2. PROTAC Epigenetics
  3. Ligands for Target Protein for PROTAC Epigenetic Reader Domain
  4. CBP/p300 ligand 4

CBP/p300 ligand 4 (Compound 4) 是口服有效的 CBP/p300 溴域抑制剂，IC50 为 91.4 nM。CBP/p300 ligand 4 是 PROTAC XYD190 (HY-161495) 的靶蛋白配体。

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CBP/p300 ligand 4 Chemical Structure

CBP/p300 ligand 4 Chemical Structure

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CBP/p300 ligand 4 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CBP/p300 ligand 4 (Compound 4) is an orally active inhibitor for CBP/p300 bromodomain, with IC50 of 91.4 nM. CBP/p300 ligand 4 serves as a ligand for target protein XYD190 (HY-161495). XYD190 is a PROTAC degrader for CBP/p300[1].

IC50 & Target

IC50: 91.4 nM (CBP/p300 bromodomain)
体外研究
(In Vitro)

CBP/p300 ligand 4 (0-1 μM, 72-120 h) 通过降解 CBP，p300 和 c-Myc 蛋白，抑制 AML 细胞系 MV4;11，MOLM-13 和 MOLM-16 增殖，IC50 分别为 20.4，102 和 12.9 nM[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

CBP/p300 ligand 4 相关抗体:

Cell Viability Assay[1]

Cell Line: MV4;11 AML, MOLM-13 and MOLM-16
Concentration: 0-1 μM
Incubation Time: 3 days for MOLM-13, 4 days for MV4;11 AML and MOLM-16
Result: Inhibited cell proliferation.

Western Blot Analysis[1]

Cell Line: MV4;11 AML, MOLM-13 and MOLM-16
Concentration: 50 nM
Incubation Time: 24 h
Result: Degraded CBP, p300 and c-Myc proteins.
体内研究
(In Vivo)

CBP/p300 ligand 4 (10 mg/kg，口服，每天一次共两周) 在 MV4;11 异种移植小鼠模型中表现出抗肿瘤活性，肿瘤生长抑制率 TGI 为 65%[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: MV4;11 xenograft NOD-SCID mice model[1]
Dosage: 10 mg/kg
Administration: p.o., once every day for 2 weeks
Result: Inhibited tumor growth
分子量

563.60

Formula

C30H31F2N5O4
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

CBP/p300 ligand 4 相关分类

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  • 稀释计算器

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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.

Keywords:

CBP/p300 ligand 4Ligands for Target Protein for PROTACEpigenetic Reader DomainTarget Protein-binding MoietyXYD190AMLNOD-SCID miceMV4;11 AMLMOLM-13MOLM-16Inhibitorinhibitorinhibit

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产品名称：
CBP/p300 ligand 4
目录号：
HY-161495
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