assays [1].

Rac1 Inhibitor W56 TFA, a peptide comprised of residues 45-60 of Rac1, selectively obstructs Rac1's interaction with the guanine nucleotide exchange factors TrioN, GEF-H1, and Tiam [1].

HDAC6-IN-37 (compound W5), an HDAC6 inhibitor, exhibits neuroprotective properties. It effectively restores the morphology of hippocampal neurons and diminishes the expression of Aβ, Tau, and p-Tau proteins in the hippocampus of AD rats. Additionally, it prevents the formation of senile plaques and neurofibrillary tangles. Consequently, HDAC6-IN-37 ameliorates the symptoms in the Aβ Cu 2+ -induced AD rat model, regulates oxidative stress, and restores balance to neurotransmitter levels in brain tissue [1].

m-PEG-OH (MW 2000) is a PEG-based linker for PROTACs, facilitating the connection of two essential ligands to form PROTAC molecules, thereby enabling selective protein degradation through the ubiquitin-proteasome system within cells.