2. PROTAC Epigenetics Apoptosis Cell Cycle/DNA Damage
  3. PROTACs Epigenetic Reader Domain Apoptosis c-Myc CDK PARP
  4. PROTAC BET Degrader-15

PROTAC BET Degrader-15 是一种 BET PORTAC 降解剂，其对于 BRD2、BRD3 和 BRD4 的 DC50 分别为 ＜0.10 nM、＜0.01 nM 和 ＜0.01 nM。PROTAC BET Degrader-15 能诱导显著的 G2/M 期细胞周期阻滞，并诱导细胞凋亡 (apoptosis)。PROTAC BET Degrader-15 可导致 c-Myc 的显著下调，并伴随细胞周期抑制蛋白 p21 的上调、CDK6 的下调以及凋亡标志物 cleaved PARP 的增加。PROTAC BET Degrader-15 可用于血液系统恶性肿瘤和肺癌的研究。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

PROTAC BET Degrader-15

PROTAC BET Degrader-15 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。

3.  试用装只面向终端客户。

规格 是否有货
50 mg   询价  
100 mg   询价  
250 mg   询价  

* Please select Quantity before adding items.

Customer Review

PROTAC BET Degrader-15 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 CDK 亚型特异性产品:

查看所有亚型
CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

查看 PARP 亚型特异性产品:

查看所有亚型
PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC BET Degrader-15 is a BET PROTAC degrader with DC50 values of <0.10 nM, <0.01 nM, and <0.01 nM against BRD2, BRD3, and BRD4, respectively. PROTAC BET Degrader-15 induces significant G2/M phase cell cycle arrest and triggers apoptosis. PROTAC BET Degrader-15 causes marked downregulation of c-Myc, accompanied by upregulation of the cell cycle inhibitory protein p21, downregulation of CDK6, and an increase in the apoptosis marker cleaved PARP. PROTAC BET Degrader-15 is applicable to the research of hematologic malignancies and lung cancer[1].

IC50 & Target[1]

BRD2

＜0.10 nM (DC50)

BRD3

＜0.01 nM (DC50)

BRD4

＜0.01 nM (DC50)

CDK6

 

体外研究
(In Vitro)

PROTAC BET Degrader-15 (Compound CR10) (72 h) 可强效抑制 MV4-11、Molm-13 和 HL-60 急性髓系白血病细胞的增殖，其 IC50 值分别为 1.21、2.14 和 0.69 nM[1]。
PROTAC BET Degrader-15 (72 h) 可强效抑制多种实体肿瘤细胞系的增殖，其 IC50 值范围为 2.83 nM (MDA-MB-231) 至 254.2 nM (A549)[1]。
PROTAC BET Degrader-15 (5-20 nM; 2 h) 可通过依赖 CRBN 和 BET 蛋白结合的泛素-蛋白酶体系统依赖性机制，在 MV4-11 和 A549 细胞中诱导 BRD2、BRD3 和 BRD4 降解[1]。
PROTAC BET Degrader-15 (1 h) 以纳摩尔亲和力结合 BRD2、BRD3 和 BRD4 溴结构域，其 IC50 值范围为 22 nM (BRD3 (1)) 至 61 nM (BRD4 (2))[1]。
PROTAC BET Degrader-15 (1-50 nM; 24 h) 以剂量依赖的方式将 MV4-11 细胞阻滞于细胞周期的 G2/M 期[1]。
PROTAC BET Degrader-15 (1-20 nM; 24 h) 可剂量依赖性地诱导 MV4-11 细胞发生细胞凋亡，在处理 24 h 后，低至 1 nM 的浓度下即可观察到显著的细胞凋亡[1]。
PROTAC BET Degrader-15 (3.3-1000 nM; 24 h) 可调控 MV4-11、A549 和 MDA-MB-231 细胞中与增殖、细胞周期调控及凋亡相关的关键蛋白，包括下调 C-Myc 和 CDK6、上调 P21 并诱导 PARP 切割[1]。
PROTAC BET Degrader-15 (4-50 nM; 8 d) 可强效抑制 A549 和 MDA-MB-231 实体瘤细胞的集落形成能力，在 10 nM 浓度下可观察到近乎完全的抑制作用[1]。
PROTAC BET Degrader-15 (50-100 nM; 0-12 h) 可在 50 nM 和 100 nM 浓度下强效抑制 MDA-MB-231 乳腺癌细胞的迁移能力[1]。

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

PROTAC BET Degrader-15 相关抗体:

Western Blot Analysis[1]

Cell Line: MV4-11 and A549 cells
Concentration: 5 nM (MV4-11 cells, 2 h); 20 nM (A549 cells, 2 h); 10 μM MG132, 10 μM Pomalidomide, 10 μM MLN4924, 100 nM compound 10 (2 h pretreatment)
Incubation Time: 2 h (PROTAC BET Degrader-15 treatment); 2 h (pretreatment prior to PROTAC BET Degrader-15 addition)
Result: Had induced degradation of BRD2, BRD3, and BRD4 completely abolished by pretreatment with MG132, Pomalidomide, MLN4924, or compound 10 in both MV4-11 and A549 cells.

Cell Cycle Analysis[1]

Cell Line: MV4-11 cells
Concentration: 1, 5, 20 and 50 nM
Incubation Time: 24 h
Result: Induced a significant, dose-dependent arrest at the G2/M phase of the cell cycle.

Apoptosis Analysis[1]

Cell Line: MV4-11 cells
Concentration: 1, 5 and 20 nM
Incubation Time: 24 h
Result: Elicited pronounced pro-apoptotic effects starting at 1 nM, with apoptosis increasing in a dose-dependent manner.

Western Blot Analysis[1]

Cell Line: MV4-11, A549, and MDA-MB-231 cells
Concentration: 3.3, 10, 100, 200 and 1000 nM
Incubation Time: 24 h
Result: Caused dose-dependent downregulation of C-Myc and CDK6, upregulation of P21, and an increase in cleaved-PARP levels (with a corresponding decrease in full-length PARP) in all three cell lines.

Cell Migration Assay [1]

Cell Line: MDA-MB-231 breast cancer cells
Concentration: 50 and 100 nM
Incubation Time: 0, 6, 12 h post-treatment monitoring
Result: Significantly suppressed cell migration relative to controls, as measured by reduced wound closure over time.
药代动力学
(Parmacokinetics)
Species Dose Route T1/2 Cmax Vss MRT0-inf CL AUC0-t AUC0-∞ Tmax CL/F Vz/F Bioavailability
Mice[1] 1 mg/kg i.v. 1.88 h 207.14 ng/mL 0.75 L/kg 2.62 h 0.28 L/h/kg 204.05 ng·h/mL 215.32 ng·h/mL / / / /
Mice[1] 20 mg/kg i.p. 4.26 h 778.68 ng/mL / 5.10 h / 4571.49 ng·h/mL 4662.67 ng·h/mL 2.00 h 3.98 mL/min/kg 1.45 L/kg 108.27 %
Mice[1] 20 mg/kg p.o. 0.92 h 350.49 ng/mL / 1.38 h / 496.20 ng·h/mL 529.67 ng·h/mL 0.33 h 40.02 mL/min/kg 3.13 L/kg 12.30 %
体内研究
(In Vivo)

PROTAC BET Degrader-15 (Compound CR10) (1-2 mg/kg; i.p.; 每 4 天一次共 21 天) 可在 A549 异种移植小鼠中诱导剂量依赖性的肿瘤生长抑制[1]。
PROTAC BET Degrader-15 (1-2 mg/kg; i.p.; 每 4 天一次共 17 天) 可在 MV4-11 异种移植小鼠中诱导剂量依赖性肿瘤生长抑制[1]。

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

Animal Model: BALB/c nude (female, 6-8 weeks old)[1]
Dosage: 1 mg/kg; 2 mg/kg
Administration: i.p.; every 4 days; 21 days
Result: Induced tumor growth inhibition rate of 54.74% at 1 mg/kg and 72.97% at 2 mg/kg, which were notably higher than the positive control dBet1.
Maintained largely unchanged body weights throughout the study.
Showed no obvious lesions in major organs (heart, liver, spleen, lung, kidney) via histopathological examination.
Showed no significant abnormalities in hematological and biochemical analyses.
Animal Model: BALB/c nude (female, 6-8 weeks old)[1]
Dosage: 1 mg/kg; 2 mg/kg
Administration: i.p.; every 4 days; 17 days
Result: Induced tumor growth inhibition rates of 44.26% at 1 mg/kg and 63.19% at 2 mg/kg, which were higher than the positive control dBet1.
Maintained largely unchanged body weights throughout the study.
Showed no obvious lesions in major organs (heart, liver, spleen, lung, kidney) via histopathological examination.
Showed no significant abnormalities in hematological and biochemical analyses.
分子量

795.88

Formula

C44H45N9O6
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 BET Degrader-15 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 BET Degrader-15PROTAC BET Degrader15PROTAC BET Degrader 15PROTACsEpigenetic Reader DomainApoptosisc-MycCDKPARPMycCyclin dependent kinasepoly ADP ribose polymerasexenograft tumorsBRD3BRD4ubiquitin-proteasome systemMV4-11 cellshematologic malignancieslung cancerMolm-13 cellsBRD2HL-60 cellsInhibitorinhibitorinhibit

您最近查看的产品:

Your information is safe with us. * Required Fields.

   产品名称：

  

* 需求量：

* 客户姓名：

 

* Email：

* 电话：

 

* 公司或机构名称：

   留言给我们：

Bulk Inquiry

Inquiry Information

产品名称：
PROTAC BET Degrader-15
目录号：
HY-181729
需求量：

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

   产品名称：

  

* Lot #：

* 客户姓名：

 

* Email：

   电话：

 

* 部门：

* 公司或机构名称：

 

   留言给我们：

Request for HNMR Report

We have received your request and will respond to you as soon as possible.

嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z