Alphabetical listing of all products

A - B - C - D - E - F - G - H - I - J - K - L - M - N - O - P - Q - R - S - T - U - V - W - X - Y - Z

Prices
  • 5 mg - 284 EUR
  • 25 mg - 1136 EUR
  • 100 mg - 3408 EUR

WAY-600

WAY-600 is a single digit nanomolar inhibitor of the mTOR kinases, with significant selectivity for these enzymes over phosphatidylinositol 3-kinase (PI3K) isofoms (>100-fold). Both in vivo and in vitro, this compound is differentiated from the rapalogs in that is blocks substrate phosphorylation by mTORC1 and mTORC2 induced by growth factors, amino acids, and hyperactive PI3K/AKT. Unlike the inhibitors of PI3K or dual-pan PI3K/mTOR inhibitors, BAY-600 achieved cellular inhibition of P-S6K1(T389) and P-AKT(S473) at significantly lower inhibitor concentrations than were required to reduce P-AKT(T308) activity (as judged by the PI3K-PDK1 readout), demonstrating its mTOR selectivity. WAY-600 inhibited the activity of proteins downstream of AKT and the proliferation of diverse cancer cell lines. These effects correlated with a strong G(1) cell cycle arrest in both rapamycin-sensitive and rapamycin-resistant cells, selective induction of apoptosis, repression of global protein synthesis, and down-regulation of angiogenic factors.

catalogue number: W089
synonyms:
CAS: 1062159-35-6
MW: 494.59 g/mol

References
Cancer Res. 2009 Aug 1;69(15):6232-40. PMID: 19584280

Prices
  • 5 mg - 84 EUR
  • 25 mg - 336 EUR
  • 100 mg - 1008 EUR

Wortmannin

Wortmannin is a fungal metabolite that has been shown to act as a selective inhibitor of phosphoinositide 3-kinases with IC50 values in low nanomolar range. It has been shown that wortmannin binds irreversibly in proximity to the substrate-binding site of PI3K. At higher concentrations, wortmannin inhibits also the ataxia telangiectasia gene (ATM)-related DNA-dependent protein kinase (DNA-PKcs).

catalogue number: W148
synonyms: KY12420
CAS: 19545-26-7
MW: 428.43 g/mol

References
Trends Biochem Sci. 1995 Aug;20(8):303-7. PMID: 7667888
Mol Cell Biol. 1996 Apr;16(4):1722-33. PMID: 8657148

Prices
  • 5 mg - 284 EUR
  • 25 mg - 1136 EUR
  • 100 mg - 3408 EUR

WYE-125132

WYE-125132 is a highly potent (subnanomolar), ATP-competitive, and specific mTOR kinase inhibitor, with an IC(50) of 0.19 nmol/L for mTOR and >5,000-fold selectivity for mTOR against the PI3Ks. WYE-132 inhibited mTORC1 and mTORC2 in diverse cancer models in vitro and in vivo. Importantly, WYE-132 inhibited the functioning of P-AKT(S473) and AKT without significantly reducing the steady-state level of the PI3K/PDK1 activity biomarker P-AKT(T308). Similar effects are induced by the genetic ablation of mTORC2, which suggests that mTORC plays a prominent and direct role in regulating AKT in cancer cells. Compared to the rapalog temsirolimus/CCI-779, WYE-132 is a significantly more potent inhibitor of cancer cell growth and survival, protein synthesis, cell growth, bioenergetic metabolism, and adaptation to hypoxia.

catalogue number: W091
synonyms: WYE-132
CAS: 1144068-46-1
MW: 519.6 g/mol

References
Cancer Res. 2010 Jan 15;70(2):621-31. PMID: 20068177
J Biol Chem. 2010 May 14;285(20):15380-92. PMID: 20233713

Prices
  • 5 mg - 194 EUR
  • 25 mg - 776 EUR
  • 100 mg - 2328 EUR

WZ3146

WZ3146 is an irreversible inhibitor of EGFR receptor kinase mutants carrying a mutation in an active site gatekeeper residue (T790M), which is detected in 50% of patients exhibiting resistance to gefitinib or erlotinib. WZ3146 is much less potent against wild-type EGFR kinase.

catalogue number: W092
synonyms:
CAS: 1214265-56-1
MW: 464.95 g/mol

References
Nature. 2009 Dec 24;462(7276):1070-4. PMID: 20033049

Prices
  • 5 mg - 194 EUR
  • 25 mg - 776 EUR
  • 100 mg - 2328 EUR

WZ8040

Like WZ3146, WZ8040 is an irreversible inhibitor of EGFR receptor kinase mutants carrying a mutation in an active site gatekeeper residue (T790M), which is detected in 50% of patients exhibiting resistance to gefitinib or erlotinib. WZ8040 is much less potent against wild-type EGFR kinase.

catalogue number: W093
synonyms:
CAS: 1214265-57-2
MW: 481.01 g/mol

References
Nature. 2009 Dec 24;462(7276):1070-4. PMID: 20033049