2. PROTAC Cell Cycle/DNA Damage
  3. PROTACs PERK
  4. YF135

YF135 是一种高效的可逆共价 KRASG12C PROTAC。以 KRAS G12C inhibitor 48 (compound 6d) 作为配体，以 MRTX849 联动 VHL 配体为支架，设计合成YF135。YF135 通过 E3 连接酶 VHL 介导的蛋白酶体途径显著诱导 KRASG12C 的可逆降解，降低 ERK 磷酸化水平。

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

YF135 Chemical Structure

YF135 Chemical Structure

CAS No. : 2913177-53-2

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

YF135 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

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

YF135 is an efficient and reversible-covalent KRASG12C PROTAC. YF135 is designed and synthesized by tethering KRAS G12C inhibitor 48 (compound 6d) as the ligand, and basing on the scaffold of MRTX849 linkage VHL ligand. YF135 significantly induces the degradation of KRASG12C in a reversible manner and decreases phospho-ERK level through the E3 ligase VHL mediated proteasome pathway[1].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
NCI-H23 IC50
243.9 nM
Compound: YF135
Antiproliferative activity against human NCI-H23 cells harboring KRAS G12C mutant measured after 72 hrs by CCK-8 assay
Antiproliferative activity against human NCI-H23 cells harboring KRAS G12C mutant measured after 72 hrs by CCK-8 assay
[PMID: 35007863]
NCI-H358 IC50
153.9 nM
Compound: YF135
Antiproliferative activity against human NCI-H358 cells harboring KRAS G12C mutant measured after 72 hrs by CCK-8 assay
Antiproliferative activity against human NCI-H358 cells harboring KRAS G12C mutant measured after 72 hrs by CCK-8 assay
[PMID: 35007863]
体外研究
(In Vitro)

YF135 inhibits the proliferation of H358 and H23 cells with IC50 values of 153.9 and 243.9 nM, respectively[1].
YF135 obviously decreases the protein level of KRASG12C and phospho-ERK in H358 and H23 cells in a time (3 μM, 0-36 h) and dose (0-10 μM, 24 h) dependent manner, while the washout by fresh medium significantly rescues such effects[1].
YF135 induces degradation of KRASG12C through the E3 ligase VHL mediated proteasome pathway. YF135 covalently bind to KRASG12C and VHL ligase to form a ternary complex[1].

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

YF135 相关抗体:

Western Blot Analysis

Cell Line: lung cancer cell lines H358, H23 and A549 [1]
Concentration: 0, 0.3, 1, 3, 10 μM
Incubation Time: 0, 12, 24, 36 h
Result: Obviously decreased the protein level of KRASG12C and phospho-ERK in a time (3 μM, 0-36 h) and dose (0-10 μM, 24 h) dependent manner, with DC50 values of 3.61, 1.68 μM in H358 cells, respectively, and 4.53, 1.44 μM in H23 cells, respectively.

Western Blot Analysis

Cell Line: lung cancer cell lines H358, H23 and A549 [1]
Concentration: 3 μM
Incubation Time: 24 h
Result: Induced the significant degradation on KRASG12C and decreased the level of phospho-ERK, while the washout by fresh medium significantly rescued such effects.
分子量

1179.86

Formula

C63H75ClN12O7S
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

YF135 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:

YF1352913177-53-2YF 135YF-135PROTACsPERKProtein kinase R-like endoplasmic reticulum kinasePKR-like endoplasmic reticulum kinaseH358 cellsH23 cellsReversible-covalentPROTACAnticancerInhibitorinhibitorinhibit

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：
YF135
目录号：
HY-144323
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