2. Metabolic Enzyme/Protease MAPK/ERK Pathway GPCR/G Protein PI3K/Akt/mTOR
  3. Acyltransferase Ras Akt
  4. Rac1-IN-5

Rac1-IN-5 是一种特异性的 RAC1 蛋白可逆抑制剂 (KD= 30 nM)。Rac1-IN-5 可与鸟嘌呤核苷酸在 RAC 蛋白上特异性结合竞争，有效阻断 RAC1 活性和 RAC1 依赖性细胞功能。Rac1-IN-5 在体内表现出抗肿瘤转移作用，并且可以提高生存率。Rac1-IN-5 可用于研究侵袭性癌症如三阴性乳腺癌，结肠癌。

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Rac1-IN-5

Rac1-IN-5 Chemical Structure

CAS No. : 694515-65-6

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Rac1-IN-5 相关抗体

Top Publications Citing Use of Products

查看 Acyltransferase 亚型特异性产品:

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ACAT1 ACAT2 MGAT2 ACAT

查看 Ras 亚型特异性产品:

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K-Ras H-Ras N-Ras Ras

查看 Akt 亚型特异性产品:

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Akt Akt1 Akt2 Akt3

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Rac1-IN-5 is a specific, reversible inhibitor of RAC1 (KD = 30 nM). Rac1-IN-5 competes with guanine nucleotides for specific binding to RAC proteins, effectively blocking RAC1 activity and RAC1-dependent cellular functions. Rac1-IN-5 exhibits anti-tumor metastasis effects in vivo and can improve survival. Rac1-IN-5 can be used to study invasive cancers such as triple-negative breast cancer and colon cancer[1].

体外研究
(In Vitro)

Rac1-IN-5 (Compound A41) (10 μM，1 小时) 可阻断 EGF 刺激的 NIH/3T3 成纤维细胞中的 RAC1 激活及其依赖性功能[1]。
Rac1-IN-5 (10 μM) 可降低表达 RAC 野生型 (RAC1 WT) 或 RAC1 突变体 (RAC1 P29S 和 RAC1b) 的 NIH-3T3 成纤维细胞中 RAC P29S 和 RAC1b 的活性[1]。
Rac1-IN-5 (0.01-10 μM) 可降低 RAC1-GTP 水平、AKT 的过度激活和细胞球的迁移区域，并抑制 TNBC MDA-MB-468 荧光素酶 (Luc) 细胞中的集落形成 (IC50 = 2.1 μM)。[1]。
Rac1-IN-5 (10 μM) 在人乳腺 CAF 球体中具有抗侵袭特性[1]。

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

Rac1-IN-5 相关抗体:

Western Blot Analysis[1]

Cell Line: MDA-MB-468 Luc cells
Concentration: 10 μM
Incubation Time: 1 h
Result: Reduced AKT overactivation, while p44/42 activation remained unchanged.
体内研究
(In Vivo)

Rac1-IN-5 (Compound A41) (25 mg/kg，腹腔注射，每日一次，4 周) 可预防小鼠 TNBC 模型中的癌细胞转移[1]。
Rac1-IN-5 (25 mg/kg，腹腔注射，每日一次，15 天) 可预防 CT26 细胞异种移植 BALB/c 雌性小鼠模型中侵袭性癌症的转移[1]。

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

Animal Model: TNBC (4 million MDA-MB-468Luc cells) xenograft NMRI nude mice (5-week-old) model[1]
Dosage: 25 mg/kg
Administration: i.p., once a day, 4 weeks
Result: Reduced primary tumor regeneration, secondary tumors in the femur, lungs, kidneys, ovaries, and uterus, reduced ex vivo luminescence intensity in the ovaries and uterus.
Animal Model: TNBC (4 million MDA-MB-468Luc cells) xenograft BALB/c female mice (7-8-week-old) model[1]
Dosage: 25 mg/kg
Administration: i.p., once a day, 4 weeks
Result: Reduced the frequency of primary tumor regrowth and metastasis, improving survival rates.
Animal Model: CT26 cells (1x106) xenograft BALB/c female mice (7-8-week-old) model[1]
Dosage: 25 mg/kg
Administration: i.p., once a day, 15 days
Result: Reduced the development of lung metastases and liver metastases, improving survival rates.
分子量

486.60

Formula

C24H26N2O5S2
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

Rac1-IN-5 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:

Rac1-IN-5694515-65-6AcyltransferaseRasAktDiacylglycerol acyltransferaseDiglyceride acyltransferaseacyl-CoA:cholesterol acyltransferasemono- acylglycerol acyltransferasePKBProtein kinase BInhibitorNIH/3T3 fibroblastsMDA-MB-468Luc cellsCT26 cellsBALB/c micetriple-negative breast cancercolon cancerinhibitorinhibit

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