Rottlerin is an angiogenesis inhibitor and an inhibitor of protein kinase Cdelta (PKCdelta) and calmodulin kinase III. Rottlerin as a novel chemotherapy agent for adrenocortical carcinoma. Rottlerin induces cyclooxygenase-2 upregulation through an ATF4 and reactive oxygen species-independent pathway in HEI-OC1 cells. Rottlerin exerts its anti-tumor activity through inhibition of Skp2 in breast cancer cells. Rottlerin suppresses growth of human pancreatic tumors in nude mice, and pancreatic cancer cells isolated from Kras(G12D) mice.
Chemical Formula: C30H28O8
Exact Mass: 516.1784
Molecular Weight: 516.546
C, 69.76; H, 5.46; O, 24.78
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
Rottlerin (20 μM, 2/6/24 hours) dramatically decreases the cyclin D-1 mRNA levels in a time-dependent manner in primary HMVEC.
Rottlerin (20 μM) exhibits cell proliferation in HMVEC.
Rottlerin (20 mg/kg, gavage 5 days per week, once daily, for 6 weeks) inhibits AsPC-1 pancreatic tumor growth in Balb C nude mice with no toxicity.
Rottlerin inhibits tumor cell proliferation, and induces apoptosis through activation of caspase-3 and cleavage of poly(ADP-ribose) polymerase (PARP).
- Woo SM, Lee WK, Min KJ, Kim DE, Park SH, Nam SI, Kwon TK. Rottlerin induces cyclooxygenase-2 upregulation through an ATF4 and reactive oxygen species-independent pathway in HEI-OC1 cells. Mol Med Rep. 2016 Jul;14(1):845-50. doi: 10.3892/mmr.2016.5320. Epub 2016 May 20. PubMed PMID: 27222046.
- Mischitelli M, Jemaà M, Almasry M, Faggio C, Lang F. Stimulation of Suicidal Erythrocyte Death by Rottlerin. Cell Physiol Biochem. 2016;40(3-4):558-566. Epub 2016 Nov 25. PubMed PMID: 27889758.
- Liao TY, Tzeng WY, Wu HH, Cherng CG, Wang CY, Hu SS, Yu L. Rottlerin impairs the formation and maintenance of psychostimulant-supported memory. Psychopharmacology (Berl). 2016 Apr;233(8):1455-65. doi: 10.1007/s00213-016-4251-8. Epub 2016 Mar 10. PubMed PMID: 26960698.
- Zhu Y, Wang M, Zhao X, Zhang L, Wu Y, Wang B, Hu W. Rottlerin as a novel chemotherapy agent for adrenocortical carcinoma. Oncotarget. 2017 Apr 4;8(14):22825-22834. doi: 10.18632/oncotarget.15221. PubMed PMID: 28423559; PubMed Central PMCID: PMC5410265.
- Yin X, Zhang Y, Su J, Hou Y, Wang L, Ye X, Zhao Z, Zhou X, Li Y, Wang Z. Rottlerin exerts its anti-tumor activity through inhibition of Skp2 in breast cancer cells. Oncotarget. 2016 Oct 11;7(41):66512-66524. doi: 10.18632/oncotarget.11614. PubMed PMID: 27582552; PubMed Central PMCID: PMC5341817.
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