2. PROTAC Epigenetics
  3. PROTACs Histone Methyltransferase
  4. DOT1L808

DOT1L808 是一种强效且高选择性的 DOT1L PROTAC 降解剂，其 DC50 值为 5 nM。DOT1L808 可促进 DOT1L 的泛素化与降解。DOT1L808 在原位白血病模型中展现出抗肿瘤活性。
(粉色: DOT1L 配体 (HY-181790)；蓝色: VHL 配体 (HY-181791)；黑色: 连接子)。

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DOT1L808

DOT1L808 Chemical Structure

1.  客户无需承担相应的运输费用。

2.  同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

规格 是否有货
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100 mg   询价  
250 mg   询价  

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Customer Review

DOT1L808 相关抗体

Top Publications Citing Use of Products

查看 PROTACs 亚型特异性产品:

查看所有亚型
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

查看 Histone Methyltransferase 亚型特异性产品:

查看所有亚型
EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

DOT1L808 is a potent and highly selective DOT1L PROTAC degrader with a DC50 value of 5 nM. DOT1L808 can promote the ubiquitination and degradation of DOT1L. DOT1L808 exhibits antitumor activity in an orthotopic leukemia model[1]. (Pink: DOT1L ligand (HY-181790); Blue: VHL ligand (HY-181791); Black: linker).

IC50 & Target[1]

VHL

 

DOT1L

5 nM (DC50)

体内研究
(In Vivo)

DOT1L808 (25 mg/kg；腹腔注射；每日 2 次；每周 5 天，持续 2 周) 可显著抑制 NSG 小鼠 MV-4−11-Luc 急性髓系白血病模型中的肿瘤生长[1]。

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

Animal Model: NSG mice (female, 6-8 weeks old, tail vein injection of 1.5 × 106 MV-4−11-Luc cells)[1]
Dosage: 25 mg/kg
Administration: i.p.; twice daily; 2 weeks (5 days per week)
Result: Markedly reduced bioluminescent signal (total photon flux per second) relative to vehicle-treated mice, indicating significant inhibition of disseminated leukemia growth.
Showed no significant body weight changes compared to vehicle controls.
分子量

1301.89

Formula

C61H72ClF3N14O9S2
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

DOT1L808 相关分类

  • 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 *
= × ×

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.

Keywords:

DOT1L808PROTACsHistone MethyltransferaseH3K79 methylationH3K79me2NSG miceMLL-rearranged leukemiaVHL E3 ubiquitin ligaseproteasomal degradationMV-4?11-Luc acute myeloid leukemiaMV-4?11 acute myeloid leukemiaDOT1Lleukemia cellsInhibitorinhibitorinhibit

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产品名称：
DOT1L808
目录号：
HY-181789
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