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KCC 07 is an MBD2 (Methyl-CpG-binding domain protein 2) inhibitor that prevents binding of MBD2 to methylated DNA and activates brain specific angiogenesis inhibitor 1 (BAI1)/p53 signaling.
| Targets |
MBD2 (methyl-CpG-binding domain protein 2)
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|---|---|
| ln Vitro |
In vitro treatment of MB cells with KCC-07 (10 μM; 72 hours) greatly decreased their proliferation, in line with anti-proliferative BAI1/p53/p21 signaling [1]. treatment of MB cells) significantly reduced the binding of MBD2 to the ADGRB1 promoter and reinstated the production of BAI1 mRNA and protein in MB cells that had been BAI1-silenced [1].
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| ln Vivo |
KCC-07 (100 mg/kg; intraperitoneal injection; 5 days/week; athymic nude mice) treatment significantly extended the lifespan of MB xenografts in vivo and suppressed tumor growth [1].
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| Cell Assay |
Cell viability assay [1]
Cell Types: Medulloblastoma (MB) cells Tested Concentrations: 10 μM Incubation Duration: 72 hrs (hours) Experimental Results: Dramatically inhibited MB cell growth in vitro. Western Blot Analysis [1] Cell Types: Medulloblastoma (MB) Cell Tested Concentrations: 10 μM Incubation Duration: 48 hrs (hours) Experimental Results: In BAI1-silenced MB cells, MBD2 binding to the ADGRB1 promoter was largely eliminated. |
| Animal Protocol |
Animal/Disease Models: outbred athymic nude mice (female; 8-10 weeks old) injected with MB cells [1]
Doses: 100 mg/kg Route of Administration: intraperitoneal (ip) injection; 5 days per week Experimental Results: Dramatically prolonged MB xenogeneic How long the graft survives in the body. |
| References |
[1]. Dan Zhu, et al. BAI1 Suppresses Medulloblastoma Formation by Protecting p53 From Mdm2-Mediated Degradation. Cancer Cell. 2018 Jun 11;33(6):1004-1016.e5.
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| Molecular Formula |
C14H11N3OS
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|---|---|
| Molecular Weight |
269.322
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| Exact Mass |
269.06
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| Elemental Analysis |
C, 62.44; H, 4.12; N, 15.60; O, 5.94; S, 11.90
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| CAS # |
315702-75-1
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| Appearance |
Solid powder
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| SMILES |
C1=CC=NC(=C1)C2=CSC(=N2)NC3=CC(=CC=C3)O
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| InChi Key |
GIGNWEDIMLUWCT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H11N3OS/c18-11-5-3-4-10(8-11)16-14-17-13(9-19-14)12-6-1-2-7-15-12/h1-9,18H,(H,16,17)
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| Chemical Name |
3-[(4-pyridin-2-yl-1,3-thiazol-2-yl)amino]phenol
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| Synonyms |
KCC 07; KCC07; KCC-07
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| HS Tariff Code |
2934.99.03.00
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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: 54~125 mg/mL (200.5~464.1 mM)
Ethanol: 54 mg/mL |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.72 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 (7.72 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: ≥ 2.08 mg/mL (7.72 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.7131 mL | 18.5653 mL | 37.1306 mL | |
| 5 mM | 0.7426 mL | 3.7131 mL | 7.4261 mL | |
| 10 mM | 0.3713 mL | 1.8565 mL | 3.7131 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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