Rottlerin

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.

Product information

CAS Number: 82-08-6

Molecular Weight: 516.54

Formula: C30H28O8

Synonym:

Kamalin

Mallotoxin

NSC 56346

Rottlerin

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

Smiles: CC(=O)C1C(O)=C(C)C(O)=C(CC2=C(O)C(=C3OC(C)(C)C=CC3=C2O)C(=O)/C=C/C2C=CC=CC=2)C=1O

InChiKey: DEZFNHCVIZBHBI-ZHACJKMWSA-N

InChi: 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+

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

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. 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.
2. 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.
3. 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.

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