2. PROTAC Epigenetics Cell Cycle/DNA Damage
  3. PROTACs HDAC
  4. TO-1187

TO-1187 是一种选择性 HDAC6 PROTAC 降解剂 (DC50: 5.81 nM)。TO-1187 可促进 HDAC6 的泛素化和降解，可用于血液系统恶性肿瘤和实体瘤的研究 (粉色：HDAC6 ligand (HY-173386)；蓝色：CRBN ligase ligand (HY-41547)；黑色：linker (HY-140212))。

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TO-1187

TO-1187 Chemical Structure

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TO-1187 的其他形式现货产品:

Customer Review

Other Forms of TO-1187:

TO-1187 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 HDAC 亚型特异性产品:

查看所有亚型
HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TO-1187 is a selective HDAC6 PROTAC degrader (DC50: 5.81 nM). TO-1187 promotes the ubiquitination and degradation of HDAC6 and can be used in the study of hematological malignancies and solid tumors (Pink: HDAC6 ligand (HY-173386); Blue: CRBN ligase ligand (HY-41547); Black: linker (HY-140212))[1].

IC50 & Target

HDAC6

5.81 nM (DC50)

Cereblon

 

体外研究
(In Vitro)

TO-1187 (100 nM, 6 h) 在人类多发性骨髓瘤细胞 (MM.1S) 中，高选择性降解 HDAC6 (Dmax: 94%, DC50: 5.81 nM)[1]。
TO-1187 (100 nM, 72 h) 在 MM.1S 细胞中未表现出显著的抗增殖活性，表明其毒性较低[1]。
TO-1187 (1-10000 nM) 在 HeLa 细胞中也表现出剂量依赖的 HDAC6 降解能力。 TO-1187 (100 nM, Pre-treatment for 1 h, then treatment for 6 h) 在 MM.1S 细胞中，通过 CRBN E3 连接酶和蛋白酶体降解 HDAC6[1]。
TO-1187 (100 nM, 6 h) 在 MM.1S 细胞中仅降解 HDAC6，未影响其他蛋白质 (如 CRBN 新底物：IKZF1, IKZF3, CK1α, SALL4 和 GSPT1)，进一步证实其高度选择性[1]。

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

TO-1187 相关抗体:

Western Blot Analysis[1]

Cell Line: human multiple myeloma cells (MM.1S)
Concentration: 100 nM
Incubation Time: 0.5-24 h
Result: Showed monoselectivity for HDAC6, and no degradation selectivity for other HDAC (such as HDAC3 and HDAC8) was observed at a concentration of 25 µM.
Initiated HDAC6 degradation within 30 minutes, the degradation rate reaches 45% within 1 hour, and the maximum degradation effect is achieved within 6 hours (Dmax: 94%).

Western Blot Analysis[1]

Cell Line: human multiple myeloma cells (MM.1S)
Concentration: 100 nM
Incubation Time: Pre-treatment for 1 h, then treatment for 6 h
Result: Degraded HDAC6 via the ubiquitin-proteasome system mediates by CRBN E3 ligase, and its degradation can be competitively inhibited by proteasome inhibitors (MG132 (HY-13259) and Bortezomib (HY-10227)).
Dose-dependently blocked HDAC6 degradation by Thalidomide (HY-14658) (CRBN ligand), demonstrated its dependence on CRBN recruitment for degradation.
体内研究
(In Vivo)

TO-1187 (5 mg/kg, i.v.，单次给药) 显著降低 C57BL/6J 小鼠模型中肝脏 HDAC6 蛋白水平，表明其具有良好的体内降解活性[1]。

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

681.70

Formula

C34H35N9O7
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

TO-1187 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 *
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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.

Keywords:

TO-1187TO1187TO 1187PROTACsHDACHistone deacetylasesHDAC6MM.1S cellsHela cellsC57BL/6J miceInhibitorinhibitorinhibit

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HY-173266
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