DAPT | GSI-IX | γ-Secretase Inhibitor | AmBeed-信号通路专用抑制剂

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DAPT {[allProObj[0].p_purity_real_show]}

货号：A150458 同义名： GSI-IX; LY-374973

DAPT is an inhibitor of γ-secretase and it can reduce the expression of Aβ40 and Aβ42 with IC50 values of 115 nM and 200 nM.

DAPT 化学结构
CAS号：208255-80-5

DAPT 3D分子结构
CAS号：208255-80-5

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DAPT 纯度/质量文件产品仅供科研

货号：A150458 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: 更多 >

自噬亚型比较
CDK 亚型比较

产品名称	Autophagy ↓ ↑	其他靶点	纯度
SBI-0206965	+++ ULK1, IC50: 108 nM ULK2, IC50: 711 nM		95%
Hydroxychloroquine sulfate	✔		99%
Valproic acid sodium	✔	HDAC	97%
PFK-015	++ PFKFB3, IC50: 207 nM		99%+
MRT68921 HCl	++++ ULK1, IC50: 2.9 nM ULK2, IC50: 1.1 nM		99%+
ROC-325	✔		99%+
Autophinib	+++ Autophagy, IC50: 40 nM		99%
Lys05	✔		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

产品名称	Cdc ↓ ↑	CDK1 ↓ ↑	CDK19 ↓ ↑	CDK2 ↓ ↑	CDK3 ↓ ↑	CDK4 ↓ ↑	CDK5 ↓ ↑	CDK6 ↓ ↑	CDK7 ↓ ↑	CDK8 ↓ ↑	CDK9 ↓ ↑	CLK ↓ ↑	其他靶点	纯度
XL413 HCl	++++ Cdc7, IC50: 3.4 nM													99%+
SU9516		+++ CDK1, IC50: 40 nM		+++ CDK2, IC50: 22 nM		++ CDK4, IC50: 200 nM								99%+
RO-3306		+++ CDK1, Ki: 20 nM											SGK,ERK	98%
R547		++++ CDK1/CyclinB, Ki: 2 nM		++++ CDK2/CyclinE, Ki: 3 nM		++++ CDK4/CyclinD1, Ki: 1 nM								99%+
BMS-265246		++++ CDK1/CyclinB, IC50: 6 nM		++++ CDK2/CyclinE, IC50: 9 nM		+ CDK4/CyclinD, IC50: 230 nM								99%+
NU6027		+ CDK1, Ki: 2.5 μM		+ CDK2, Ki: 1.3 μM									DNA-PK	98%
Purvalanol A	++++ Cdc2/CyclinB, IC50: 4 nM			+++ CDK2/CyclinA, IC50: 70 nM CDK2/CyclinE, IC50: 35 nM		+ CDK4/CyclinD1, IC50: 850 nM								99%+
SCH900776				++ CDK2, IC50: 0.16 μM										99%+
AUZ 454				++++ CDK2(A144C), Kd: 9.7 nM CDK2(C118L), Kd: 18.6 nM										99%+
A-674563 HCl				++ CDK2, Ki: 46 nM									PKA	99%
JNJ-7706621		++++ CDK1/CyclinB, IC50: 9 nM		++++ CDK2/CyclinA, IC50: 4 nM CDK2/CyclinE, IC50: 3 nM	++ CDK3/CyclinE, IC50: 58 nM	+ CDK4/CyclinD1, IC50: 253 nM		++ CDK6/CyclinD1, IC50: 175 nM						99%+
AT7519		++ CDK1/CyclinB, IC50: 210 nM		++ CDK2/CyclinA, IC50: 47 nM	+ CDK3/CyclinE, IC50: 360 nM	++ CDK4/CyclinD1, IC50: 100 nM	+++ CDK5/p35, IC50: 13 nM	++ CDK6/CyclinD3, IC50: 170 nM			++++ CDK9/CyclinT, IC50: <10 nM			98+%
PHA-793887		++ CDK1/CyclinB, IC50: 60 nM		++++ CDK2/CyclinA, IC50: 8 nM CDK2/CyclinE, IC50: 8 nM		++ CDK4/CyclinD1, IC50: 62 nM	++++ CDK5/p25, IC50: 5 nM		++++ CDK7/CyclinH, IC50: 10 nM		++ CDK9/CyclinT1, IC50: 138 nM			99%+
Milciclib		+ CDK1/CyclinB, IC50: 398 nM		++ CDK2/CyclinA, IC50: 45 nM CDK2/CyclinE, IC50: 363 nM		++ CDK4/CyclinD1, IC50: 160 nM	+ CDK5/p35, IC50: 265 nM		++ CDK7/CyclinH, IC50: 150 nM					99%+
Kenpaullone		+ CDK1/CyclinB, IC50: 0.4μM		+ CDK2/CyclinA, IC50: 0.68μM CDK2/CyclinE, IC50: 7.5μM			+ CDK5/p35, IC50: 0.85μM							98%
SNS-032				+++ CDK2/CyclinA, IC50: 38 nM CDK2/CyclinE, IC50: 48 nM			+ CDK5/p35, IC50: 340 nM		++ CDK7/CyclinH, IC50: 62 nM		++++ CDK9/CyclinT, IC50: 4 nM			99%+
Dinaciclib		++++ CDK1, IC50: 3 nM		++++ CDK2, IC50: 1 nM			++++ CDK5, IC50: 1 nM				++++ CDK9, IC50: 4 nM			99%+
PHA-767491 HCl	++++ Cdc7, IC50: 10 nM	+ CDK1, IC50: 250 nM		+ CDK2, IC50: 240 nM			+ CDK5, IC50: 460 nM				+++ CDK9, IC50: 34 nM		MK2	99%
(R)-Roscovitine	+ Cdc2/CyclinB, IC50: 0.65 μM			+ CDK2/CyclinA, IC50: 0.7 μM CDK2/CyclinE, IC50: 0.7 μM			++ CDK5/p35, IC50: 0.16 μM							99%+
Narazaciclib						++++ CDK4/CyclinD1, IC50: 3.87 nM		++++ CDK6/CyclinD1, IC50: 9.82 nM					RET	99%+
Palbociclib						++++ CDK4/CyclinD3, IC50: 9 nM CDK4/CyclinD1, IC50: 11 nM		+++ CDK6/CyclinD2, IC50: 15 nM						99%
Abemaciclib						++++ CDK4, IC50: 2 nM		++++ CDK6, IC50: 10 nM						99%
Ribociclib						++++ CDK4, IC50: 10 nM		+++ CDK6, IC50: 39 nM						98%
Palbociclib isethionate						++++ CDK4/CyclinD3, IC50: 9 nM CDK4/CyclinD1, IC50: 11 nM		+++ CDK6/CyclinD2, IC50: 15 nM						99%+
BS-181 HCl									+++ CDK7, IC50: 21 nM					99%+
(E/Z)-THZ1 2HCl									++++ CDK7, IC50: 3.2 nM					99%+
LDC4297									++++ CDK7, IC50: 0.13 nM					99%+
Senexin A			+ CDK19, Kd: 0.31 μM							+ CDK8, Kd: 0.83 μM				99%
MSC2530818										++++ CDK8, IC50: 2.6 nM				99%+
Wogonin											✔			99%+
Riviciclib HCl		++ CDK1/CyclinB, IC50: 79 nM		+ CDK2/CyclinA, IC50: 224 nM CDK2/CyclinE, IC50: 2.54 μM		++ CDK4/CyclinD1, IC50: 63 nM		+ CDK6/CyclinD3, IC50: 396 nM	+ CDK7/CyclinH, IC50: 2.87 μM		+++ CDK9/CyclinT1, IC50: 20 nM			98%
LDC000067				+ CDK2, IC50: 2.441 μM							++ CDK9, IC50: 44 nM			98%
Flavopiridol		+++ CDK1, IC50: 40 nM		+++ CDK2, IC50: 40 nM		+++ CDK4, IC50: 40 nM		+++ CDK6, IC50: 40 nM	+ CDK7, IC50: 300 nM		+++ CDK9, IC50: 20 nM			99%+
LY2857785									+ CDK7, IC50: 0.246 μM	+++ CDK8, IC50: 0.016 μM	+++ CDK9, IC50: 0.011 μM			99%+
AZD-5438		+++ CDK1, IC50: 16 nM		++++ CDK2, IC50: 6 nM							+++ CDK9, IC50: 20 nM			99%+
ML167												++ Dyrk1B , IC50: 1648 nM CLK4, IC50: 136 nM		99%+
(E/Z)-TG003												+++ mCLK1, IC50: 200 nM mCLK4, IC50: 15 nM		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

DAPT 生物活性

描述

DAPT (GSI-IX), a powerful and orally bioavailable γ-secretase inhibitor, exhibits IC50 values of 115 nM for total amyloid-β (Aβ) and 200 nM for Aβ42. It blocks Notch 1 signaling activation and promotes cell differentiation. Additionally, DAPT triggers autophagy and apoptosis, offers neuroprotective effects, and holds therapeutic potential for autoimmune, lymphoproliferative disorders, degenerative diseases, and cancer^[1]^[2]. DAPT (GSI-IX) (GMP) refers to DAPT manufactured according to GMP standards. GMP-compliant small molecules function effectively as supporting agents in the production of cell therapies. DAPT acts as a potent, orally administrable γ-secretase inhibitor^[1]^[2].

DAPT 细胞研究

细胞系	浓度	检测类型	检测时间	活性说明	数据源
A549	10 μM	Growth Inhibition Assay	24h	decreases the cell viability combined with PTE	23671619
A549 CD133−	2 μM	Growth Inhibition Assay	48 h	enhances cell growth inhibition induced by CDDP	24502949
A549 CD133+	2 μM	Growth Inhibition Assay	48 h	enhances cell growth inhibition induced by CDDP	24502949
GC-B	6.25-100 μM	Growth Inhibition Assay	24 h	inhibits the cell growth in a dose-dependent manner	19542446

DAPT 动物研究

Animal study

DAPT is given to PDAPP mice at a dosage of 100 mg/kg subcutaneously, with subsequent measurement of DAPT and Aβ levels in the brain cortex. Maximum DAPT concentrations reach 490 ng/g in the brain 3 hours post-treatment, maintaining levels above 100 ng/g (~200 nM) for the initial 18 hours. These brain concentrations of DAPT surpass its IC50 for reducing Aβ in neuronal cultures (115 nM), leading to a significant and prolonged pharmacodynamic response^[1].DAPT shields the brain from cerebral ischemia by reducing Notch 1 and Nuclear factor kappa B expression in rats. Western blot analysis further reveals a notable decline in Notch 1 and NF-κB levels in the DAPT (0.03 mg/kg) treated group compared to the MCAO group (P<0.05)^[2].

DAPT 参考文献

[1]Dovey HF, et al. Functional gamma-secretase inhibitors reduce beta-amyloid peptide levels in brain. J Neurochem. 2001 Jan;76(1):173-81.

[2]Li S, et al. DAPT protects brain against cerebral ischemia by down-regulating the expression of Notch 1 and nuclear factor κB in rats. Neurol Sci. 2012 Dec;33(6):1257-64.

[3]Zhou JX, et al. γ-secretase inhibition combined with NSC 119875 enhances apoptosis of nasopharyngeal carcinoma cells.Exp Ther Med. 2012 Feb;3(2):357-361.

DAPT 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.31mL

0.46mL

0.23mL

11.56mL

2.31mL

1.16mL

23.12mL

4.62mL

2.31mL

DAPT 技术信息

CAS号	208255-80-5
分子式	C₂₃H₂₆F₂N₂O₄
分子量	432.46
SMILES Code	O=C(OC(C)(C)C)[C@@H](NC([C@@H](NC(CC1=CC(F)=CC(F)=C1)=O)C)=O)C2=CC=CC=C2
MDL No.	MFCD04974585

别名	GSI-IX; LY-374973; N-(2FPhAc)Ala-phenyl-Gly t-butyl ester.; DAPT peptide
运输	蓝冰
InChI Key	DWJXYEABWRJFSP-XOBRGWDASA-N
Pubchem ID	5311272

存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Keep in dark place, sealed in dry, store in freezer, under -20°C

动物实验配方

IP 2% DMSO+2% Tween80+40% PEG300+water 5 mg/mL clear

PO 0.5% CMC-Na 27 mg/mL suspension

DAPT {[allProObj[0].p_purity_real_show]}

DAPT 纯度/质量文件产品仅供科研

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DAPT 质控信息

DAPT 生物活性

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DAPT 动物研究

DAPT 参考文献

DAPT 实验方案

DAPT 技术信息

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DAPT {[allProObj[0].p_purity_real_show]}

DAPT 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

DAPT 质控信息

DAPT 生物活性

DAPT 细胞研究

DAPT 动物研究

DAPT 参考文献

DAPT 实验方案

DAPT 技术信息

最近浏览的产品

大规格询价

摩尔计算器

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总药量计算器

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