2. Epigenetics PI3K/Akt/mTOR MAPK/ERK Pathway
  3. AMPK p38 MAPK
  4. OICR19451

OICR19451 是一种具有口服活性的双重 NUAK1/NUAK2 与 MARK2/MARK3 激酶抑制剂，对 NUAK1 和 NUAK2 的 IC50 为 12 和 10 nM，对 MARK2 和 MARK3 的 IC50 为 101 和 124 nM。OICR19451 可调控 Hippo 信号通路，提高 YAP 的磷酸化水平，增强 YAP/TAZ 的细胞质定位，并抑制促癌基因的表达。OICR19451 可抑制癌细胞生长、减少转移、促进肿瘤包膜形成，并在原位乳腺癌模型中提高小鼠存活率。OICR19451 可用于三阴性乳腺癌的相关研究。

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OICR19451

OICR19451 Chemical Structure

CAS No. : 2803349-61-1

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OICR19451 相关抗体

Top Publications Citing Use of Products

查看 AMPK 亚型特异性产品:

查看所有亚型
NUAK1 NUAK2 AMPK AMPK α1β1γ1 AMPK α2β1γ1 AMPK α1β2γ1 AMPK α2β2γ1 BRSK1 BRSK2 HUNK AMPKα

查看 p38 MAPK 亚型特异性产品:

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p38 MAPK Akt1 p38α p38β MAPK13 p38δ p38γ

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

OICR19451 is an orally active dual NUAK1/NUAK2 and MARK2/MARK3 kinase inhibitor, with IC50 values of 12 nM and 10 nM against NUAK1 and NUAK2, and 101 nM and 124 nM against MARK2 and MARK3, respectively. OICR19451 modulates the Hippo signaling pathway, increases the phosphorylation level of YAP, enhances the cytoplasmic localization of YAP/TAZ, and inhibits the expression of oncogenes. OICR19451 inhibits cancer cell growth, reduces metastasis, promotes tumor capsule formation, and improves mouse survival in an orthotopic breast cancer model. OICR19451 can be used for research related to triple-negative breast cancer[1].

IC50 & Target[1]

NUAK1

12 nM ()

NUAK2

10 nM ()

体外研究
(In Vitro)

OICR19451 可调控 MDA-MB-231 细胞中的 Hippo 通路活性，促进 YAP 磷酸化 (EC50 = 125 nM)，诱导 YAP/TAZ 定位于细胞质 (EC50 = 144 nM)，并抑制细胞生长 (EC50 = 202 nM)[1]。

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

OICR19451 相关抗体:
体内研究
(In Vivo)

OICR19451 (30-60 mg/kg；口服；每日一次；连续 14 天) 可抑制肿瘤生长、减少转移、降低肿瘤 YAP/TAZ 水平，并在原位转移性乳腺癌小鼠模型中延长生存期[1]。

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

Animal Model: NOD/SCID-gamma (NSG) (female, 10 weeks old)[1]
Dosage: 30 mg/kg; 60 mg/kg
Administration: p.o.; daily; 14 days
Result: Inhibited tumor growth relative to controls.
Prolonged survival relative to controls.
Reduced metastasis to peritoneal space (mesentery) and liver relative to controls.
Decreased YAP/TAZ protein levels in tumors (60 mg/kg group).
Induced widespread tumor necrosis and collagenous tumor encapsulation.
Caused acceptable, reversible body weight loss with no gross behavioral or CNS-related side effects.
分子量

593.09

Formula

C26H31ClF2N8O2S
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

OICR19451 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:

OICR194512803349-61-1OICR 19451OICR-19451AMPKp38 MAPKAMP-activated protein kinaseYAPMARK2TAZNUAK1Caco-2NUAK2MDA-MB-231 cellsMARK3triple-negative breast cancerHippo pathwayInhibitorinhibitorinhibit

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