2. PROTAC Epigenetics
  3. PROTACs Epigenetic Reader Domain
  4. XYD198

XYD198 (Compound 14h) 是口服有效的 CBP/p300 降解剂。XYD198 抑制 CBP/p300 溴结构域，IC50 为 213.5 nM。XYD198 对急性髓系白血病具有抗肿瘤活性。(Structure: Pink, CBP/p300 ligand 4 (HY-161495); Blue, E3 ligase ligand (HY-14658); Black: linker (HY-161499))

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XYD198 Chemical Structure

XYD198 Chemical Structure

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XYD198 相关抗体

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

XYD198 (Compound 14h) is an orally active degrader for CBP/p300. XYD198 inhibits CBP/p300 bromodomain with IC50 of 213.5 nM. XYD198 exhibits antitumor activity against acute myeloid leukemia. (Structure: Pink, CBP/p300 ligand 4 (HY-161495); Blue, E3 ligase ligand (HY-14658); Black: linker (HY-161499))[1]

体外研究
(In Vitro)

XYD198 (0-1 μM，72-120 h) 抑制急性髓系白血病 (AML) 细胞 MV4;11，MOLM-13 和 MOLM-16 的增殖，IC50 分别为 0.9，47 和 5.5 nM[1]。
XYD198 (0-150 nM，6 h) CRBN 和蛋白酶体依赖地诱导溴结构域蛋白家族中 CBP 和 p300 的降解i[1]。

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

XYD198 相关抗体:

Cell Proliferation 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: 0-150 nM
Incubation Time: 6 h
Result: Degraded CBP and p300 proteins.
体内研究
(In Vivo)

CBP/p300 ligand 4 (5 mg/kg，口服，每 2 天一次，共 2 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 93%[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: 5 mg/kg
Administration: p.o., every other day for 2 weeks
Result: Inhibited tumor growth with a TGI of 93%.
分子量

1002.03

Formula

C54H49F2N11O7
非同位 CAS

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

XYD198 相关分类

  • 摩尔计算器

  • 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:

XYD198XYD 198XYD-198PROTACsEpigenetic Reader DomainAMLNOD-SCID miceMV4;11MOLM-13MOLM-16leukemiaInhibitorinhibitorinhibit

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产品名称：
XYD198
目录号：
HY-161498
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