1. Cell Cycle/DNA Damage
  2. DNA/RNA Synthesis
  3. VARS1-IN-1

VARS1-IN-1 是一种缬氨酰-tRNA 合成酶 (VARS1) 抑制剂,其 Kd 值为 0.213 μM。VARS1-IN-1 能抑制 VARS1 的 tRNA 氨基酰化活性,降低缬氨酸 tRNA 的荷电水平,并减少总蛋白合成速率。VARS1-IN-1 可抑制 PC3 前列腺癌异种移植模型中侵袭性肿瘤的生长和细胞增殖。VARS1-IN-1 可用于前列腺癌研究。

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VARS1-IN-1

VARS1-IN-1 Chemical Structure

CAS No. : 428830-84-6

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

VARS1-IN-1 is a valyl-tRNA synthetase (VARS1) inhibitor with a Kd of 0.213 μM. VARS1-IN-1 suppresses VARS1’s tRNA aminoacylation activity, reduces charged levels of valine tRNAs and redues total protein synthesis rate. VARS1-IN-1 suppresses aggressive tumor growth and cell proliferation in PC3 prostate cancer xenograft models. VARS1-IN-1 can be used for the research of prostate cancer[1].

体外研究
(In Vitro)

VARS1-IN-1 (Compound 2701) (10 µM;2 天) 干扰 VARS1 的 tRNA 氨基酰化活性,但不影响其表达,导致前列腺癌细胞中荷电 tRNA-Val 与总 tRNA-Val 比例降低[1]
VARS1-IN-1 (10 µM;2 天) 可降低 PC3 细胞中的总蛋白合成速率[1]

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

体内研究
(In Vivo)

VARS1-IN-1 (Compound 2701) (15 mg/kg;腹腔注射;每隔一天一次,持续 20 天) 可抑制雄性 BALB/c-nu 裸鼠 PC3 前列腺癌异种移植模型的肿瘤生长和细胞增殖[1]

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

Animal Model: BALB/c-nu nude mice with PC3 xenograft (male, 6-7 weeks old)[1]
Dosage: 15 mg/kg
Administration: i.p.; once every other day for 20 days
Result: Inhibited tumor growth with significant reduction in tumor weight compared to DMSO control.
Decreased cell proliferation index as shown by Ki-67 immunohistochemical staining.
分子量

385.44

Formula

C21H15N5OS

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
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  • 稀释计算器

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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)
× = ×
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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.

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VARS1-IN-1
目录号:
HY-180995
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