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 (GSI-IX)是一种强效且具有口服活性的 γ-secretase 抑制剂，可用于细胞疗法中的辅助试剂。

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

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自噬亚型比较
CDK 亚型比较

产品名称	Autophagy ↓ ↑	其他靶点	纯度
SBI-0206965	+++ ULK2, IC50: 711 nM ULK1, IC50: 108 nM		97%
Hydroxychloroquine sulfate	✔		99%
Valproic acid sodium	✔	HDAC	97%
PFK-015	++ PFKFB3, IC50: 207 nM		99%+
MRT68921 hydrochloride	++++ ULK2, IC50: 1.1 nM ULK1, IC50: 2.9 nM		99%+
ROC-325	✔		99%+
Autophinib	+++ Autophagy, IC50: 40 nM		97%
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 hydrochloride	++++ 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											ERK,SGK	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	98%
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 hydrochloride	++++ Cdc7, IC50: 10 nM	+ CDK1, IC50: 250 nM		+ CDK2, IC50: 240 nM			+ CDK5, IC50: 460 nM				+++ CDK9, IC50: 34 nM		MK2	98%
(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/CyclinD1, IC50: 11 nM CDK4/CyclinD3, IC50: 9 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/CyclinD1, IC50: 11 nM CDK4/CyclinD3, IC50: 9 nM		+++ CDK6/CyclinD2, IC50: 15 nM						99%+
BS-181 HCl									+++ CDK7, IC50: 21 nM					99%+
(E/Z)-THZ1 dihydrochloride									++++ 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				98+%
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			99+%
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												+++ mCLK4, IC50: 15 nM mCLK1, IC50: 200 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].
体内研究	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].
体外研究	DAPT can inhibit the production of more than 90% of Aβ, but has little effect on APPβ in the medium. Although DAPT treatment reduces APPβ by approximately 30%, this effect is not concentration-dependent and is reversed by removal of DAPT^[1]. CNE-2 cells exposed to escalating doses of DAPT (0, 25, 50, and 75 μM) show a reduction in the γ-secretase-generated Notch 1 fragment Val1744-NICD after 48 hours, with the decrease being dose-responsive (P<0.01). At a concentration of 50 μM, DAPT nearly fully blocks γ-secretase activation^[3]. DAPT (GMP) over a period of 9 days prompts the development of human induced pluripotent stem cells into expandable myoblasts^[1]. DAPT (GMP) administered for 13 days leads to the differentiation of human pluripotent stem cells (hPSCs) into functional neurons^[2].
作用机制	DAPT targets the C-terminal fragment of PS which represents the catalytic center of γ-secretase, especially the transmembrane domain 7 or more C-terminal region. DAPT can completely abolish the proteolytic activity of γ-secretase.^[5]^[6]

DAPT 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	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

Dose	Mice: 10 mg/kg^[7] (s.c.), 100 mg/kg^[1] (s.c.); 1 mg/kg - 5 mg/kg^[8] (i.p.), 200 mg/kg^[9] (i.p.) Rat: 10 mg/kg, 50 mg/kg^[10] (i.p.), 0.03 mg/kg^[11] (stereotactically injected into lateral cerebral ventricle)
Administration	s.c., i.p.

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]Qi Y, et al. Combined small-molecule inhibition accelerates the derivation of functional cortical neurons from human pluripotent stem cells. Nat Biotechnol. 2017 Feb;35(2):154-163.

[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

别名	GSI-IX;LY-374973;N-(2FPhAc)Ala-phenyl-Gly t-butyl ester.;DAPT peptide
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C

溶解度

DMSO: 60 mg/mL(138.74 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

无水乙醇: 8 mg/mL(18.5 mM)，配合低频超声助溶，注意：无水乙醇开封后，易挥发，也会吸收空气中的水分，导致溶解能力下降，请避免使用开封较久的乙醇

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]}

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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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