DAPT

目录号 M1746 所有产品仅供科研使用，严禁用于人或动物的治疗等任何其他用途，不为任何个人提供产品和服务

DAPT (GSI-IX)是一种新型γ-分泌酶（γ-secretase）抑制剂，抑制HEK 293细胞中全部Aβ产量，IC50为20 nM。DAPT 也是一种Notch信号通路抑制剂，能够有效抑制 Notch 信号通路的活化传导。

别名：GSI-IX

规格	价格	库存状态
Free Sample (0.5-1 mg)	¥ 0	中国库存现货
10mM*1mL in DMSO	¥ 495	中国库存现货
5mg	¥ 450	中国库存现货
10mg	¥ 765	中国库存现货
50mg	¥ 2250	中国库存现货

其他规格数量报价？

质量标准及产品资料

纯度： 99.50%
COA
MSDS
H-NMR
HPLC

产品信息

生物活性

DAPT (GSI-IX)是一种新型γ-分泌酶抑制剂，抑制HEK 293细胞中全部Aβ产量，IC50为20 nM。DAPT功能性抑制γ-分泌酶而降低HEK 293细胞中全部Aβ产量，IC50为20 nM。DAPT作用于原代培养的人神经细胞，也抑制Aβ产量，作用于全部Aβ和Aβ42时, IC50分别为115 nM和200 nM，比作用于HEK 293细胞时低5-10倍。DAPT 也是一种Notch信号通路抑制剂，能够有效抑制 Notch 信号通路的活化传导。最新研究显示DAPT 抑制SK-MES-1 细胞增殖，这种作用存在浓度依赖性，IC50为11.265 μM。

使用AbMole产品发表的文献

Front Surg. 2023 Jan 16;9:1027067.

Bacterial cellulose membrane combined with BMSCs promotes wound healing by activating the notch signaling pathway
Glycoconj J. 2022 Jun 6.

Notch/NICD/RBP-J signaling axis regulates M1 polarization of macrophages mediated by advanced glycation end products
J Ethnopharmacol. 2019 Oct 28;243:112092.

Study of the aqueous extract of Aloe vera and its two active components on the Wnt/β-catenin and Notch signaling pathways in colorectal cancer cells.
Circ Res. 2017 Jul 31.

SUMOylation Negatively Regulates Angiogenesis by Targeting Endothelial NOTCH Signaling
Oncol Lett. 2017 July 5;4: 3616-3622.

The role of Jagged1/Notch pathway‑mediated angiogenesis of hepatocarcinoma cells in vitro, and the effects of the spleen‑invigorating and blood stasis‑removing recipe
Sci Adv. 2015 Apr 10.

PlGF-induced VEGFR1-dependent vascular remodeling determines opposing antitumor effects and drug resistance to Dll4-Notch inhibitors.
2015 May.

Acquisition of resistance to trastuzumab in gastric cancer cells is associated with activation of IL-6/STAT3/Jagged-1/Notch positive feedback loop

产品使用成果展示

	数据来源	Oncol Lett (2017). Figure 6. DAPT (AbMole BioScience, Shanghai, China)
	方法	Co‑IP assay
	细胞系/动物模型	SMMC‑7721 cells
	浓度	1 μM
	处理时间
	实验结果	The interaction between Jagged1 and Notch1 in SMMC‑7721 cells was also significantly reduced after adding DAPT compared with that of the normal serum group (P<0.01) (Fig. 6).

	数据来源	Oncol Lett (2017). Figure 5. DAPT (AbMole BioScience, Shanghai, China)
	方法	Western blot
	细胞系/动物模型	SMMC‑7721 cells
	浓度	1 μM
	处理时间
	实验结果	The levels of Jagged1 and Notch1 were decreased after adding the Notch inhibitor, DAPT, indicating that DAPT successfully inhibited the Jagged1/Notch signaling pathway. In addition, the expression of VEGF protein was reduced after adding DAPT (Fig. 5).

	数据来源	Circ Res (2017). Figure 2. DATP (Abmole Bioscience)
	方法	Retina dissection and whole mount staining
	细胞系/动物模型	mice
	浓度	100 mg/kg
	处理时间
	实验结果	DAPT treatment resulted in a large increase in vessel density and expansion of the vascular plexus in the postnatal retina of control mice (Fig. 2A, C, E, G). DAPT completely rescued the defect in SENP1-ecKO pups (Fig. 2B, D, F, H), which resulted in vascular length, vascular coverage, and tip sprouts growth comparable to the control group (Fig. 2I-K).

	数据来源	Sci adv (2015). Figure 5. The DAPT g-secretase inhibitor was obtained from AbMole BioScience.
	方法	Immunohistochemistry
	细胞系/动物模型
	浓度	100 mg/kg, daily
	处理时间
	实验结果	"The PlGF-modulated opposing vascular effects in relation to Dll4-Notch inhibition alter tumor growth by changing the microenvironment, tumor cell proliferation, and apoptosis."

	数据来源	Sci adv (2015). Figure 4. The DAPT g-secretase inhibitor was obtained from AbMole BioScience.
	方法	human tumor models, Immunohistochemistry
	细胞系/动物模型
	浓度	100 mg/kg, daily
	处理时间
	实验结果	PlGF mediates opposing vascular effects in nontreated and Dll4-Notch inhibitor–treated mouse tumors.

	数据来源	Sci adv (2015). Figure 3. The DAPT g-secretase inhibitor was obtained from AbMole BioScience.
	方法	Immunohistochemistry
	细胞系/动物模型	Human JE-3, BeWo, MDA-MB-231 cells
	浓度	100 mg/kg, daily
	处理时间
	实验结果	"Both terminal deoxynucleotidyl transferase–mediated deoxyuridine triphosphate nick end labeling (TUNEL) staining and measurements of the activated or cleaved caspase 3 showed reductions of apoptotic cells in Dll4-Notch inhibitor–treated JE-3 and BeWo tumors. In contrast, treatment of PlGF-negative MDAMB-231 tumors with DAPT and Dll4 blockade showed completely opposite effects on cell proliferation and apoptosis, tipping the balance toward an apoptotic phenotype."

	数据来源	Sci adv (2015). Figure 1. The DAPT g-secretase inhibitor was obtained from AbMole BioScience.
	方法	Immunohistochemistry
	细胞系/动物模型	Human JE-3, BeWo, MDA-MB-231 cells
	浓度	100 mg/kg, daily
	处理时间
	实验结果	"PlGF expression determines opposing effects of Dll4-Notch inhibition on human tumor growth and vascular remodeling."

实验参考

体外实验*
细胞系	SK-MES-1
方法	Cells are seeded into 96-well plates and exposed to 0.1% DMSO or DAPT at concentrations in the range of 2.5 μM–160 μM for 72 hours. Cytotoxicity is determined with 3-(4, 5)-dimethylthiahiazo-(-z-y1)-3, 5-di-phenytetrazoliumromide (MTT) dye reduction assay with minor modifications. Briefly, after incubation with DAPT, 20 μL MTT solution (5 mg/mL in PBS) is added to 180 μL medium in each well and plates are incubated for 4 hours at 37 °C, and subsequently 150 μL DMSO is added to each well, and mixed by shaking at room temperature for 15 minutes. Absorption is measured by an enzyme-linked immunosorbent assay at 490 nm to determine absorbance values.
浓度	2.5 ~ 160 μM
处理时间	72 h

*上述方法来自公开文献，仅供相同目的实验参考。如实验目的、材料、方法不同，请参考其他文献。

体内实验*
动物模型	three‐ to four‐month‐old heterozygous PDAPP transgenic mice overexpressing the APPV717F mutant form of the amyloid precursor protein
配制	formulated in corn oil, 5% (v/v) ethanol
剂量	100 mg/kg
给药处理	s.c.

*上述方法来自公开文献，仅供相同目的实验参考。如实验目的、材料、方法不同，请参考其他文献。

化学性质

分子量	432.46
分子式	C23H26F2N2O4
CAS号	208255-80-5
溶解性（25°C）	DMSO 60 mg/mL
储存条件	粉末型式 -20°C 3年；4°C 2年溶于溶剂 -80°C 6个月；-20°C 1个月
运输方式	冰袋运输，根据产品的不同，可能会有相应调整。

储备液配制

*下述溶液配置方法仅为基于分子量计算出的理论值。不同产品在配置溶液前，需考虑其在不同溶剂中的溶解度限制。

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.3124 mL	11.5618 mL	23.1235 mL
5 mM	0.4625 mL	2.3124 mL	4.6247 mL
10 mM	0.2312 mL	1.1562 mL	2.3124 mL

不同实验动物依据体表面积的等效剂量转换表（参考来源于公开文献）

	小鼠	大鼠	兔	豚鼠	仓鼠	狗
重量 (kg)	0.02	0.15	1.8	0.4	0.08	10
体表面积 (m²)	0.007	0.025	0.15	0.05	0.02	0.5
K_m 系数	3	6	12	8	5	20

动物 A (mg/kg) = 动物 B (mg/kg) ×	动物 B的K_m系数
	动物 A的K_m系数

例如，依据体表面积折算法，将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量，需要将20 mg/kg 乘以小鼠的K_m系数（3），再除以大鼠的K_m系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。

参考文献

[1] Kim BK et al. J Am Coll Cardiol. A New Strategy for Discontinuation of Dual Antiplatelet Therapy: The RESET Trial (REal Safety and Efficacy of 3-month dual antiplatelet Therapy following Endeavor zotarolimus-eluting stent implantation).

[2] Kedhi E et al. EuroIntervention. Stent thrombosis: insights on outcomes, predictors and impact of dual antiplatelet therapy interruption from the SPIRIT II, SPIRIT III, SPIRIT IV and COMPARE trials.

[3] Oikawa et al. Neurosci Lett. The γ-secretase inhibitor DAPT increases the levels of gangliosides at neuritic terminals of differentiating PC12 cells.

[4] Zou et al. Clin Exp Med. Gamma-secretase inhibitor DAPT suppresses glioblastoma growth via uncoupling of tumor vessel density from vessel function.

[5] H F Dovey, et al. J Neurochem. Functional gamma-secretase inhibitors reduce beta-amyloid peptide levels in brain

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