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PKC inhibitor
Antiestrogen with anti-cancer activity. Selective protein kinase C (PKC) inhibitor and induces PKC epsilon translocation. Induces apoptosis in estrogen receptor-negative human cancer cell lines.
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Product Details
| Alternative Name |
(Z)-2-[4-(1,2-Diphenyl-1-butenyl)phenoxy]-N,N-dimethyl-ethanamine . citrate |
|---|---|
| Appearance |
White to off-white powder. |
| CAS |
54965-24-1 |
| Couple Target |
PKC |
| Couple Type |
Inhibitor |
| Formula |
C26H29NO . C6H8O7 |
| Identity |
Determined by IR. |
| MI |
14: 9048 |
| MW |
371.5 . 192.1 |
| Purity |
≥99% (Assay) |
| RTECS |
KH2387000 |
| Solubility |
Soluble in methanol or ethanol; very slightly soluble in water or acetone. |
Handling & Storage
| Use/Stability |
As indicated on product label or CoA when stored as recommended. |
|---|---|
| Long Term Storage |
+4°C |
| Shipping |
Ambient Temperature |
| Regulatory Status |
RUO – Research Use Only |
|---|
- RORgt+ c-Maf+ Vg4+ gd T cells are generated in the adult thymus but do not reach the periphery: T. Yang, et al.; Cell Rep. 42, 113230 (2023), Abstract
- Progesterone limits the tumor-promoting effects of the beta-subunit of human chorionic gonadotropin via non-nuclear receptors: Sarkar, M., Sharma, H., et al.; iScience 25, 104527 (2022), Abstract
- Niche-mediated repair of airways is directed in an occupant-dependent manner: H. Lyu, et al.; Cell Rep. 41, 111863 (2022), Abstract
- Mitochondrial Dysfunction Leads to Cortical Under-Connectivity and Cognitive Impairment: Fernandez, A., Meechan, D. W., et al.; Neuron 102, 1127 (2019), Abstract
- Loss of the N-terminal methyltransferase NRMT1 increases sensitivity to DNA damage and promotes mammary oncogenesis: Bonsignore, L. A., Butler, J. S., et al.; Oncotarget 6, 12248 (2015), Abstract
- Is tamoxifen the Rosetta stone for breast cancer?: V.C. Jordan; J. Natl. Cancer Inst. 95, 338 (2003), Abstract
- Tamoxifen: a most unlikely pioneering medicine: V.C. Jordan; Nat. Rev. Drug Discov. 2, 205 (2003), Abstract
- Tamoxifen for prevention of breast cancer: R.J. Cersosimo; Ann. Pharmacother. 37, 268 (2003), Abstract
- Update on clinical role of tamoxifen: J.R. Benson and V. Pitsinis; Curr. Opin. Obstet. Gynecol. 15, 13 (2003), Abstract
- Pharmacodynamics of tamoxifen and its 4-hydroxy and N-desmethyl metabolites: activation of caspases and induction of apoptosis in rat mammary tumors and in human breast cancer cell lines: S. Mandlekar, et al.; Cancer Res. 60, 6601 (2000), Abstract — Full Text
- Activation of caspase-3 and c-Jun NH2-terminal kinase-1 signaling pathways in tamoxifen-induced apoptosis of human breast cancer cells: S. Mandlekar, et al.; Cancer Res. 60, 5995 (2000), Abstract — Full Text
- Effective tamoxifen therapy of breast cancer involves both antiproliferative and pro-apoptotic changes: D.A. Cameron, et al.; Eur. J. Cancer. 36, 845 (2000), Abstract
- Tamoxifen in the treatment of metastatic malignant melanoma: still a controversy? (Review): S. Toma, et al.; Int. J. Oncol. 15, 321 (1999), Abstract
- Tamoxifen induces oxidative stress and apoptosis in oestrogen receptor-negative human cancer cell lines: C.Ferlini et al.; Br. J. Cancer 79, 257 (1999), Abstract
- Activation of nitric oxide synthase is involved in tamoxifen-induced apoptosis of human erythroleukemia K562 cells: M. Maccarrone, et al.; FEBS Lett. 434, 421 (1998), Abstract
- Recent advances in understanding the molecular mechanisms of tamoxifen action: Z.Y. Friedman; Cancer Invest. 16, 391 (1998), Abstract
- Tamoxifen induces selective membrane association of protein kinase C epsilon in MCF-7 human breast cancer cells: Y. Lavie et al.; Int. J. Cancer. 77, 928 (1998), Abstract
- Antagonist effect of insulin-like growth factor I on protein kinase inhibitor-mediated apoptosis in human glioblastoma cells in association with bcl-2 and bcl-xL: S.A. Toms et al.; J. Neurosurg. 88, 884 (1998), Abstract
- Steroidal and nonsteroidal oestrogen antagonists in breast cancer: basic and clinical appraisal: R.E. Favoni & A. de Cupis; TIPS 19, 406 (1998), (Review), Abstract
- Genomic effects of tamoxifen: J.A. Kellen; Anticancer Res. 16, 3537 (1996), Abstract
- Tamoxifen: teaching an old drug new tricks?: D.J. Grainge & J.C. Metcalfe; Nat. Med. 2, 381 (1996), (Review), Abstract
- Protein kinase C inhibitors induce apoptosis in human malignant glioma cell lines: W.T. Couldwell, et al.; FEBS Lett. 345, 43 (1994), Abstract
- Signalling targets for anticancer drug development: G. Powis; TIPS 12, 188 (1991), (Review), Abstract
- Opposite effects of tamoxifen on in vitro protein kinase C activity and endogenous protein phosphorylation in intact MCF-7 cells: M. Issandou, et al.; Cancer Res. 50, 5845 (1990), Abstract
- Inhibition of protein kinase C by tamoxifen: C.A. O’Brian, et al.; Cancer Res. 45, 2462 (1985), Abstract
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