Rottlerin, Inhibitor

Rottlerin

Cat. Num. AAA5755482

• Purity: 98.00%
• Synonyms: Rottlerin; Mallotoxin; NSC 56346; NSC 94525; inhibitor

• Purity/Purification: 98.00%
• Form/Format: Solid. Powder

• Solubility: DMSO: 2mg/mL (3.87mM) Need ultrasonic; (<1mg/ml refers to the product slightly soluble or insoluble)
• Formula: C30H28O8
• SMILES: O=C(C1=C2C(C=CC(C)(C)O2)=C(O)C(CC3=C(O)C(C)=C(O)C(C(C)=O)=C3O)=C1O)/C=C/C4=CC=CC=C4
• CAS Number: 82-08-6
• Target & IC50: PKCdelta: ic50 3uM (Porcine spleen); PKCalpha: ic50 30uM (baculovirus-infected Sf9 insect cells); PKCgamma: ic50 40uM (baculovirus-infected Sf9 insect cells); PKCbeta: ic50 42uM (baculovirus-infected Sf9 insect cells); PKCeta: ic50 82uM (baculovirus-infected Sf9 insect cells); PKCzeta: ic50 100uM (baculovirus-infected Sf9 insect cells); PKCepsilon: ic50 100uM (baculovirus-infected Sf9 insect cells); CKII: ic50 0uM (holoenzyme expressed in E Coli); PKA: ic50 78uM; CaM kinase III: ic50 5.3uM
• In Vitro: Rottlerin inhibits tumor cell proliferation and causes apoptosis through activation of caspase-3 and cleavage of the poly polymerase. Rottlerin (20mg/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 [3].
• Preparation and Storage: Store at -20 degree C for 3 years powder; -80 degree C for 2 years in solvent

Structure

Related Product Information for Rottlerin, inhibitor

Rottlerin is a natural product purified from Mallotus Philippinensis and is a specific PKC inhibitor (IC50: PKCdelta of 3-6uM, PKCalpha, beta, gamma of 30-42uM, PKCepsilon, eta, zeta of 80-100uM). Rottlerin causes apoptosis via caspase 3 activation.

Product Categories/Family for Rottlerin, inhibitor

Cytoskeletal Signaling; PKC

References

Gschwendt M, et al. Rottlerin, a novel protein kinase inhibitor. Biochem Biophys Res Commun. 1994 Feb 28;199(1):93-8.
Gschwendt M, et al. Rottlerin, a novel protein kinase inhibitor. Biochem Biophys Res Commun. 1994 Feb 28;199(1):93-8.
Valacchi G, et al. Rottlerin exhibits antiangiogenic effects in vitro. Chem Biol Drug Des. 2011 Jun;77(6):460-70.
Valacchi G, et al. Rottlerin exhibits antiangiogenic effects in vitro. Chem Biol Drug Des. 2011 Jun;77(6):460-70.
Minzhao Huang, et al. Rottlerin suppresses growth of human pancreatic tumors in nude mice, and pancreatic cancer cells isolated from KrasG12D mice. Cancer Letters 353 (2014) 32-40.
Minzhao Huang, et al. Rottlerin suppresses growth of human pancreatic tumors in nude mice, and pancreatic cancer cells isolated from KrasG12D mice. Cancer Letters 353 (2014) 32-40.