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。

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YF135 Chemical Structure

YF135 Chemical Structure

CAS No. : 2913177-53-2

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YF135 相关抗体

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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].

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

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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:

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

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HY-144323
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