2. PROTAC Cell Cycle/DNA Damage Apoptosis
  3. PROTACs CDK Caspase
  4. PROTAC CDK2/4/6 Degrader-2

PROTAC CDK2/4/6 Degrader-2 是一种靶向 CDK2/4/6 的 PROTAC 降解剂。PROTAC CDK2/4/6 Degrader-2可与特戊酸氯甲酯发生一步反应，转化为前药 PROTAC CDK2/4/6 Degrader-1 (HY-171826)。PROTAC CDK2/4/6 Degrader-2 能够在恶性黑色素瘤细胞中降解 CDK2/4/6 蛋白及其复合物，诱导细胞周期阻滞使其凋亡 (apoptosis) ，对黑色素瘤细胞的作用尤为显著。PROTAC CDK2/4/6 Degrader-2 可用于恶性黑色素瘤的相关研究。
(粉色: CDK2 和 CDK4 和 CDK6 配体 (HY-168440)；蓝色: Cereblon 配体 (HY-10984)；黑色: 连接子)。

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

我们将采用定制合成服务的方式为您快速提供所需产品和技术服务

PROTAC CDK2/4/6 Degrader-2

PROTAC CDK2/4/6 Degrader-2 Chemical Structure

CAS No. : 2541626-49-5

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 CDK2/4/6 Degrader-2 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 Caspase 亚型特异性产品:

查看所有亚型
Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC CDK2/4/6 Degrader-2 is a CDK2/4/6 PROTAC degrader. PROTAC CDK2/4/6 Degrader-2. PROTAC CDK2/4/6 Degrader-2 can be converted into the prodrug PROTAC CDK2/4/6 Degrader-1 (HY-171826) through a one-step reaction with chloromethyl pivalate. PROTAC CDK2/4/6 Degrader-2 degrades CDK2/4/6 and their complex in malignant melanomas cells. PROTAC CDK2/4/6 Degrader-2 induces cell cycle arrest and cell apoptosis in various cancer cells, in particular for melanomas. PROTAC CDK2/4/6 Degrader-2 can be used for malignant melanomas research[1]. (Pink: CDK2 and CDK4 and CDK6 ligand (HY-168440); Blue: Cereblon ligand (HY-10984); Black: linker).

IC50 & Target[1]

CDK2

 

CDK3

 

CDK6

 

Caspase 3

 

CDK4

 

体外研究
(In Vitro)

PROTAC CDK2/4/6 Degrader-2 (compound 3) (作用 72 小时) 对 B16F10 和 A375 细胞均表现出显著的抗增殖活性，IC50 分别为 0.09861 μM 和 0.1659 μM[1]。
PROTAC CDK2/4/6 Degrader-2 (0-2000 nM，0-12 小时) 可通过劫持 E3 泛素连接酶 CRBN，在 B16F10 和 A375 细胞中介导 CDK2/4/6 蛋白降解，并减弱下游 Rb 信号通路的激活[1]。
PROTAC CDK2/4/6 Degrader-2 (50-500 nM，作用 7 天) 对 B16F10 和 A375 细胞具有显著的抗增殖活性[1]。
PROTAC CDK2/4/6 Degrader-2 (125-1000 nM，作用 48 小时) 可在 B16F10 和 A375 细胞中以剂量依赖的方式显著诱导细胞凋亡[1]。
PROTAC CDK2/4/6 Degrader-2 (0-2000 nM，作用 48 小时) 可通过经典的 P53/Bcl-2/Bax 凋亡通路，在 B16F10 和 A375 细胞中诱导半胱天冬酶依赖性凋亡[1]。
PROTAC CDK2/4/6 Degrader-2 (25-1000 nM，作用 48 小时) 可通过降解细胞周期相关蛋白 CDK2/4/6，在 A375 和 B16F10 细胞中诱导细胞周期阻滞[1]。

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

PROTAC CDK2/4/6 Degrader-2 相关抗体:

Western Blot Analysis[1]

Cell Line: B16F10 and A375 cells
Concentration: 0, 62.5, 100, 125, 250, 500, 1000 and 2000 nM
Incubation Time: 0, 3, 6, 9 and 12 h
Result: Induced significant intracellular cleavage of all CDK 2, CDK 4 and CDK 6 proteins in both concentration-dependent and time dependent manners.
Mitigated downstream p-Rb signaling pathway activation of melanoma cells.
Induced CDK2/4/6 protein degradation via the proteasomal pathway at 100 nM and 6 h.

Cell Proliferation Assay[1]

Cell Line: B16F10 and A375
Concentration: 50, 100, 250, 500 nM
Incubation Time: 7 days
Result: Exerted a remarkable inhibiting effect on colony formation in A375 and B16F10 in low nano molar concentration.

Apoptosis Analysis[1]

Cell Line: B16F10 and A375 cells
Concentration: 125, 250, 500, 1000 nM
Incubation Time: 48 h
Result: Significantly induced apoptosis.

Western Blot Analysis[1]

Cell Line: B16F10 and A375 cells
Concentration: 0, 62.5, 125, 250, 500, 1000 and 2000 nM
Incubation Time: 48 h
Result: Upregulated casepase-3 and cleaved PARP protein expression.
Also significantly induced up-regulation of the pro-protein level of P-53 and Bax.
Downregulated the anti-apoptotic protein level of Bcl-2.

Cell Cycle Analysis[1]

Cell Line: B16F10 and A375 cells
Concentration: 0, 25, 50, 100, 250, 500, 1000 nM
Incubation Time: 48 h
Result: Increased accumulation of A375 cell population in G0/G1 phase, but G2/M phase for B16F10 cell.
药代动力学
(Parmacokinetics)
Species Dose Route Indicator value
Rat[1] 10 mg/kg i.v. Cmax 59851 ng/mL
Rat[1] 200 mg/kg p.o. Cmax 692268 ng/mL
Rat[1] 10 mg/kg i.v. Tmax 0.75 h
Rat[1] 200 mg/kg p.o. Tmax 0.25 h
Rat[1] 10 mg/kg i.v. AUC0-24 1607045 ng/mL
Rat[1] 200 mg/kg p.o. AUC0-24 822803.9967 ng/mL
分子量

747.84

Formula

C40H45N9O6
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 CDK2/4/6 Degrader-2 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 CDK2/4/6 Degrader-22541626-49-5PROTACsCDKCaspaseCyclin dependent kinaseCDK2/4/6PROTACdegraderprodrugmalignant melanomasapoptosisInhibitorinhibitorinhibit

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 CDK2/4/6 Degrader-2
目录号：
HY-185121
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