2. Protein Tyrosine Kinase/RTK JAK/STAT Signaling
  3. DYRK EGFR
  4. Dyrk1A-IN-16

Dyrk1A-IN-16 是一种选择性、可透过血脑屏障的 ATP 竞争性 DYRK 抑制剂，其对 Dyrk1A 的 IC50 为 53 nM。Dyrk1A-IN-16 在广泛的激酶组中 (对 DYRK 激酶具有特异性) 表现出纳摩尔级效力和高选择性。Dyrk1A-IN-16 在体外可损害神经球的自我更新能力、细胞侵袭能力以及 EGFR 的稳定性。Dyrk1A-IN-16 在体内能抑制肿瘤生长并延长生存期。Dyrk1A-IN-16 在胶质母细胞瘤的研究中具有应用潜力。

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Dyrk1A-IN-16

Dyrk1A-IN-16 Chemical Structure

CAS No. : 2805339-74-4

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Dyrk1A-IN-16 相关抗体

Top Publications Citing Use of Products

查看 DYRK 亚型特异性产品:

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DYRK1 DYRK2 DYRK3 DYRK4 HIPK PRP4

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Dyrk1A-IN-16 is a selective, brain-penetrant and ATP-competitive Dyrk1A inhibitor with a IC50 of 53 nM. Dyrk1A-IN-16 displays high selectivity across a broad kinase panel (specific for DYRK kinases) with nanomolar potency. Dyrk1A-IN-16 impairs neurosphere self-renewal, cell invasion, and EGFR stability in vitro. Dyrk1A-IN-16 inhibits tumor growth and prolongs survival in vivo. Dyrk1A-IN-16 has potential for glioblastoma (GBM) research[1].

IC50 & Target[1]

DYRK1A

50 nM (IC50)

体外研究
(In Vitro)

Dyrk1A-IN-16 (compound FC-3) (0-100 nM) 为可逆的 ATP 竞争性抑制剂，其抑制作用可被更高浓度的 ATP 所克服[1]。
Dyrk1A-IN-16 (5-20 µM，处理 72 小时) 在 GBM 细胞系 U87MG 中主要靶向 DYRK1A[1]。
Dyrk1A-IN-16 (5-10 µM，处理 24 小时) 通过对 DYRK1A 的靶上作用，抑制 GBM 细胞系 U87MG 的侵袭能力[1]。
Dyrk1A-IN-16 (1-10 µM，处理 20 小时) 能加速 EGFR 去稳定化，从而在 EGFR 依赖的胶质母细胞瘤细胞系 U87MG 中导致其溶酶体降解[1]。

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

Dyrk1A-IN-16 相关抗体:

Cell Proliferation Assay[1]

Cell Line: GBM cell line U87MG
Concentration: 5, 10, 20 µM
Incubation Time: 72 h
Result: Was resistant to the mutant but the mutant retained its kinase activity, when DYRK1A-knockout clones were Rescued with the DYRK1A wild-type and the F238L-M240R double mutant[1].
Dyrk1a-in-16 reduced neurosphere size and number only in the populations rescued with wild-type DYRK1A, but not in those expressing the F238L-M240R mutant[1].
Not decreased neurosphere proliferation, unlike the DYRK1A knockout clones in DYRK2 and DYRK3-knockout clones[1].

Cell Invasion Assay[1]

Cell Line: GBM cell line U87MG
Concentration: 5 or 10 µM
Incubation Time: 24 h
Result: Reduced invasion of U87MG cells in a dose-dependent manner[1].
Did not observe any significant reduction of invasion in cells rescued with the DYRK1A F238L-M240R mutant as opposed to rescue with DYRK1A wild type[1].

Western Blot Analysis[1]

Cell Line: GBM cell line U87MG
Concentration: 1 or 10 µM
Incubation Time: 20 h
Result: Observed a reduction in total EGFR and ERK phosphorylation levels in U87MG DYRK1A-knockout cell lines.
Induced the accumulation of EGFR when lysosomal degradation was inhibited by BaFA1.
Increased EGFR degradation, a phenotype also observed in DYRK1A-knockout cells.
体内研究
(In Vivo)

Dyrk1A-IN-16 (2 mg/kg，腹腔注射，每日一次持续 30 天) 在由 U87MG 或 U87MG-DYRK1A KO 细胞 (1×106 个) 诱导的皮下异种移植小鼠模型中抑制肿瘤生长，延长动物存活期[1]。

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

Animal Model: U87MG or U87MG-DYRK1A KO cells (1 x 106) induced- NuJ nude mice[1]
Dosage: 2 mg/kg
Administration: i.p., daily for 30 days
Result: Observed the tumors substantially smaller.
Failed to develop any tumors in the the DYRK1A-knockout line cohort.
Had markedly lower EGFR levels.
分子量

303.29

Formula

C14H9NO5S
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

Dyrk1A-IN-16 相关分类

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Keywords:

Dyrk1A-IN-162805339-74-4DYRKEGFRDual specificity tyrosine phosphorylation regulated kinaseDual specificity tyrosine regulated kinaseEpidermal growth factor receptorErbB-1HER1blood-brain barrier-penetrantglioblastomaInhibitorinhibitorinhibit

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