2. PROTAC MAPK/ERK Pathway GPCR/G Protein Apoptosis
  3. PROTACs Ras p38 MAPK TNF Receptor
  4. ZJK-807

ZJK-807 是一种高效且具有选择性的 PROTAC 降解剂，靶向 KRASG12D (在 AsPC-1 细胞中 DC50 = 79.5 nM)。ZJK-807 对野生型 KRAS 或其他突变体 (G12C/S/V、G13D) 的影响极小，可诱导突变体特异性细胞毒性。ZJK-807 抑制 RAS/MAPK 信号通路，并独特地调节 TNF 信号通路和真核生物核糖体生物合成。ZJK-807 可用于 KRAS 驱动的胰腺癌的研究。黄色：KRASG12D 配体 (HY-W087383)；绿色：E3 连接酶 CRBN 配体 (HY-178507)。黑色：连接子 (HY-178506)。

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ZJK-807

ZJK-807 Chemical Structure

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ZJK-807 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ZJK-807 is a highly effective and selective PROTAC degrader targeting KRASG12D (DC50 = 79.5 nM in AsPC-1 cells). ZJK-807 shows minimal impact on wild-type KRAS or other mutants (G12C/S/V, G13D), inducing mutant-specific cytotoxicity. ZJK-807 suppresses RAS/MAPK signaling and uniquely modulates TNF signaling and eukaryotic ribosome biogenesis. ZJK-807 can be used for the study of KRAS-driven pancreatic cancer. Yellow: KRASG12D ligand (HY-W087383); Green: E3 ligase CRBN ligand (HY-178507); Black: Linker (HY-178506)[1].

体外研究
(In Vitro)

ZJK-807 (Compound A11) (10 μM，0.5-24小时) 可导致 KRASG12D 水平随时间推移而降低，并显著降低 pERK 水平，即使在 AsPC-1 细胞中药物清除后仍能继续降解[1]。
在 AsPC-1 细胞中，ZJK-807 (1-3 μM，12-16 h) 在1 μM浓度下处理 16 小时可促进 HA-KRASG12D 与CRBN E3 连接酶的强烈结合，证实了三元复合物的形成；在 3 μM 浓度下处理 12 小时可显著增强同一细胞系中 KRASG12D 的多聚泛素化[1]。
ZJK-807 (0.1-3 μM，24 小时) 可显著诱导 AsPC-1 (KRASG12D) 细胞中 KRAS 蛋白的浓度依赖性降解，但在其他 KRAS 突变细胞系中未观察到明显的 KRAS 蛋白降解[1]。
ZJK-807 (1.5-10000 nM，24 小时) 对 KRASG12D 表现出强效且浓度依赖性的降解作用，在 AsPC-1 细胞中 DC50 值为 79.5 nM (DMAX 92%)，在 GP2D 细胞中为 130.8 nM (DMAX 92%)，在 AGS 细胞中为 313.8 nM (DMAX 70%)，但不会诱导 AsPC-1 和 GP2D 细胞中 CK1α 或 GSPT1 的浓度依赖性降解[1]。
ZJK-807 (3 或 5 天) 对 KRASG12D 突变细胞系表现出抗增殖作用，在 AsPC-1 细胞中 IC50 值为 219.6 nM，在 AGS 细胞中为 273.5 nM，在 GP2D 细胞中为 1.1 μM。在野生型或其他 KRAS 突变细胞系或正常细胞系 HEK-293T 中未观察到明显的抗增殖活性[1]。
ZJK-807 (0.01-10 μM，24 小时) 即使在存在继发突变的情况下，也能以浓度依赖的方式降低 AGS 细胞中 KRASG12D 蛋白的水平。尽管其抑制效力有所降低，但仍能抑制携带 KRASG12D/95mut 或 KRASG12D/96mut 的 Ba/F3 细胞[1]。
ZJK-807 显著改变了转录组，在 RAS/MAPK 信号通路中表现出明显的下调和通路富集[1]。

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

ZJK-807 相关抗体:

Western Blot Analysis[1]

Cell Line: AsPC-1 cells
Concentration: 10 μM
Incubation Time: 0.5 h, 1 h, 2 h, 4 h, 8 h, 12 h, 24 h
Result: Resulted in a time-dependent reduction in KRASG12D levels and a significant decrease in pERK levels, observed as early as 2 h post-treatment, indicating sustained downregulation of the ERK pathway for up to 24 h in AsPC-1 cells.

Western Blot Analysis[1]

Cell Line: AsPC-1 cells
Concentration: 3 μM
Incubation Time: 12 h
Result: KRASG12D degradation was significantly alleviated by the competitive binding of MRTX1133 (1 μM) and thalidomide (40 μM).
Pretreatment with the NEDD8-activating E1 enzyme inhibitor MLN4924 (1 μM) or the proteasome inhibitor MG132 (3 μM) for 4 h effectively attenuated the degradation of KRASG12D protein in AsPC-1 cells.

Western Blot Analysis[1]

Cell Line: AGS cells
Concentration: 0.01 μM, 0.1 μM, 1 μM, 10 μM
Incubation Time: 24 h
Result: Reduced KRASG12D protein levels in a concentration-dependent manner, even in the presence of secondary mutations in AGS cells.
体内研究
(In Vivo)

ZJK-807 (Compound A11) (30 mg/kg，皮下注射，每日一次，持续 28 天) 在体内能有效抑制 AsPC-1 异种移植小鼠体内 KRASG12D 驱动的肿瘤生长，并通过降解 KRASG12D 蛋白发挥其抗肿瘤作用，同时还表现出良好的耐受性[1]。

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

Animal Model: 5.0 × 106 AsPC-1 cells suspended in 100 μL of PBS and Matrigel were subcutaneously implanted into the right flank of male BALB/c nude mice[1].
Dosage: 30 mg/kg
Administration: S.c., once daily for 28 days
Result: Tumor growth was significantly inhibited with a 47% reduction in tumor volume compared to the Vehicle group.
No significant decrease in body weight was observed.
The tumor weight was significantly lower than that in the Vehicle group.
KRASG12D protein expression level was significantly reduced.
分子量

906.98

Formula

C50H48F2N10O5
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

ZJK-807 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • 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:

ZJK-807ZJK807ZJK 807PROTACsRasp38 MAPKTNF ReceptorTumor Necrosis Factor ReceptorTNFRKRASG12DCRBNCereblonProtein DegradationTernary Complex FormationDrug ResistanceInhibitorinhibitorinhibit

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