1. Epigenetics
  2. Epigenetic Reader Domain
  3. CZL-077

CZL-077 是一种高效、选择性强且口服有效的 p300/CBP 溴结构域 (BRD) 抑制剂 (p300 IC50 = 0.034 μM,CBP IC50 = 0.052 μM),对 BET 蛋白的 BRD (BRD2/3/4) 具有高度选择性。CZL-077 抑制 OPM-2 和 22RV1 细胞的生长,IC50 值分别为 0.024 μM 和 5.6 μM。CZL-077 在 OPM-2 和 22RV1 异种移植小鼠模型中显示出抗肿瘤活性。CZL-077 可用于多发性骨髓瘤和前列腺癌的研究。

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CZL-077

CZL-077 Chemical Structure

CAS No. : 3032444-06-4

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CZL-077 is a potent, selective, and orally active p300/CBP bromodomain (BRD) inhibitor (p300 IC50 = 0.034 μM, CBP IC50 = 0.052 μM) exhibiting high selectivity over the BRDs of BET proteins (BRD2/3/4). CZL-077 inhibits cell growth with IC50 values of 0.024 μM and 5.6 μM in OPM-2 and 22RV1 cells, respectively. CZL-077 shows antitumor efficacy in OPM-2 and 22RV1 xenograft mouse models. CZL-077 can be used for multiple myeloma and prostate cancer research[1].

IC50 & Target[1]

BRD2 (BD1)

3.81 μM (IC50)

BRD2 (BD2)

>10 μM (IC50)

BRD3 (BD1)

5.54 μM (IC50)

BRD3 (BD2)

>10 μM (IC50)

BRD4 BD1

6.45 μM (IC50)

BRD4 BD2

>10 μM (IC50)

p300

0.034 μM (IC50)

CBP

0.052 μM (IC50)

分子量

577.62

Formula

C30H26F3N5O2S

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
CZL-077
目录号:
HY-180804
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