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[CAS NO. 82-08-6] Rottlerin
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-18980 |
| Brand: | MCE |
| CAS: | 82-08-6 |
Overview
| MDL | MFCD00017361 |
|---|---|
| Molecular Weight | 516.54 |
| Molecular 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 |
3 Publications Citing Use of MCE
Summary
Rottlerin, a natural product purified from Mallotus Philippinensis , is a specific PKC inhibitor, with IC 50 values for PKCδ of 3-6 μM, PKCα ,β,γ of 30-42 μM, PKCε ,η,ζ of 80-100 μM. Rottlerin acts as a direct mitochondrial uncoupler, and stimulates autophagy by targeting a signaling cascade upstream of mTORC1 . Rottlerin induces apoptosis via caspase 3 activation [1] [2] [3] . Rottlerin inhibits HIV-1 integration and Rabies virus (RABV) infection [4] [5] .
IC50 & Target
|
PKCδ 3 μM (IC 50 , Porcine spleen) |
PKCα 30 μM (IC 50 , baculovirus-infected Sf9 insect cells) |
|
|
PKCγ 40 μM (IC 50 , baculovirus-infected Sf9 insect cells) |
PKCβ 42 μM (IC 50 , baculovirus-infected Sf9 insect cells) |
|
|
PKCη 82 μM (IC 50 , baculovirus-infected Sf9 insect cells) |
PKCζ 100 μM (IC 50 , baculovirus-infected Sf9 insect cells) |
|
|
PKCε 100 μM (IC 50 , baculovirus-infected Sf9 insect cells) |
CaM kinase III 5.3 μM (IC 50 , EF-2 kinase activity in cytosol of murine pancreas) |
|
|
CKII 30 μM (IC 50 , holoenzyme expressed in E.coli) |
PKA 78 μM (IC 50 , catalytic subunit from porcine heart) |
|
|
HIV-1
|
||
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
[2]
.
Rottlerin (20 μM) exhibits cell proliferation in HMVEC
[2]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Western Blot Analysis [2]
| Cell Line: | Primary HMVEC (Human Microvascular Endothelial Cell). |
| Concentration: | 20 μM. |
| Incubation Time: | 2, 6, 24 hours. |
| Result: | Dramatically decreased the cyclin D-1 mRNA levels in a time-dependent manner. After 2 h of treatment, the mRNA level was reduced to 50% of the control, to circa 40% after 6 h, and to 20% after 24 h. Consistently, a similar trend was observed in the protein levels, where the decrease was circa 50% after 2 h, 80% after 6 h, and to almost undetectable levels after 24 h. |
Cell Proliferation Assay [2]
| Cell Line: | Primary HMVEC (Human Microvascular Endothelial Cell). |
| Concentration: | 20 μM. |
| Incubation Time: | 24/48 hours. |
| Result: | Exhibited a strong growth inhibition, with a reduction in thymidine incorporation respect to the control cells (DMSO 0.1%) of circa 75% and 80%, respectively. |
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
[3]
.
Rottlerin inhibits tumor cell proliferation, and induces apoptosis through activation of caspase-3 and cleavage of poly(ADP-ribose) polymerase (PARP)
[3]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Balb C nude mice (4-6 weeks old) with AsPC-1 cells (2×10 6 cells mixed with Matrigel, 50:50 ratio) injection [3] . |
| Dosage: | 0 or 20 mg/kg. |
| Administration: | Gavage 5 days per week, once daily, for 6 weeks. |
| Result: | Inhibited AsPC-1 pancreatic tumor growth in Balb C nude mice and had no effect on the body weight of AsPC-1 tumor-bearing mice. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 12.5 mg/mL ( 24.20 mM ; ultrasonic and warming and heat to 60°C)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.9360 mL | 9.6798 mL | 19.3596 mL |
| 5 mM | 0.3872 mL | 1.9360 mL | 3.8719 mL |
| 10 mM | 0.1936 mL | 0.9680 mL | 1.9360 mL |
References
- [1] Gschwendt M, et al. Rottlerin, a novel protein kinase inhibitor. Biochem Biophys Res Commun. 1994 Feb 28;199(1):93-8.
- [2] Valacchi G, et al. Rottlerin exhibits antiangiogenic effects in vitro. Chem Biol Drug Des. 2011 Jun;77(6):460-70.
- [3] 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.
- [4] María Rosa López-Huertas, et al. Protein kinase Ctheta is a specific target for inhibition of the HIV type 1 replication in CD4+ T lymphocytes. J Biol Chem. 2011 Aug 5;286(31):27363-77.
- [5] Zoé Lama, et al. Kinase inhibitors tyrphostin 9 and rottlerin block early steps of rabies virus cycle. Antiviral Res. 2019 Aug;168:51-60.
Synonyms
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