2. PROTAC Epigenetics Cell Cycle/DNA Damage
  3. PROTACs HDAC Ligands for E3 Ligase
  4. PROTAC HDAC6 degrader 5

PROTAC HDAC6 degrader 5 (Compound 5a) 是一种高度选择性的靶向 HDAC6 的 PROTAC。PROTAC HDAC6 degrader 5 可有效降解细胞中的 HDAC6 (IC50 = 43 nM)。PROTAC HDAC6 degrader 5 通过蛋白酶体和 CRBN 依赖的机制降低 HDAC6 水平。(Pink: Target protein ligand (HY-174408), Target protein ligand + linker (HY-174409); Pomalidomide (HY-10984), Pomalidomide 4'-alkylC3-azide (HY-139341))。

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PROTAC HDAC6 degrader 5

PROTAC HDAC6 degrader 5 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。

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Customer Review

PROTAC HDAC6 degrader 5 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

查看 Ligands for E3 Ligase 亚型特异性产品:

查看所有亚型
von Hippel-Lindau (VHL) MDM2 Cereblon IAP KLHDC2 Fbxo3 RNF4 DCAF11 DCAF1 UHRF1 TRIM21

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC HDAC6 degrader 5 (Compound 5a) is a highly selective PROTAC targeting HDAC6. PROTAC HDAC6 degrader 5 can effectively degrade HDAC6 in cells (IC50 = 43 nM). PROTAC HDAC6 degrader 5 reduces HDAC6 levels through proteasome- and CRBN-dependent mechanisms (Pink: Target protein ligand (HY-174408), Target protein ligand + linker (HY-174409); Blue: Pomalidomide (HY-10984), Pomalidomide 4'-alkylC3-azide (HY-139341))[1].

IC50 & Target

hHDAC1

162 nM (IC50)

hHDAC8

864 nM (IC50)

hHDAC10

2447 nM (IC50)

体外研究
(In Vitro)

PROTAC HDAC6 degrader 5 (Compound 5a) (1 μM, 48 h) 在 IMR-90 细胞中破坏 TGF-β1 诱导的 α-SMA 纤维结构，逆转肌成纤维细胞分化[1]。

PROTAC HDAC6 degrader 5 (1 μM, 10 μM, 3-48 h) 在 IMR-90 细胞中显著降低 HDAC6 蛋白水平[1]。

PROTAC HDAC6 degrader 5 (0.1 μM, 1 μM, 24 h) 在 IMR-90 细胞中有效降解HDAC6并恢复α-微管蛋白乙酰化，浓度依赖性强[1]。

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

PROTAC HDAC6 degrader 5 相关抗体:

Immunofluorescence[1]

Cell Line: IMR-90 cells (TGF-β1-induced fibrosis model)
Concentration: 1 μM
Incubation Time: 48 h
Result: Disrupted the fibers, rendering them less organized.
Reduced and reversed the inhibitory effects on HDAC6 when co-treated with MG-132, and restored TGF-β1-induced fibronectin expression.

Western Blot Analysis[1]

Cell Line: A549 cells, IMR-90 cells, IMR-90 cells (TGF-β1-induced fibrosis model)
Concentration: 0.1 μM, 1 μM, 10 μM
Incubation Time: 3 h, 6 h, 18 h, 24 h, 30 h, 48 h
Result: Had a good degradation effect on HDAC6 at 10 μM, and the degradation reached peaks at 6 and 18 hours in A549 cells.
Reduced the expression of sirtuins significantly and caused a statistically significant increase in the content of acetylated α-tubulin.
Induced maximal degradation of HDAC6 at 1 μM after 24 h of treatment, whereas no decrease in the expression of HDAC1 was observed.
Selectively degraded HDAC6 via the CRBN-proteasome pathway, and the neddylation-independent CRL4 complex was not activated.
分子量

898.96

Formula

C47H50N10O9
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

PROTAC HDAC6 degrader 5 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:

PROTAC HDAC6 degrader 5PROTACsHDACLigands for E3 LigaseHistone deacetylasesE3 ligase-recruiting MoietyIdiopathic Pulmonary Fibrosis (IPF)TGF-β1-induced fibrosisA549 cellsIMR-90 cellsHDAC6CRBNPROTACInhibitorinhibitorinhibit

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产品名称：
PROTAC HDAC6 degrader 5
目录号：
HY-174401
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