DAPT (GSI-IX) - Moligand™, 10mM in DMSO , CAS No.208255-80-5

CAS: 208255-80-5 Cat. No.: D408190 Molecular Weight: 432.46

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

LY-374973 | (S)-tert-butyl 2-((S)-2-(2-(3,5-difluorophenyl)acetamido)propanamido)-2-phenylacetate

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

DAPT (GSI-IX, LY-374973) is a novelγ-secretaseinhibitor, which inhibits Aβ production withIC50of 20 nM in HEK 293 cells. DAPT enhances theapoptosisof human tongue carcinoma cells and regulatesautophagy.
In vitro

In human primary neuronal cultures, DAPT also shows inhibitory effects on Aβ production with IC50 of 115 nM and 200 nM respectively for Aβ total and Aβ42, which is 5-10-fold lower than is observed in HEK 293 cells. A recent study shows that DAPT inhibits the proliferation of SK-MES-1 cells in a concentration-dependent manner with IC50 of 11.3 μM. In addition, DAPT also induces caspase-dependent and caspase-independent apoptosis in lung squamous cell carcinoma cells by inhibiting Notch receptor signaling pathway.

In vivo

DAPT administration (100mg/kg) leads to a robust and sustained pharmacodynamic effect in PDAPP mice that DAPT levels in the brain exceeds 100 ng/g within 1 hour and persists up to 18 hours after administration, with peak levels of 490 ng/g observed after 3 hour. And during the period, DAPT (100 mg/kg) also reduces the cortical total Aβ and Aβ42 in a dose-dependent manner with a 50% reduction. In rat cerebral cortexes, DAPT (40 mg/kg) suppresses the LPS-induced activity of γ-secretase and increases the cell apoptosis with the prolonged neuroinflammation.
Cell Data

cell lines：

Concentrations：2.5 μM to 160 μM

Incubation Time：72 hours

Powder Purity:≥98%

Specifications

Synonyms

LY-374973 | (S)-tert-butyl 2-((S)-2-(2-(3, 5-difluorophenyl)acetamido)propanamido)-2-phenylacetate

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

DAPT (GSI-IX, LY-374973) is a novel γ-secretase inhibitor, which inhibits Aβ production with IC50 of 20 nM in HEK 293 cells. DAPT enhances the apoptosis of human tongue carcinoma cells and regulates autophagy.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Names and Identifiers

• Isomeric SMILES: C[C@@H](C(=O)N[C@@H](C1=CC=CC=C1)C(=O)OC(C)(C)C)NC(=O)CC2=CC(=CC(=C2)F)F
• WGK Germany: 3
• Alternate CAS: 208255-80-5
• MeSH Entry Terms: DAPT butylester;DAPT peptide;GSI-IX cpd;N-(2FPhAc)Ala-phenyl-Gly t-butyl ester;N-(N-(3,5-difluorophenacetyl)alanyl)-S-phenylglycine t-butyl ester;N-(N-(3,5-difluorophenacetyl)alanyl)phenylglycine t-butyl ester;N-(N-(3,5-difluorophenacetyl)alanyl)phenylgly
• Molecular Weight: 432.46
• Reaxy-Rn: 24866565
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=24866565&ln=

Chemical and Physical Properties

• Solubility: Solubility (25°C) In vitro DMSO: 27 mg/mL (199.82 mM)

References

1. Huimin Chen, Xin Li, Wenjiang Li, Aoao Lu, Chenguang Li, Qiang Li, Dabin Liu, Hongfei Ma, Binbin Wang.  (2025)  Porous organic polymers containing Tröger's base for enhanced NOx adsorption.  POLYMER DEGRADATION AND STABILITY,      [PMID:] [10.1016/j.polymdegradstab.2025.111548]

2. Wenshuai Hao, Ruitao Cha, Mingzheng Wang, Juanjuan Li, Hongbo Guo, Ran Du, Fengshan Zhou, Xingyu Jiang.  (2023)  Ligand-Modified Gold Nanoparticles as Mitochondrial Modulators: Regulation of Intestinal Barrier and Therapy for Constipation.  ACS Nano,      [PMID:37449942] [10.1021/acsnano.3c01656]

3. Qiufang Chen, Bin Deng, Qing Luo, Guanbin Song.  (2020)  Deep tumor‐penetrated nanosystem eliminates cancer stem cell for highly efficient liver cancer therapy.  CHEMICAL ENGINEERING JOURNAL,      [PMID:] [10.1016/j.cej.2020.127874]

4. Chunxia Pang, Huanhuan You, Sijie Lei, Fan Su, Lili Liang, Zhanguo Li, Xiaoyan Lin, Yaping Zhang, Hao Zhang, Xunhai Pan, Yang Hu.  (2024)  Chemically tailored molecular surface modification of bamboo pulp fibers for manipulating the electret performance of electret filter media.  CARBOHYDRATE POLYMERS,      [PMID:38368109] [10.1016/j.carbpol.2024.121830]

5. Na Li, Baokun Tang, Tao Zhu.  (2024)  Efficient detection of carbendazim using an electrochemical sensor for a novel NiFeLDH@HsGY-NH2/MWCNTs heterostructure with lattice-strain.  Analytical Methods,  16  (38): (6529-6537).  [PMID:39248409] [10.1039/D4AY01265H]

6. Tang Xu, Wenshuai Hao, Ran Du, Dai Dai, Cuixia Wang, Suhua Li, Carol Sze Ki Lin, Ruitao Cha, Jianbin Yan, Chong Li.  (2024)  Mercaptoimidazole-capped gold nanoparticles as a potent agent against plant pathogenic fungi.  Journal of Materials Chemistry B,      [PMID:39344784] [10.1039/D4TB01032A]

7. Peipei Li, Jing Kang, Xiaojie Wu, Duo Wang, Yongjun Li, Nan Liang, Rui Du, Minjie Wang, Alideertu Dong, Yuliang Li.  (2024)  Mild phototherapy strategies for efficient treatment of bacterial keratitis while avoiding side effects.  Nano Today,      [PMID:] [10.1016/j.nantod.2024.102336]

8. Li Na, Mao Jingwei, Tang Haiying, Tan Xiaoyan, Bi Jian, Wu Hao, Chen Xiuli, Wang Yingde.  (2025)  FLT3 ligand regulates expansion of regulatory T-cells induced by regulatory dendritic cells isolated from gut-associated lymphoid tissues through the Notch pathway.  CHINESE MEDICAL JOURNAL,      [PMID:40211734] [10.1097/CM9.0000000000003493]