Rottlerin


Catalog No. size PriceQuantity
M6789-2 2mg solid $90
M6789-10 10mg solid $365

Description

Cas:82-08-6

Product Information

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

 

Elemental Analysis: 

C, 69.76; H, 5.46; O, 24.78

 

Synonym:

 

Rottlerin

Kamalin

Mallotoxin

NSC 56346

NSC 94525.

 

Chemical Name:

(E)-1-(6-((3-Acetyl-2,4,6-trihydroxy-5-methylphenyl)methyl)-5,7-dihydroxy-2,2-dimethyl-2H-1-benzopyran-8-yl)-3-phenyl-2-propen-1-one

 

InChi Key:

DEZFNHCVIZBHBI-ZHACJKMWSA-N

 

InChi Code:

InChI=1S/C30H28O8/c1-15-24(33)19(27(36)22(16(2)31)25(15)34)14-20-26(35)18-12-13-30(3,4)38-29(18)23(28(20)37)21(32)11-10-17-8-6-5-7-9-17/h5-13,33-37H,14H2,1-4H3/b11-10+

 

Smiles Code:

CC1(C)C=CC2=C(O)C(CC3=C(C(C)=C(C(C(C)=O)=C3O)O)O)=C(O)C(C(/C=C/C4=CC=CC=C4)=O)=C2O1

 

Technical Data:

 

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

 

In Vitro:

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.

 

In Vivo:

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).

 

References

 

  1. 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.

 

  1. 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.

 

  1. 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.

 

  1. 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.

 

  1. 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.

 

Products are for research use only. Not for human use.

 

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