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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 |
[1]. Bowers EM, et al. Virtual ligand screening of the p300/CBP histone acetyltransferase: identification of a selective small molecule inhibitor. Chem Biol. 2010 May 28;17(5):471-82.
[2]. Oike T, et al. C646, a selective small molecule inhibitor of histone acetyltransferase p300, radiosensitizes lung cancer cells by enhancing mitotic catastrophe. Radiother Oncol. 2014 May;111(2):222-7. [3]. Zheng WW, et al. EDAG positively regulates erythroid differentiation and modifies GATA1 acetylation through recruiting p300. Stem Cells. 2014 Aug;32(8):2278-89. [4]. Zhen Fan, et al. Type 2 diabetes-induced overactivation of P300 contributes to skeletal muscle atrophy by inhibiting autophagic flux. Life Sci. 2020 Aug 10;258:118243. |
| Molecular Formula |
C24H19N3O6
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| Molecular Weight |
445.42
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| CAS # |
328968-36-1
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| Related CAS # |
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| SMILES |
O=C(O)C1=CC=C(N2N=C(C)/C(C2=O)=C\C3=CC=C(C4=CC(C)=C(C)C=C4[N+]([O-])=O)O3)C=C1
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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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| 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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