Size | Price | Stock | Qty |
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1mg |
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5mg |
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10mg |
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Other Sizes |
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Purity: ≥98%
Targets |
Rat Brain PKC: 158 nM (IC50)
PKC-α: 53 nM (IC50) PKC-βI: 195 nM (IC50) PKC-βII: 163 nM (IC50) PKC-γ: 213 nM (IC50) PKC-ε: 175 nM (IC50) |
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ln Vitro |
In a time-dependent and TRA-8 dose-dependent manner, bisindolylmaleimide VIII acetate (Ro 31-7549 acetate; 5 μM; 8, 12 hours) markedly accelerated TRA-8-induced cell death[2]. Following simultaneous treatment with TRA-8, procaspase-8 was greatly decreased at 4 hours and totally gone at 6 hours with bisindolylmaleimide VIII acetate (5 μM; 6 hours) [2].
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ln Vivo |
Tumor regression was almost entirely achieved when bisindolylmaleimide VIII acetate (Ro 31-7549 acetate; 100 μg; i.p.; every other day for three doses) was coupled with TRA-8. Significant tumor regression is not achieved with bisindolylmaleimide VIII acetate treatment alone [2].
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Enzyme Assay |
The protein kinase C (PKC) family of isoenzymes is believed to mediate a wide range of signal-transduction pathways in many different cell types. A series of bisindolylmaleimides have been evaluated as inhibitors of members of the conventional PKC family (PKCs-alpha, -beta, -gamma) and of a representative of the new, Ca(2+)-independent, PKC family, PKC-epsilon. In contrast with the indolocarbazole staurosporine, all the bisindolylmaleimides investigated showed slight selectivity for PKC-alpha over the other isoenzymes examined. In addition, bisindolylmaleimides bearing a conformationally restricted side-chain were less active as inhibitors of PKC-epsilon. Most noticeable of these was Ro 32-0432, which showed a 10-fold selectivity for PKC-alpha and a 4-fold selectivity for PKC-beta I over PKC-epsilon.[1]
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Cell Assay |
Apoptosis analysis [2]
Cell Types: 1321N1 Cell Tested Concentrations: 5 μM Incubation Duration: 8, 12 hrs (hours) Experimental Results: TRA-8-induced cell death was Dramatically increased in a time-dependent and TRA-8 dose-dependent manner. Western Blot Analysis[2] Cell Types: 1321N1 Cell Tested Concentrations: 5 μM Incubation Duration: 6 hrs (hours) Experimental Results: procaspase-8 was Dramatically diminished at 4 hrs (hours) and completely disappeared at 6 hrs (hours). |
Animal Protocol |
Animal/Disease Models: 6-8 weeks old female NOD/SCID (severe combined immunodeficient) mouse [2].
Doses: 100 μg Route of Administration: IP; every other day for three doses Experimental Results: Combined with TRA-8, tumor regression was almost complete. |
References |
[1]. Wilkinson SE, et al. Isoenzyme specificity of bisindolylmaleimides, selective inhibitors of protein kinase C. Biochem J. 1993 Sep 1;294 ( Pt 2):335-7.
[2]. Ohtsuka T, et al. Bisindolylmaleimide VIII enhances DR5-mediated apoptosis through the MKK4/JNK/p38 kinase and the mitochondrial pathways. J Biol Chem. 2002 Aug 9;277(32):29294-303. |
Molecular Formula |
C26H26N4O4
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Molecular Weight |
458.50904
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Exact Mass |
458.19540
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Elemental Analysis |
C, 68.11; H, 5.72; N, 12.22; O, 13.96
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CAS # |
138516-31-1
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Appearance |
Brown to reddish brown solid powder
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tPSA |
119Ų
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SMILES |
CN1C=C(C2=C(C(NC2=O)=O)C3=CN(C4=CC=CC=C34)CCCN)C5=CC=CC=C51.CC(O)=O
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InChi Key |
VEOXVBTXROWDAH-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C24H22N4O2.C2H4O2/c1-27-13-17(15-7-2-4-9-19(15)27)21-22(24(30)26-23(21)29)18-14-28(12-6-11-25)20-10-5-3-8-16(18)20;1-2(3)4/h2-5,7-10,13-14H,6,11-12,25H2,1H3,(H,26,29,30);1H3,(H,3,4)
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Chemical Name |
3-(1-(3-aminopropyl)-1H-indol-3-yl)-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione acetate
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Synonyms |
Ro 31-7549 acetate;bisindolylmaleimide viii; 138516-31-1; Ro 31-7549;Bis VIII
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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 : ~250 mg/mL (~545.24 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.54 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 20.8 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: ≥ 2.08 mg/mL (4.54 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: Formulation 1: ≥ 2.1 mg/mL (4.5 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + + 45% Saline |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.1810 mL | 10.9049 mL | 21.8098 mL | |
5 mM | 0.4362 mL | 2.1810 mL | 4.3620 mL | |
10 mM | 0.2181 mL | 1.0905 mL | 2.1810 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.