2. Cell Cycle/DNA Damage Cytoskeleton
  3. PAK Cdc42-binding kinase
  4. Rac/Cdc42-IN-1

Rac/Cdc42-IN-1 是口服 Rac/Cdc42 抑制剂 MBQ-167 (HY-112842) 的体内主要 I 相代谢产物，是一种选择性 Rac 抑制剂。Rac/Cdc42-IN-1 通过阻断 Rac1 的 GTP 结合活化发挥作用，靶向下游 PAK1/2/3 的 Thr423/Thr402/Thr436 和 Ser141/Ser144/Ser154 自磷酸化，且抑制效果优于 MBQ-167。Rac/Cdc42-IN-1 能显著抑制细胞迁移，在 HER2 + 乳腺癌小鼠模型中抑制肿瘤生长和肺、肝、肾远端转移。Rac/Cdc42-IN-1 可用于转移性乳腺癌的靶向研究。

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Rac/Cdc42-IN-1

Rac/Cdc42-IN-1 Chemical Structure

CAS No. : 2143950-05-2

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Rac/Cdc42-IN-1 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

Rac/Cdc42-IN-1, the major phase I metabolite of the oral Rac/Cdc42 inhibitor MBQ-167 (HY-112842) in vivo, is a selective Rac inhibitor. Rac/Cdc42-IN-1 functions by blocking the GTP-binding activation of Rac1, targeting the autophosphorylation of Thr423/Thr402/Thr436 and Ser141/Ser144/Ser154 in downstream PAK1/2/3, with an inhibitory effect superior to that of MBQ-167. Rac/Cdc42-IN-1 significantly inhibits cell migration, and suppresses tumor growth and distant metastasis to the lung, liver and kidney in HER2+ breast cancer mouse models. Rac/Cdc42-IN-1 can be used for targeted research on metastatic breast cancer[1].

体外研究
(In Vitro)

Rac/Cdc42-IN-1 (M6) (500 nM；72 h) 对三阴性乳腺癌细胞 MDA-MB-231、MDA-MB-468 和 HER2 过表达乳腺癌细胞 HER2-BM 的细胞活力无显著影响[1]。
Rac/Cdc42-IN-1 (0.001-1000 nM；120 h) 对正常人乳腺上皮细胞 HMEC 的细胞活力无显著毒性[1]。
Rac/Cdc42-IN-1 (15-1000 nM；72 h) 对 HER2-BM 细胞的细胞活力无显著影响[1]。
Rac/Cdc42-IN-1 (500 nM；48 h) 未显著诱导 MDA-MB-231、MDA-MB-468 和 HER2-BM 细胞的凋亡 (caspase-3/7 活性无明显变化)[1]。
Rac/Cdc42-IN-1 (250 nM；24 h) 显著抑制 HER2-BM 细胞中 Group 1 PAK (PAK1/2/3) 在 Thr423/Thr402/Thr436 和 Ser141/Ser144/Ser154 位点的自磷酸化，且抑制效果优于母药 MBQ-167 (HY-112842)[1]。
Rac/Cdc42-IN-1 (25 nM，250 nM；24 h) 抑制 HER2-BM 细胞迁移[1]。

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

Rac/Cdc42-IN-1 相关抗体:

Apoptosis Analysis[1]

Cell Line: MDA-MB-231, MDA-MB-468, HER2-BM
Concentration: 500 nM
Incubation Time: 48 h
Result: Did not significantly alter caspase-3/7 activity in MDA-MB-231, MDA-MB-468 and HER2-BM cells, indicating no obvious induction of apoptosis, whereas MBQ-167 (HY-112842) significantly induced apoptosis at the same concentration.
体内研究
(In Vivo)

Rac/Cdc42-IN-1 (M6) (10 mg/kg；腹腔注射；每周 5 次；共 8 周) 在雌性严重联合免疫缺陷 (SCID) 小鼠 HER2 的乳腺癌原位移植瘤模型中，可抑制约 90% 的肿瘤生长，并使肺、肝、肾的远端转移减少约 90%[1]。

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

Animal Model: Female Severe Combined Immunodeficiency (SCID) mice bearing orthotopic GFP-HER2-BM breast cancer tumors[1]
Dosage: 10 mg/kg
Administration: i.p.; 5 times per week; for 8 consecutive weeks
Result: Significantly inhibited tumor growth by approximately 90% compared with the vehicle-treated group.
Also prevented the development of distal metastases to the lungs, livers, and kidneys by about 90%, showing comparable antitumor and antimetastatic efficacy to the parent compound MBQ-167 (HY-112842) at the same dosage.
分子量

310.35

Formula

C20H14N4
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

Rac/Cdc42-IN-1 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:

Rac/Cdc42-IN-12143950-05-2PAKCdc42-binding kinasep21 activated kinasesmyotonic dystrophy kinase-related Cdc42-binding kinasesMRCKRacCdc42Inhibitorinhibitorinhibit

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