2. Protein Tyrosine Kinase/RTK
  3. DYRK
  4. GNF2133

GNF2133 是一种有效的、选择性的、具有口服活性的 DYRK1A 抑制剂，对 DYRK1A 和 GSK3β 的 IC50 分别为 0.0062、>50 µM。GNF2133 对大鼠和人原代 β 细胞具有良好的增殖能力和功效。GNF2133 显著提高葡萄糖处理能力并增加胰岛素分泌。GNF2133 具有研究1型糖尿病的潜力。

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GNF2133 Chemical Structure

GNF2133 Chemical Structure

CAS No. : 2561414-56-8

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥3824
In-stock
1 mg ￥1600
In-stock
5 mg ￥4000
In-stock
10 mg ￥6000
In-stock
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Customer Review

Other Forms of GNF2133:

GNF2133 相关抗体

Top Publications Citing Use of Products

查看 DYRK 亚型特异性产品:

查看所有亚型
DYRK1 DYRK2 DYRK3 DYRK4

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

GNF2133 is a potent, selective and orally active DYRK1A inhibitor with IC50s of 0.0062, >50 µM for DYRK1A and GSK3β, respectively. GNF2133 shows good proliferation potency and efficacy on rat and human primary β-cell. GNF2133 significantly improves glucose disposal capacity and increases insulin secretion. GNF2133 has the potential for the research of type 1 diabetes[1].

IC50 & Target[1]

DYRK1

 

DYRK1A

0.0062 μM (IC50)

GSK3β

>50 μM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO IC50
> 30 μM
Compound: 13g; GNF2133
Displacement of [3H]dofetilide from human ERG expressed in CHO cells incubated for 90 mins by microbeta scintillation counting method
Displacement of [3H]dofetilide from human ERG expressed in CHO cells incubated for 90 mins by microbeta scintillation counting method
[PMID: 32077280]
Pancreatic beta cell EC50
0.21 μM
Compound: 13g; GNF2133
Induction of cell proliferation in human beta cells incubated for 96 hrs by EdU incorporation assay
Induction of cell proliferation in human beta cells incubated for 96 hrs by EdU incorporation assay
[PMID: 32077280]
Pancreatic beta cell EC50
0.4 μM
Compound: 13g; GNF2133
Induction of cell proliferation in rat beta cells incubated for 96 hrs by EdU incorporation assay
Induction of cell proliferation in rat beta cells incubated for 96 hrs by EdU incorporation assay
[PMID: 32077280]
Sf21 IC50
0.0062 μM
Compound: 13g; GNF2133
Inhibition of recombinant human N-terminal GST-tagged DYRK1A (1 to 763 residues) expressed in Sf21 cells using Ulight-glycogen synthase as substrate incubated for 60 mins by TR-FRET LANCE method
Inhibition of recombinant human N-terminal GST-tagged DYRK1A (1 to 763 residues) expressed in Sf21 cells using Ulight-glycogen synthase as substrate incubated for 60 mins by TR-FRET LANCE method
[PMID: 32077280]
Sf9 IC50
> 50 μM
Compound: 13g; GNF2133
Inhibition of recombinant human His/GST-tagged GSK3beta (2 to 433 residues) expressed in baculovirus infected Sf9 cells using Ulight-glycogen synthase peptide as substrate incubated for 30 mins by TR-FRET LANCE method
Inhibition of recombinant human His/GST-tagged GSK3beta (2 to 433 residues) expressed in baculovirus infected Sf9 cells using Ulight-glycogen synthase peptide as substrate incubated for 30 mins by TR-FRET LANCE method
[PMID: 32077280]
体内研究
(In Vivo)

GNF2133 (30 mg/kg; p.o.) shows good oral absorption with oral bioavailability of 22.3%[1].
GNF2133 (30 mg/kg; p.o.; once a day for 5 days) shows the ability to proliferate β-cells in vivo[1].
GNF2133 (3, 10, 30 mg/kg) significantly improves glucose disposal capacity and increased insulin secretion in RIP-DTA mice[1].
Pharmacokinetic Parameters of GNF2133 in CD-1 mice[1].

plasma (iv) plasma (po) pancreas (po)
CL (mL/min/kg) 23.5 / /
Vss (L/kg) 11 / /
AUC (h·nM) 3268 10974 144420
Cmax(nM) 1977 1675 13319
tmax<(h) 0.03 3.0 3.0
Clast(nM) 36.6 19 1324
t1/2<(h) 6.6 3.4 6.6
F (%) / 22.3 /
CD-1 mice; 30 mg/kg; p.o.[1].

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

Animal Model: CD-1 mice[1]
Dosage: 30 mg/kg
Administration: P.o.
Result: Showed good oral absorption and moderate plasma exposure with oral bioavailability of 22.3%.
Animal Model: Wistar Han rat[1]
Dosage: 30 mg/kg (0.5% methylcellulose + Tween-80)
Administration: P.o.; once a day for 5 days
Result: Increased cyclin D1 levels and overall cell density, and increased in cell proliferation marker Ki67 and insulin.
Animal Model: Diphtheria toxin A (RIP-DTA) mice[1]
Dosage: 3, 10, 30 mg/kg (20 mg/kg doxycycline (Dox) for 5 days)
Administration: P.o., once a day for 35 days
Result: Significantly improves glucose disposal capacity and increased insulin secretion.
分子量

434.53

Formula

C24H30N6O2
CAS 号
性状

固体

颜色

Off-white to pink

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 4 mg/mL (9.21 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.3013 mL 11.5067 mL 23.0134 mL
5 mM 0.4603 mL 2.3013 mL 4.6027 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 98.49%

COA (268 KB) HNMR (144 KB) RP-HPLC (163 KB)

产品使用指南 (1538 KB)
参考文献

GNF2133 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3013 mL 11.5067 mL 23.0134 mL 57.5334 mL
5 mM 0.4603 mL 2.3013 mL 4.6027 mL 11.5067 mL
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:

GNF21332561414-56-8GNF 2133GNF-2133DYRKDual specificity tyrosine phosphorylation regulated kinaseDual specificity tyrosine regulated kinaseorally activeβ-cellglucose disposalinsulin secretionCD-1 miceRIP-DTA miceInhibitorinhibitorinhibit

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目录号：
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