2. Protein Tyrosine Kinase/RTK Metabolic Enzyme/Protease
  3. SHP2 Phosphatase
  4. GS-493

GS-493 是一种选择性的酪氨酸磷酸酶 SHP2 (PTPN11) 抑制剂，IC50 为 71 nM，对 SHP2 的活性比 SHP1 和 PTP1B 高 29 倍和 45 倍。 GS-493 抑制细胞运动和癌细胞生长。GS-493 具有抗肿瘤活性。

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GS-493 Chemical Structure

GS-493 Chemical Structure

CAS No. : 1710337-31-7

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GS-493 相关抗体

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MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

GS-493 is a selective protein tyrosine phosphatase SHP2 (PTPN11) inhibitor with an IC50 of 71 nM. GS-493 is 29- and 45-fold more active toward SHP2 than related SHP1 and PTP1B. GS-493 blocks cellular motility and growth of cancer cells. Antitumor activity[1].

IC50 & Target

IC50: 71 nM (SHP2); 2.08 μM (SHP1); 3.17 μM (PTP1B)[1]
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HPAF-II IC50
3.4 μM
Compound: 3; GS493
Inhibition of HGF-induced cell scattering in human HPAF-II cells incubated for 1 hr by Hoechst staining based assay
Inhibition of HGF-induced cell scattering in human HPAF-II cells incubated for 1 hr by Hoechst staining based assay
[PMID: 33210922]
体外研究
(In Vitro)

GS-493 (0.0625-10 μM) blocks hepatocyte growth factor (HGF)-stimulated epithelial-mesenchymal transition of human pancreatic adenocarcinoma (HPAF) cells[1].
GS-493 (40 μM, a couple of days) blocks growth of the human NSCL cancer cell line LXFA 526L in soft agar and decreases the number of tumor cell colonies to 32%[1].

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

GS-493 相关抗体:
体内研究
(In Vivo)

GS-493 (46 mg/kg; i.p.; daily for 27 days) inhibits tumor growth significantly in a murine xenograft model[1].

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

Animal Model: Nude mouse xenograft model (strain NMRI nu/nu mice)
Dosage: 46 mg/kg (45.93 mg in 3 mL DMSO per kg)
Administration: i.p.; daily for 27 days
Result: Inhibited tumor growth significantly.
分子量

510.44

Formula

C21H14N6O8S
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

GS-493 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:

GS-4931710337-31-7GS493GS 493SHP2PhosphataseSrc homology phosphatase 2PTPN11selectivetumor growthtranslationtyrosine phosphataseHGFHPAFInhibitorinhibitorinhibit

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