2. PROTAC Epigenetics Apoptosis
  3. PROTACs Epigenetic Reader Domain Apoptosis c-Myc Caspase
  4. PROTAC BRD4 Degrader-6

PROTAC BRD4 Degrader-6 (compound 32a) 是一种有效的小分子 BRD4 PROTAC 降解剂, BRD4 BD1 的 IC50 值为 2.7 nM。PROTAC BRD4 Degrader-6 能有效降解 BRD4 蛋白并抑制 c-Myc 的表达。PROTAC BRD4 Degrader-6 能抑制胰腺癌细胞系 BxPC3 的增殖并诱导细胞凋亡。PROTAC BRD4 Degrader-6 可用于人类胰腺癌研究(Pink: Mivebresib (HY-100015); Black: linker, Azido-PEG1-CH2CO2H (HY-108369); Blue: Lenalidomide (HY-A0003))。

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PROTAC BRD4 Degrader-6 Chemical Structure

PROTAC BRD4 Degrader-6 Chemical Structure

CAS No. : 2410947-56-5

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PROTAC BRD4 Degrader-6 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

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC BRD4 Degrader-6 (compound 32a) is a potent small-molecule BRD4PROTAC degrader with IC50 value of 2.7 nM for BRD4 BD1. PROTAC BRD4 Degrader-6 potently degrades BRD4 protein and inhibits the expression of c-Myc. PROTAC BRD4 Degrader-6 inhibits the proliferation of pancreatic cancer cell line BxPC3 and induces apoptosis. PROTAC BRD4 Degrader-6 can be used for human pancreatic cancer research (Pink: Mivebresib (HY-100015); Black: linker, Azido-PEG1-CH2CO2H (HY-108369); Blue: Lenalidomide (HY-A0003))[1].

IC50 & Target[1]

BRD4 BD1

2.7 μM (IC50)

Caspase 3

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
BXPC-3 IC50
0.17 μM
Compound: 11
Antiproliferative activity against human BXPC-3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human BXPC-3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 36202064]
体外研究
(In Vitro)

PROTAC BRD4 Degrader-6 (compound 32a) (72 hours; BxPC3 cell) has anti-proliferation activity with IC50 value of 0.165 μM[1].
PROTAC BRD4 Degrader-6 (compound 32a) (1 μM; 48 hours; BxPC3 cell) induces BRD4 protein degradation in a time-dependent manner, which results in the continuous decrease of c-Myc expression[1].
PROTAC BRD4 Degrader-6 (compound 32a) (1 μM; 48 hours; BxPC3 cell) induces the cell cycle arrest and apoptosis[1].

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

PROTAC BRD4 Degrader-6 相关抗体:

Western Blot Analysis[1]

Cell Line: BxPC3 cell
Concentration: 1 μM
Incubation Time: 48 hours
Result: Degraded BRD4 protein in a time-dependent manner and inhibits the expression of c-Myc.

Cell Cycle Analysis[1]

Cell Line: BxPC3 cell
Concentration: 1 μM
Incubation Time: 48 hours
Result: Increase in G0/G1 and G2/M phase cells, and a decrease of S phase cells.

Apoptosis Analysis[1]

Cell Line: BxPC3 cell
Concentration: 1 μM
Incubation Time: 48 hours
Result: The percentage of cells in early and late apoptosis was recorded as 10.10% and 12.36%, respectively.

Western Blot Analysis[1]

Cell Line: BxPC3 cell
Concentration: 1 μM
Incubation Time: 48 hours
Result: The expression of caspase 3 and cleaved-caspase 3 significantly increased.
分子量

926.90

Formula

C43H40F2N10O10S
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 BRD4 Degrader-6 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:

PROTAC BRD4 Degrader-62410947-56-5PROTACsEpigenetic Reader DomainApoptosisc-MycCaspaseMycapoptosispancreatic cancerBRD4anticancerInhibitorinhibitorinhibit

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