GCN2iB

製品コードS8929 バッチS892902

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder

化学式

C₁₈H₁₂ClF₂N₅O₃S

分子量

451.83

CAS No.

2183470-12-2

Solubility (25°C)*

体外

DMSO

15 mg/mL (33.19 mM)

Water

Insoluble

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

Clear solution

5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O

0.75mg/ml

Taking the 1 mL working solution as an example, add 50 μL of 15 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	GCN2iB is an ATP-competitive serine/threonine-protein kinase general control nonderepressible 2 (GCN2) inhibitor with IC50 of 2.4 nM.

生物活性

製品説明	GCN2iB is an ATP-competitive serine/threonine-protein kinase general control nonderepressible 2 (GCN2) inhibitor with IC50 of 2.4 nM.
in vitro	The treatment of acute lymphoblastic leukemia (ALL) cells with GCN2iB renders ALL cells sensitive to ASNase by preventing the induction of ASNS, resulting in reduced levels of de novo protein synthesis. Combined treatment with ASNase and GCN2iB induces the stress-activated MAPK pathway, thereby triggering apoptosis. By using cell-panel analyses, we also shows that acute myelogenous leukemia and pancreatic cancer cells are highly sensitive to the combined treatment. ^[1]
in vivo	The combination of ASNase treatment with GCN2iB synergistically blocks in vivo tumor growth in ALL, AML, and pancreatic xenograft models. ^[1]

プロトコル(参考用のみ)

キナーゼアッセイ	GCN2 kinase assay
キナーゼアッセイ	Recombinant GCN2 (1 nmol/L) protein is pre-incubated with GCN2 inhibitors for 60 min and then incubated with ATP (K_M value of GCN2 = 190 μmol/L) and the green fluorescent protein-eIF2α substrate (130 nmol/L) at 25°C. The amount of phosphorylated substrate is determined using the LanthaScreen Tb-anti-p-eIF2α (pSer52) antibody kit. The IC50 value of eIF2α kinase is measured using the XLfit software.
細胞アッセイ	細胞株	Pancreatic cancer cells, CCRF-CEM cells, MEF cells (GCN2-WT or -KO), CCRF-CEM, MV-4-11, SU.86.86 cells
	濃度	37 nM, 110 nM, 330 nM, 1.0 μM
	反応時間	4 h, 72 h
	実験の流れ	CCRF-CEM cells are treated with GCN2iB as indicated for 4 h. Cell lysates are analyzed by western blot; MEF cells (GCN2-WT or -KO) are treated with GCN2 inhibitors as indicated for 72 h. Cell viability is measured; CCRF-CEM, MV-4-11, and SU.86.86 cells are treated with 1 μmol/L GCN2iB as indicated for 72 h. Cell viability is measured at day 0 and day 3; CCRF-CEM and SU.86.86 cells are treated with GCN2 inhibitors as indicated for 72 h. Cell viability is measured.
動物実験	動物モデル	6-week-old female SCID mice
	投薬量	1 mg/kg, 3 mg/kg, 10 mg/kg
	投与方法	Oral gavage, IP

参考

[1] Akito Nakamura, et al. Proc Natl Acad Sci U S A. 2018 Aug 14;115(33):E7776-E7785.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Nucleus pulposus cells regulate macrophages in degenerated intervertebral discs via the integrated stress response-mediated CCL2/7-CCR2 signaling pathway [ Exp Mol Med, 2024, 56(2):408-421.]	PubMed: 38316963
Adipocytes disrupt the translational programme of acute lymphoblastic leukaemia to favour tumour survival and persistence [ Nat Commun, 2021, 12(1):5507]	PubMed: 34535653

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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