Rottlerin
Rottlerin
CAS: 82-08-6
Molecular Formula: C30H28O8
Rottlerin - Names and Identifiers
Rottlerin - Physico-chemical Properties
| Molecular Formula | C30H28O8 |
| Molar Mass | 516.54 |
| Density | 1.2051 (rough estimate) |
| Melting Point | 200 °C |
| Boling Point | 521.39°C (rough estimate) |
| Solubility | Soluble in DMSO (up to 50 mg/ml). |
| Appearance | Powder |
| Color | Orange to brown |
| pKa | 6.92±0.40(Predicted) |
| Storage Condition | 2-8°C |
| Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 1 month. |
| Refractive Index | 1.4900 (estimate) |
| In vitro study | 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. Western Blot Analysis 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 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 study | 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). 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. 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. |
Rottlerin - Risk and Safety
| Hazard Symbols | Xn - Harmful |
| Risk Codes | R20/21/22 - Harmful by inhalation, in contact with skin and if swallowed. R22 - Harmful if swallowed |
| Safety Description | S36/37 - Wear suitable protective clothing and gloves. S24/25 - Avoid contact with skin and eyes. |
| WGK Germany | 3 |
| RTECS | AM6913800 |
| HS Code | 29329990 |
Rottlerin - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.936 ml | 9.68 ml | 19.36 ml |
| 5 mM | 0.387 ml | 1.936 ml | 3.872 ml |
| 10 mM | 0.194 ml | 0.968 ml | 1.936 ml |
| 5 mM | 0.039 ml | 0.194 ml | 0.387 ml |
Last Update：2024-01-02 23:10:35
Rottlerin - Reference Information
| biological activity | Rottlerin (Mallotoxin, NSC 56346, NSC 94525) is a natural compound purified from Mallotus Philippinensis, a specific inhibitor of Protein kinase, IC50 values for PKCδ (Sf9 insect cells from baculovirus infection), PKCδ (from pig spleen) and CaM kinase III were 3 μM, 6 μM and 5.3 μM, respectively. Rottlerin can also inhibit PKCα, PKCγ, PKCβ, PKCη, CKII and PKA with IC50 values of 30 μM, 40 μM, 42 μM, 82 μM, 30 μM and 78 μM respectively. |
| target | TargetValue PKCδ (Cell-free assay) 3 μM CKIII (Cell-free assay) 5.3 μM PKCα (Cell-free assay) 30 μM CKII (Cell-free assay) 30 μM PKCγ (Cell-free assay) 40 μM |
| Target | Value |
| PKCδ (Cell-free assay) | 3 μM |
| CKIII (Cell-free assay) | 5.3 μM |
| PKCα (Cell-free assay) | 30 μM |
| CKII (Cell-free assay) | 30 μM |
| PKCγ (Cell-free assay) | 40 μM |
| in vitro study | 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. Western Blot Analysis 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 banner. 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 Cell Line: Primary HMVEC (Human Microvascular Endothelial Cell). Concentration: 20 μ m. 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. |
| Cell Line: | Primary HMVEC (Human Microvascular Endothelial Cell). Primary HMVEC (Human Microvascular Endothelial Cell). |
| Concentration: | 20 μM. 20 μM. |
| Incubation Time: | 2, 6, 24 hours. 24/48 hours. |
| Result: | Dramatically decreased the cyclin D-1 mRNA levels in a time-dependent banner. 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. 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. 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. |
| in vivo study | 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). 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. 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. |
| 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. |
| Dosage: | 0 or 20 mg/kg. |
| Administration: | Gavage 5 days per week, once daily, for 6 weeks. |
Last Update：2024-04-09 21:04:16
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Product Name: (E)-1-(6-(3-Acetyl-2,4,6-trihydroxy-5-methylbenzyl)-5,7-dihydroxy-2,2-dimethyl-2H-chromen-8-yl)-3-phenylprop-2-en-1-one Request for quotationCAS: 82-08-6
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Mobile: +86-18621343501
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Tel: 609-228-6898
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