C-646
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Cat.No：IC3420 Solarbio
CAS：328968-36-1
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：Solid
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> Small Molecule Compounds > Inhibitors & Antagonists & Agonists > Epigenetics > C-646
Product Information
| CAS | 328968-36-1 |
| Name | C-646 |
| Molecular Formula | C24H19N3O6 |
| Molecular Weight | 445.42 |
| Solubility | Soluble in DMSO |
| Purity | ≥98% |
| Appearance | Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD01311760 |
| 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 |
| InChIKey | HEKJYZZSCQBJGB-UNOMPAQXSA-N |
| InChI | 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- |
| PubChem CID | 1285941 |
| Target Point | Histone Acetyltransferase;p300/CBP |
| Passage | Epigenetics |
| Background | C646 is a histone acetyltransferase inhibitor that inhibits p300. |
| Biological Activity | C646 是选择性，竞争性的 histone acetyltransferase p300 抑制剂，Ki 值为 400 nM，对其他的乙酰转移酶作用较小[1-3]。 |
| In Vitro | C646是p300与乙酰辅酶A的线性竞争性抑制剂，Ki为400 nM。 C646显示相对于H4-15肽底物的p300抑制的非竞争性模式。 C646处理降低组蛋白H3和H4乙酰化水平并消除细胞中TSA诱导的乙酰化。 C646对细胞生长的影响比Lys-CoA-Tat更有效[1]。 C646增强IR后的有丝分裂突变并抑制IRin A549细胞后CHK1的磷酸化[2]。 C646减弱了由EDAG诱导的GATA1乙酰化增加和GATA1转录活性增加[3]。 |
| Cell Experiment | 将细胞接种在6孔板中，在37℃下孵育4-10小时以进行附着，并暴露(或不暴露于)C646。温育2小时后，将细胞进行(或不进行)IR，并孵育10天以形成集落。用甲醇固定细胞并用结晶紫染色。计数至少50个细胞的集落。将存活的部分标准化为相应的对照。通过使用线性二次模型计算将存活分数降低至照射细胞的10％(D10)所需的剂量。 |
| Kinase Experiment | 在以下反应条件下，反应在30℃下进行2至4分钟：50mM HEPES，pH 7.9，50mM NaCl，0.05mg/mL BSA，5mM DTT，0.05mM EDTA，0.25％DMSO，10μM的X.laevis组蛋白H3和不同浓度的C646(0，3，10μM)。反应包含70纳克的Rtt109/Vps75，15纳克的yGcn5，300纳克的SAS络合物或1微克的hMOZ。通过比较样品的考马斯蓝染色与牛血清白蛋白标准品，通过SDS-PAGE分析来估计每个测定中使用的酶量。使混合物在30℃下平衡10分钟，然后加入12C-AcCoA和14C-AcCoA的1：1混合物至终浓度为20μM。在适当的时间后，用6×Tris-Tricine凝胶上样缓冲液淬灭反应，该缓冲液含有0.2mol/LTris-Cl pH 6.8，40％v/v甘油，14％w/v SDS，0.3mol/LDTT和0.06％ w/v考马斯蓝。在16.5％Tris-Tricine SDS-PAGE凝胶上将14 C标记的组蛋白底物与反应物分离。通过放射自显影定量14C掺入组蛋白H3的速率。所有测定均一式两份，这些通常在20％内达成一致。 |
| Data Literature Source | [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 |
| Unit | Bottle |
| Specification | 5mg 10mg |
C646 是一种histone acetyltransferase抑制剂，抑制p300。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
Note：
1. The products are all for scientific research use only. Do not use it for medical, clinical diagnosis or treatment, food and cosmetics, etc. Do not store them in ordinary residential areas.
2. For your safety and health, please wear laboratory clothes, disposable gloves and masks.
3. The experimental results may be affected by many factors, after-sale service is limited to the product itself and does not involve other compensation.
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