Shanghai Nianxing Industrial Co., Ltd
China
Product Name: Palmitic acid
Price: Check
Purity: 98.0%
Stocking Period: 10 Day
Contact: Yang
Email: sales@echemcloud.com

2396465-33-9

2396465-33-9 structure

2396465-33-9 structure

Name: GCN2-IN-7
Chemical Name: GCN2-IN-7
CAS Number: 2396465-33-9
Molecular Formula: C₂₂H₂₃BrN₈OS
Molecular Weight: 527.44
Catalog: Research Areas Cancer
Create Date: 2022-10-12 11:11:00
Modify Date: 2024-04-03 14:37:32
GCN2-IN-7 (compound 39) is an orally active and selective general control nonderepressible 2 (GCN2) inhibitor (IC50=5 nM). GCN2-IN-7 shows anti-tumor activity in vivo[1].

Name	GCN2-IN-7

Description	GCN2-IN-7 (compound 39) is an orally active and selective general control nonderepressible 2 (GCN2) inhibitor (IC50=5 nM). GCN2-IN-7 shows anti-tumor activity in vivo[1].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> Others >> Others
Target	IC50: 5 nM (GCN2)[1]
In Vitro	GCN2-IN-7 (600 nM; 3 d) alleviates myeloid-derived suppressive cells (MDSC)-related T cell suppression and restores T cell proliferation[1]. Cell Proliferation Assay[1] Cell Line: CD8+ T cells from WT and GCN2KO cells Concentration: 600 nM Incubation Time: 3 days Result: Relieved MDSC suppression of proliferation of the co-cultured CD8+ T cells with significant relief at 600 nM.
In Vivo	GCN2-IN-7 (oral gavage; 15 mg/kg; BID; 17 d) shows robust target engagement in vivo at a reasonable dose[1]. GCN2-IN-7 (oral gavage; 50 mg/kg; BID; 17 d) inhibits tumor growth in vivo of the LL2 syngeneic mouse tumor model[1]. Animal Model: Balb/c mice injected with RENCA cells[1] Dosage: 15 mg/kg Administration: Oral gavage; 15 mg/kg; BID; 17 days Result: Showed robust target engagement of GCN2 in both tumor (average of 84%) and spleen (average of 80%) tissues. Showed an average of 65% reduction of downstream marker Activation Transcription Factor 4 (ATF4) in compound-treated mice compared to the vehicle treatment group. Animal Model: LL2 syngeneic mouse model[1] Dosage: 50 mg/kg Administration: Oral gavage; 50 mg/kg; BID; 17 days Result: Showed tumor growth inhibition (56%) after 26 days of dosing compared to the vehicle group.
References	[1]. Jackson JJ, et al. Potent GCN2 Inhibitor Capable of Reversing MDSC-Driven T Cell Suppression Demonstrates In Vivo Efficacy as a Single Agent and in Combination with Anti-Angiogenesis Therapy. J Med Chem. 2022 Sep 20.

Molecular Formula	C₂₂H₂₃BrN₈OS
Molecular Weight	527.44

The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.