2. PROTAC Epigenetics
  3. PROTACs Histone Methyltransferase
  4. DOT1L705

DOT1L705 是一种具靶向 DOT1L 的 PROTAC 降解剂。DOT1L705 招募 VHL E3 泛素连接酶以诱导 DOT1L 的蛋白酶体降解。DOT1L705 可降低白血病细胞的活力。DOT1L705 可抑制 H3K79 甲基化。DOT1L705 可用于 MLL 重排白血病的相关研究。
(粉色: DOT1L 配体 (HY-135127)；蓝色: VHL E3 连接酶配体；黑色: 连接子)。

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DOT1L705

DOT1L705 Chemical Structure

CAS No. : 3050756-34-5

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DOT1L705 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

DOT1L705 is a PROTAC degrader that targets DOT1L. DOT1L705 recruits the VHL E3 ubiquitin ligase to induce proteasomal degradation of DOT1L. DOT1L705 reduces the viability of leukemia cells. DOT1L705 inhibits H3K79 methylation. DOT1L705 can be used in studies related to MLL-rearranged leukemia[1]. (Pink: DOT1L ligand (HY-135127); Blue: VHL E3 ligase ligand; Black: linker).

体外研究
(In Vitro)

DOT1L705 (0-10 μM，96 h) 可降低 DOT1L 蛋白水平，抑制 H3K79 甲基化水平。
DOT1L808 (0.01-100 μM，5 days) 可降低 MLL 重排型急性髓系白血病细胞系的存活率。

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

DOT1L705 相关抗体:

Western Blot Analysis[1]

Cell Line: MV-4-11
Concentration: 0-10 μM
Incubation Time: 6 h-96 h
Result: Induced dose-dependent degradation of DOT1L in MV-4-11 cells with a DC50 of 0.33 μM, achieving near-complete degradation within 4-6 hours (sustained for 96 hours).
Reduced H3K79me2 levels in MV-4-11 cells with an IC50 of 0.026 μM, 13-fold more potent than its effect on DOT1L protein levels.

Cell Viability AssayWestern Blot AnalysisCell Proliferation AssayApoptosis AnalysisCell Cytotoxicity AssayCell Cycle AnalysisRT-PCRCell Autophagy AssayImmunofluorescenceCell Differentiation AssayCell Invasion AssayCell Migration Assay Real Time qPCRELISA Assay[1]

Cell Line: MLL-rearranged cell lines
Concentration: 0.01-100 μM
Incubation Time: 5 days
Result: Selectively inhibited viability of MLL-rearranged cell lines (MV-4-11 IC50 = 0.29 μM; EOL-1 IC50 = 0.39 μM; Pfeiffer IC50 = 0.80 μM) while showing minimal activity against non-MLL-rearranged lines (KG-1 IC50 > 50 μM).
体内研究
(In Vivo)

DOT1L705 (1-10 mg/kg；腹腔注射；每日 2 次) 在 MV-4-11 异种移植模型中表现出体内疗效，且具有良好的药代动力学特性[1]。

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

Animal Model: C57 BL/6 female mice ( 7−8 week old)[1]
Dosage: 1 mg/kg (pharmacokinetics); 10 mg/kg (in vivo efficacy)
Administration: in vitro; i.p. (single dose, pharmacokinetics); i.p. (BID, in vivo efficacy)
Result:
Reduced tumor volumes by >50% relative to vehicle control in an MV-4-11 subcutaneous xenograft model at 10 mg/kg BID i.p., with no significant body weight loss.
Showed reduced H3K79me2 levels in tumor lysates from the MV-4-11 subcutaneous xenograft model, confirming on-target activity.
分子量

1337.88

Formula

C61H72ClF3N12O13S2
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

DOT1L705 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • 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:

DOT1L7053050756-34-5PROTACsHistone MethyltransferaseH3K79 methylationorthotopic modelsVHL E3 ubiquitin ligaseMLL-rearranged acute myeloid leukemia cell linesDOT1Lproteasomal degradationMV-4-11 xenograft modelMLL-rearranged leukemia cellsmenin inhibitor-resistant leukemia cellsInhibitorinhibitorinhibit

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目录号：
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