| Size | Price | Stock | Qty |
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| 10mg |
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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%
C646 is a potent, selective and competitive inhibitor for histone acetyltransferase p300. It inhibits p300 with a Ki of 400 nM in a cell-free assay. It is less potent for other acetyltransferases and preferentially selective for p300. C646 induces cell cycle arrest and apoptosis selectively in AML1-ETO-positive AML cells. C646 reverses epithelial to mesenchymal transition of human peritoneal mesothelial cells via blocking TGF-β1/Smad3 signaling pathway in vitro. C646 shows a noncompetitive pattern of p300 inhibition versus H4-15 peptide substrate. C646 treatment reduces histone H3 and H4 acetylation levels and abrogates TSA-induced acetylation in cells.
| ln Vitro |
C646 is a linear competitive inhibitor of p300 and acetyl-CoA with Ki of 400 nM. C646 demonstrates a noncompetitive method of p300 inhibition with the H4-15 peptide substrate. C646 treatment lowered histone H3 and H4 acetylation levels and eliminated TSA-induced acetylation in cells. C646 has a more effective effect on cell proliferation than Lys-CoA-Tat [1]. C646 promotes mitotic catastrophe after IR and suppresses the phosphorylation of CHK1 following IRin in A549 cells [2]. C646 attenuates the rise in GATA1 acetylation and the EDAG-induced increase in GATA1 transcriptional activity [3].
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| ln Vivo |
Inhibition of P300 by c646 (intraperitoneal injection, 30 nmol/g/d, for 2 weeks) dramatically lowered blood glucose levels in db/db mice [4].
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| Animal Protocol |
Animal/Disease Models: Fourteenweeks old male db/db mice and normal m/m mice[4]
Doses: 30 nmol/g Route of Administration: Intraperitoneally injected; daily; 2 weeks Experimental Results: The db/db mice demonstrated greater body masses and higher levels of fasting blood glucose than the m/m mice. |
| References |
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| Additional Infomation |
C646 is a pyrazolone that is 5-methyl-4-methylene-2-(p-carboxyphenyl)-2,4-dihydro-3H-pyrazol-3-one in which the exocyclic carbon of the methylene group is attached to a 5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl group by a single bond. C646 is a potent, cell permeable and selective competitive inhibitor of p300 and CBP (p300/CBP) histone acetyltransferases. It has a role as an EC 2.3.1.48 (histone acetyltransferase) inhibitor, an apoptosis inducer and a radiosensitizing agent. It is a member of furans, a biaryl, a pyrazolone, a member of benzoic acids and a C-nitro compound.
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| Molecular Formula |
C24H19N3O6
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|---|---|---|
| Molecular Weight |
445.42
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| Exact Mass |
445.127
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| CAS # |
328968-36-1
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| Related CAS # |
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| PubChem CID |
1285941
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| Appearance |
Brown to reddish brown solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
662.6±65.0 °C at 760 mmHg
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| Melting Point |
224-226℃
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| Flash Point |
354.5±34.3 °C
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| Vapour Pressure |
0.0±2.1 mmHg at 25°C
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| Index of Refraction |
1.663
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| LogP |
4.87
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
33
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| Complexity |
857
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=CC(=C(C=C1C)[N+](=O)[O-])C2=CC=C(O2)/C=C\3/C(=NN(C3=O)C4=CC=C(C=C4)C(=O)O)C
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| InChi Key |
HEKJYZZSCQBJGB-UNOMPAQXSA-N
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| InChi Code |
InChI=1S/C24H19N3O6/c1-13-10-20(21(27(31)32)11-14(13)2)22-9-8-18(33-22)12-19-15(3)25-26(23(19)28)17-6-4-16(5-7-17)24(29)30/h4-12H,1-3H3,(H,29,30)/b19-12-
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| Chemical Name |
4-[(4Z)-4-[[5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl]methylidene]-3-methyl-5-oxopyrazol-1-yl]benzoic acid
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| Synonyms |
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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 |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 1.67 mg/mL (3.75 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 16.7 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: 1.67 mg/mL (3.75 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 16.7 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: 5% DMSO+30% PEG 300+ddH2O:1mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2451 mL | 11.2254 mL | 22.4507 mL | |
| 5 mM | 0.4490 mL | 2.2451 mL | 4.4901 mL | |
| 10 mM | 0.2245 mL | 1.1225 mL | 2.2451 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.
Inhibition of p300 enhances LTP in the infralimbic PFC. J Neurosci. 2011 May 18; 31(20): 7486–7491. |
Inhibition of p300 in the ILPFC enhances fear extinction memory. J Neurosci. 2011 May 18; 31(20): 7486–7491. |
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