2. Cell Cycle/DNA Damage
  3. Eukaryotic Initiation Factor (eIF)
  4. CMLD012612

CMLD012612 是一类含有异羟肟酸酯基团的 amidino-rocaglate，并且是有效的真核生物起始因子 4A (eIF4A) 抑制剂。CMLD012612 抑制细胞翻译，对 NIH/3T3 细胞具有细胞毒性，IC50 值为 2 nM。CMLD012612 通过修饰RNA解旋酶 eIF4A 来抑制真核细胞翻译起始，并具有有效的抗肿瘤活性。

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CMLD012612 Chemical Structure

CMLD012612 Chemical Structure

CAS No. : 2368900-35-8

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规格 价格 是否有货
1 mg ￥16500
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CMLD012612 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CMLD012612 is an amidino-rocaglate containing a hydroxamate group and is a potent eukaryotic initiation factor 4A (eIF4A) inhibitor. CMLD012612 inhibits cell translation and is cytotoxic to NIH/3T3 cells with an IC50 value of 2 nM. CMLD012612 inhibits eukaryotic translation initiation by modifying the behavior of the RNA helicase (eIF4A) and possesses potent anti-neoplastic activity[1].

IC50 & Target

eIF4

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
NIH3T3 IC50
2 nM
Compound: 10; CMLDO12612
Cytotoxicity against mouse NIH/3T3 cells assessed as reduction in cell viability incubated for 4 days by SRB assay
Cytotoxicity against mouse NIH/3T3 cells assessed as reduction in cell viability incubated for 4 days by SRB assay
[PMID: 33592144]
体外研究
(In Vitro)

CMLD012612 对 NIH/3T3 细胞的 IC50 为 2 nM。CMLD012612 的主要作用机制依赖于 eIF4A1，因为 eIF4A1em1jp 细胞的耐药性至少是亲本 NIH/3T3 细胞的 10 倍。在较高浓度下观察到的 eIF4A1em1jp 细胞对 CMLD012612 的敏感性可能是由于细胞中存在野生型 eIF4A2[1]。

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

CMLD012612 相关抗体:
体内研究
(In Vivo)

CMLD012612 (0.5 mg/kg；腹腔注射；持续 3 小时；雌性 C57BL/6 小鼠) 处理在注射后 3 小时有效抑制肝脏多核糖体，表明对蛋白质合成具有抑制活性[1]。
当对携带 myr-Akt/Em-Myc 淋巴瘤的小鼠给药时，CMLD012612 (0.2 mg/kg；腹膜内注射；每天；持续 5 天；雌性 C57BL/6 小鼠) 处理与多柔比星有效协同作用，导致肿瘤完全消失[1]。

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

Animal Model: Female C57BL/6 mice[1]
Dosage: 0.5 mg/kg
Administration: Intraperitoneal injection; for 3 hours
Result: Effectively suppressed liver polysomes 3 hours after injection.
分子量

559.61

Formula

C31H33N3O7
CAS 号
性状

固体

颜色

White to light yellow

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
纯度 & 产品资料
参考文献

CMLD012612 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?

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Keywords:

CMLD0126122368900-35-8CMLD 012612CMLD-012612Eukaryotic Initiation Factor (eIF)Inhibitorinhibitorinhibit

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