| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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Purity: ≥98%
Rottlerin (NSC-56346; NSC-94525), a naturally occuring compound isolated from Mallotus Philippinensis with the potential to be used as a chemotherapeutic agent for adrenocortical carcinoma, is a novel and specific protein kinase C (PKC) inhibitor with IC50 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. Rottlerin is an angiogenesis inhibitor and an inhibitor of protein kinase Cdelta (PKCdelta) and calmodulin kinase III.
| ln Vitro |
In primary HMVECs, rottlerin (20 μM, 2/6/24 hours) significantly and time-dependently lowers the levels of cyclin D-1 mRNA [2]. In HMVEC, rottlerin (20 μM) causes cell growth [2].
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| ln Vivo |
In Balb C nude mice, Rottlerin (20 mg/kg, once daily, five days a week, for six weeks) inhibits the growth of AsPC-1 pancreatic tumors without causing toxicity [3]. Rottlerin activates caspase-3 and cleaves poly(ADP-ribose) polymerase (PARP) to induce apoptosis.
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| Cell Assay |
Western blot analysis[2]
Cell Types: primary HMVEC (human microvascular endothelial cells). Tested Concentrations: 20μM. Incubation Duration: 2, 6, 24 hrs (hours). Experimental Results: Cyclin D-1 mRNA levels were Dramatically diminished in a time-dependent manner. After 2 hrs (hours) of treatment, mRNA levels diminished to 50% of control, after 6 hrs (hours) to approximately 40%, and after 24 hrs (hours) to 20%. A similar trend was observed at the protein level, with a decrease of approximately 50% after 2 hrs (hours), an 80% decrease after 6 hrs (hours), and a decrease to almost undetectable levels after 24 hrs (hours). Cell proliferation assay [2] Cell Types: primary HMVEC (human microvascular endothelial cells). Tested Concentrations: 20μM. Incubation Duration: 24/48 hrs (hours). Experimental Results: demonstrated strong growth inhibition, with thymidine incorporation diminished by approximately 75% and 80%, respectively, relative to control cells (DMSO 0.1%). |
| Animal Protocol |
Animal/Disease Models: Balb C nude mice (4-6 weeks old) were injected with AsPC-1 cells (2×106 cells mixed with Matrigel, 50:50 ratio) [3].
Doses: 0 or 20 mg/kg. Route of Administration: Administer one time/day, 5 days a week, for 6 weeks. Experimental Results: Inhibited the growth of AsPC-1 pancreatic tumors in Balb C nude mice and had no effect on the body weight of AsPC-1 tumor-bearing mice. |
| 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. |
| Molecular Formula |
C30H28O8
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|---|---|
| Molecular Weight |
516.53852
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| CAS # |
82-08-6
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| SMILES |
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
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| InChi Key |
DEZFNHCVIZBHBI-ZHACJKMWSA-N
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| 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+
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| 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
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| Synonyms |
Mallotoxin; NSC 56346; NSC 94525; NSC56346; NSC94525; Kamalin; NSC-56346; NSC-94525.
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~12.5 mg/mL (~24.20 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (2.42 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.25 mg/mL (2.42 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 22 mg/mL (42.59 mM) in 0.5% CMC-Na/saline water (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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