製品番号: HY-129492

GNF4877

1 Cited Publications

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Based on 1 publication(s) in Google Scholar

GNF4877 is a potent DYRK1A and GSK3β inhibitor with IC₅₀s of 6 nM and 16 nM, respectively, which leads to blockade of nuclear factor of activated T-cells (NFATc) nuclear export and increased β-cell proliferation (EC₅₀ of 0.66 μM for mouse β (R7T1) cells).

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純度: 99.82%
CAS 番号: 2041073-22-5
分子式: C₂₅H₂₇FN₆O₄
分子量:494.52

保管条件:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

GNF4877 構造式

CAS 番号: 2041073-22-5

容量

価格（税別）

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数量

Amount: USD 0.00

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- 体内実験
化学情報
Publications (1)
溶剤 & 溶解度
- 体外
純度とドキュメンテーション
参考文献
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target^[1]

GSK3β

16 nM (IC₅₀)

DYRK1A

6 nM (IC₅₀)

DYRK アイソフォーム固有の製品をすべて表示 :

GSK-3 アイソフォーム固有の製品をすべて表示 :

Cellular Effect

Cell Line	Type	Value	Description	References
HT-22	IC₅₀	16.3 μM Compound: 12; GNF-4877	Cytotoxicity against mouse HT-22 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay Cytotoxicity against mouse HT-22 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay	[PMID: 36876904]
Pancreatic beta cell	EC₅₀	0.19 μM Compound: GNF4877	Induction of cell proliferation in rat beta cells incubated for 4 days by EdU incorporation assay Induction of cell proliferation in rat beta cells incubated for 4 days by EdU incorporation assay	[PMID: 32077280]
Pancreatic beta cell	EC₅₀	0.54 μM Compound: GNF4877	Induction of cell proliferation in human beta cells incubated for 4 days by EdU incorporation assay Induction of cell proliferation in human beta cells incubated for 4 days by EdU incorporation assay	[PMID: 32077280]

体外実験

High glucose concentrations and glucokinase activators (GKAs) increase Ca²⁺ signalling in β-cells, and increase intracellular Ca²⁺ leads to activation of calcineurin and nuclear translocation of NFATc proteins. Indeed, concentrations of GNF4877 ((0.1 μM, 0.3 μM) well below the EC₅₀ for β-cell proliferation are able to induce proliferation in the presence of high glucose or pharmacological activators of glucokinase. Finally, increasing intracellular Ca²⁺ with glibenclamide (a sulfonylurea receptor 1 inhibitor) or Bay K8644 (an L-type Ca²⁺ channel activator) show additive activity with GNF4877^[1].

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

体内実験

GNF4877 (50 mg/kg; oral gavage; twice a day; for 15 days; double transgenic RIP-DTA male mice) treatment induces β-cell proliferation, increases β-cell mass and insulin content, and improves glycaemic control^[1].

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

Animal Model:

Double transgenic RIP-DTA male mice (Tg (Ins 2-rtTA) 2 Efr Tg (teto-DTA) 1 Gfi/J) with Doxycycline (28.8±2.4 g; 82±2 days)^[1]
Dosage:

50 mg/kg
Administration:

Oral gavage; twice a day; for 15 days
Result:

Induced β-cell proliferation, increased β-cell mass and insulin content, and improved glycaemic control.

化学情報

CAS 番号 2041073-22-5
性状 Solid
分子量 494.52
分子式 C₂₅H₂₇FN₆O₄
Color Light yellow to yellow
SMILES

O=C([C@H]1CN(C2=C(NC(C3=NC(C4=CC(OC(C)C)=CC=C4F)=CN=C3N)=O)C=NC=C2)CCC1)O
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (1)

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Nat Commun

CRISPR-based genome editing in primary human pancreatic islet cells. [Abstract]

2021 Apr 23;12(1):2397. PMID: 33893274

溶剤 & 溶解度

体外:

DMSO : 3.33 mg/mL (6.73 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0222 mL

10.1108 mL

20.2216 mL

5 mM

0.4044 mL

2.0222 mL

4.0443 mL

10 mM

---

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (274 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[1]. Shen W, et al. Inhibition of DYRK1A and GSK3β induces human β-cell proliferation. Nat Commun. 2015 Oct 26;6:8372. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0222 mL	10.1108 mL	20.2216 mL	50.5541 mL
DMSO	5 mM	0.4044 mL	2.0222 mL	4.0443 mL	10.1108 mL

Keywords

GNF4877

1 Cited Publications

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GNF4877

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MedChemExpress（MCE）の使用を引用している文献 GNF4877

DYRK アイソフォーム固有の製品をすべて表示

GSK-3 アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (1)

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

GNF4877 関連分類

HY-129492 関連分類