2. GPCR/G Protein MAPK/ERK Pathway Apoptosis PI3K/Akt/mTOR
  3. Ras Apoptosis PI3K Akt p38 MAPK
  4. pan-KRAS-IN-5

pan-KRAS-IN-5 是一种泛 KRAS 翻译抑制剂，靶向作用于 5′-UTR RNA G- 四链体 (rG4s)。pan-KRAS-IN-5 能与 KRAS rG4s 强结合并稳定其活性，抑制 KRAS 翻译，阻断 MAPK 和 PI3K-AKT 通路。pan-KRAS-IN-5 可诱导细胞周期停滞，促进 KRAS 驱动型癌细胞凋亡 (apoptosis)。pan-KRAS-IN-5 可抑制 KRAS 突变异种移植瘤的肿瘤生长和 KRAS 表达，可用于 KRAS 驱动型癌症的研究。

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pan-KRAS-IN-5

pan-KRAS-IN-5 Chemical Structure

CAS No. : 3027172-23-9

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规格 价格 是否有货
1 mg ￥1700
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5 mg ￥4250
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pan-KRAS-IN-5 相关抗体

Top Publications Citing Use of Products

查看 Ras 亚型特异性产品:

查看所有亚型
K-Ras H-Ras N-Ras Ras

查看 PI3K 亚型特异性产品:

查看所有亚型
PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

查看 Akt 亚型特异性产品:

查看所有亚型
Akt Akt1 Akt2 Akt3

查看 p38 MAPK 亚型特异性产品:

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p38 MAPK p38α p38β MAPK13 p38δ p38γ

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

pan-KRAS-IN-5 is a pan-KRAS translation inhibitor by targeting 5′-UTR RNA G-quadruplexes (rG4s). pan-KRAS-IN-5 strongly binds to and stabilizes KRAS rG4s, inhibits KRAS translation, and blocks the MAPK and PI3K-AKT pathways. pan-KRAS-IN-5 induces cell cycle arrest, prompts apoptosis in KRAS-driven cancer cells. pan-KRAS-IN-5 inhibits tumor growth and KRAS expression in KRAS-mutant xenograft. KRAS-IN-5 can be used for KRAS-driven cancer research[1].

体外研究
(In Vitro)

pan-KRAS-IN-5 (compound 15a) 与 KRAS rG4s 强结合，对 utr-z 的 KD 值为 2.3 μM，对 utr-1 的 KD 值为 0.9 μM[1]。
pan-KRAS-IN-5 (24 小时) 选择性杀死 KRAS 驱动型癌细胞，包括 MIA PaCa-2 (IC50 = 3.3 μM)、PANC-1 (IC50 = 5.6 μM)、HPAF-II (IC50 = 5.4 μM)、SW620 (IC50 = 5.1 μM)、HCT116 (IC50 = 4.0 μM) 和 NCI-H358 细胞 (IC50 = 4.8 μM)，但对 KRASWT 胶质母细胞瘤细胞或 KRASWT 正常细胞无明显的细胞毒性[1]。
Pan-KRAS-IN-5 (1.25-5.0 μM，0-48 小时) 可抑制 PANC-1、MIA PaCa-2 和 NCI-H358 细胞中的 KRAS 蛋白表达，且不改变 KRAS mRNA 水平[1]。
pan-KRAS-IN-5 (1.25-5.0 μM，0-24 小时) 以剂量和时间依赖性的方式抑制 MEK、ERK、AKT 和 mTOR 的磷酸化[1]。
pan-KRAS-IN-5 (0.32-1.25 μM，10 天) 可抑制 MIA PaCa-2 细胞的增殖[1]。
pan-KRAS-IN-5 (1.25-5.0 μM，24 小时) 可诱导 MIA PaCa-2 细胞剂量依赖性 G2/M 期阻滞，并诱导 KRAS 突变型 MIA PaCa-2 癌细胞中 caspase 3 的裂解[1]。

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

pan-KRAS-IN-5 相关抗体:

Apoptosis Analysis[1]

Cell Line: MIA PaCa-2 cells
Concentration: 1.25, 2.5, and 5.0 μM
Incubation Time: 24 h
Result: Decreased Caspase-3 and increased CL- Caspase-3 leves in MIA PaCa-2 cells.

Cell Cycle Analysis[1]

Cell Line: MIA PaCa-2 cells
Concentration: 1.25, 2.5, and 5.0 μM
Incubation Time: 24 h
Result: Induced G2/M phase arrest in MIA PaCa-2 cells dose-dependently.

Cell Proliferation Assay[1]

Cell Line: MIA PaCa-2 cells
Concentration: 0.32, 0.63, and 1.25 μM
Incubation Time: 10 days
Result: Almost completely inhibited the proliferation of MIA PaCa-2 cells at the concentration of 1.25 μM.

Western Blot Analysis[1]

Cell Line: MIA PaCa-2 cells
Concentration: 1.25, 2.5, and 5.0 μM
Incubation Time: 0, 6, 12, and 24 h
Result: Reduced p-MEK, p-ERK, p-AKT and p-mTOR in MIA PaCa-2 cells in a dose-dependent manner.
Decreased p-MEK, p-ERK, p-AKT and p-mTOR in MIA PaCa-2 cells in a time-dependent manner.
体内研究
(In Vivo)

pan-KRAS-IN-5 (2.5 和 5.0 mg/kg，腹腔注射，每日给药，持续 18 天) 抑制肿瘤生长并降低 KRAS 蛋白表达，但不影响 KRAS 突变 MIA PaCa-2 异种移植模型中的总 KRAS mRNA 水平[1]。

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

Animal Model: Male BALB/C-nu/nu (4 weeks old) subcutaneously injected with MIA PaCa-2 cells[1]
Dosage: 2.5 and 5.0 mg/kg
Administration: i.p., every day for 18 days
Result: Inhibited tumor growth in a dose-dependent manner, with Tumor Growth Inhibition (TGI) of 62.0 % (2.5 mg/ kg) and 70.3 % (5.0 mg/kg).
Revealed no significant body weight loss in mice.
Exhibited no evident signs of toxicity in the anatomized viscera.
分子量

642.55

Formula

C31H36FIN4O2
CAS 号
性状

固体

颜色

Brown to black

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

纯度 & 产品资料
参考文献

pan-KRAS-IN-5 相关分类

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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:

pan-KRAS-IN-53027172-23-9RasApoptosisPI3KAktp38 MAPKPhosphoinositide 3-kinasePKBProtein kinase BTumorKRAS pan-KRASrG4s MAPK pathwayPI3K-AKT pathway KRAS-Driven Cancer Cellscycle arrest apoptosis MIA PaCa-2 cellspancreatic cancer cellscolorectal cancer cellslung cancer cellsInhibitorinhibitorinhibit

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