2. PROTAC Epigenetics Cell Cycle/DNA Damage Apoptosis
  3. PROTACs HDAC Apoptosis
  4. PROTAC HDAC6 degrader 1

PROTAC HDAC6 degrader (Compound A6) 是一种有效的、选择性的 PROTAC HDAC6 降解剂，DC50 为 3.5 nM。PROTAC HDAC6 degrader 在髓系白血病细胞系中通过诱导凋亡 (apoptosis) 显示出抗增殖活性。

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PROTAC HDAC6 degrader 1 Chemical Structure

PROTAC HDAC6 degrader 1 Chemical Structure

CAS No. : 2785404-76-2

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PROTAC HDAC6 degrader 1 相关抗体

Top Publications Citing Use of Products

查看 PROTACs 亚型特异性产品:

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

查看 HDAC 亚型特异性产品:

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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

PROTAC HDAC6 degrader (Compound A6) is a potent and selective PROTAC HDAC6 degrader with a DC50 of 3.5 nM. PROTAC HDAC6 degrader shows promising antiproliferative activity via inducing apoptosis in myeloid leukemia cell lines[1].

IC50 & Target[1]

HDAC6

3.5 nM (DC50)

HDAC6

4.86 nM (IC50)

HDAC1

0.1 μM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
MOLM-13 IC50
17.4 μM
Compound: A6
Cytotoxicity against human MOLM-13 cells assessed as reduction in cell viability incubated for 72 hrs by ATP based Celltiter-glo luminescent assay
Cytotoxicity against human MOLM-13 cells assessed as reduction in cell viability incubated for 72 hrs by ATP based Celltiter-glo luminescent assay
[PMID: 36473103]
体外研究
(In Vitro)

PROTAC HDAC6 degrader (Compound A6) (0.1-10 μM; 6 h) 不会降解 HDAC1，但对 HDAC1 表现出抑制活性。PROTAC HDAC6 degrader 在 U266 和 HL-60 细胞中显示出强大的 HDAC6 降解以及α-微管蛋白的高乙酰化，证实其活性不局限于白血病细胞系[1]。
PROTAC HDAC6 degrader (0.5-50 μM) 抑制白血病细胞活性，其对数 IC50 值为 1.2-1.7 μM[1]。
PROTAC HDAC6 degrader (8-24 μM; 48 h) 诱导 MOLM13 细胞凋亡，细胞周期阻滞于亚 G1 期[1]。

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

PROTAC HDAC6 degrader 1 相关抗体:

Western Blot Analysis[1]

Cell Line: HL-60 cells
Concentration: 100 nM, 1 μM, 10 μM
Incubation Time: 6 h
Result: Degraded HDAC6 but not HDAC1. Induced hyperacetylation of α-tubulin and caused hyperacetylation of histone H3.

Cell Viability Assay[1]

Cell Line: Acute myeloid leukemia or AML (HL-60, Kasumi, THP-1, HL-60, SKNO1, and MOLM13) and B-cell acute lymphoblastic leukemia or B-ALL (REH and 697)
Concentration: 0.5-50 μM
Incubation Time: 72 h
Result: Inhibited cell viability with log IC50 values of 1.2-1.7 μM.

Apoptosis Analysis[1]

Cell Line: MOLM13
Concentration: 8, 16 and 24 μM
Incubation Time: 48 h
Result: Induced caspase 3/7-dependent apoptosis in dose-dependent fashion.

Cell Cycle Analysis[1]

Cell Line: MOLM13
Concentration: 8, 16 and 24 μM
Incubation Time: 48 h
Result: Induced a dose-dependent increase in the sub-G1 fraction with a concomitant reduction of cell population in G2/M phase.
分子量

734.80

Formula

C37H46N6O10
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

PROTAC HDAC6 degrader 1 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:

PROTAC HDAC6 degrader 12785404-76-2PROTACsHDACApoptosisHistone deacetylasesHL-60U266leukemiaMOLM13Inhibitorinhibitorinhibit

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