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

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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											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(C118L), Kd: 18.6 nM CDK2(A144C), Kd: 9.7 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。

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]

Cell Line UT-SCC-42B cells Human induced pluripotent stem cell– and human embryonic stem cells–derived retinal organoids HEK293T cells SH-SY5Y cells Non-differentiated embryonic multipotent mesenchymal progenitor cell line (10T1/2 cells) Human coronary artery smooth muscle cells (HCASMCs) C2C12 cells Human Umbilical Vein Endothelial Cells (HUVEC) Human Umbilical Vein Endothelial Cells (HUVEC)	Concentration	Treated Time	Description	References
UT-SCC-42B cells	2.5 µM	72 hours	To evaluate the effect of CB-103 on the expression of Notch signaling-related genes, results showed no significant changes in mRNA levels after CB-103 treatment.	Sci Rep. 2023 Aug 22;13(1):13700.
Human induced pluripotent stem cell– and human embryonic stem cells–derived retinal organoids	50 μM	2 days	DAPT did not drive significant differentiation	Invest Ophthalmol Vis Sci. 2022 Sep 1;63(10):12.
HEK293T cells	10 μM	12 h	DAPT was used to inhibit γ-secretase activity to study the effect of H2O2 on γ-secretase activity. The results showed that pretreatment with DAPT significantly reduced the H2O2-induced luciferase activity, indicating that γ-secretase activity was inhibited.	J Biol Chem. 2008 Jun 20;283(25):17721-30.
SH-SY5Y cells	1-10 μM	3 h	DAPT, as a γ-secretase inhibitor, was used to study the role of H2O2 in activating γ-secretase through the JNK-dependent pathway. The results showed that pretreatment with DAPT effectively reduced the H2O2-induced AICD level, indicating that γ-secretase activity was inhibited.	J Biol Chem. 2008 Jun 20;283(25):17721-30.
Non-differentiated embryonic multipotent mesenchymal progenitor cell line (10T1/2 cells)	10 μM	overnight	Inhibited Notch signaling and significantly downregulated Hes1, Acta2, and Cnn1 gene expression, suggesting these genes are downstream targets of Notch signaling.	Cells. 2021 Aug 14;10(8):2089.
Human coronary artery smooth muscle cells (HCASMCs)	10 μM	overnight	Inhibited Notch signaling and significantly attenuated the bead-bound Jagged1 induced gene response, suggesting a direct cause and effect of Notch signaling and gene expression.	Cells. 2021 Aug 14;10(8):2089.
C2C12 cells	10 μM	5 min, 15 min, 30 min, 1 hr 4 h	To investigate the effect of the duration of Notch activation after DAPT removal on Hes1 and Hey1/L gene expression. The results showed that Hes1 responded strongly to brief pulses of Notch activation, while Hey1 and HeyL required sustained Notch activation.	Cell. 2018 Feb 8;172(4):869-880.e19.
Human Umbilical Vein Endothelial Cells (HUVEC)	10 µM	24 h	To study the effect of DAPT on the cell cycle distribution of HUVEC, the results showed that DAPT treatment significantly reduced the proportion of cells in G1 phase and increased the proportion of cells in S/G2/M phase.	Nat Commun. 2017 Dec 15;8(1):2149.
Human Umbilical Vein Endothelial Cells (HUVEC)	10 µM	1 hour	To verify whether fluid shear stress (FSS) induces NOTCH signaling, the results showed that FSS significantly increased the cleavage of the NOTCH intracellular domain (NICD), and this effect was blocked by pre-treatment with DAPT.	Nat Commun. 2017 Dec 15;8(1):2149.

Species Mice Kunming mice Mice	Animal Model Wild-type and Gja4−/− mice Focal cerebral ischemia/reperfusion injury model Snail1 LOF mutant mice	Administration	Dosage	Frequency	Description	References
Mice	Wild-type and Gja4−/− mice	Subcutaneous injection	100 mg/kg	Injected once at 24 hours and once at 12 hours prior to killing	To study the effect of DAPT on retinal vascular remodeling in mice, the results showed that DAPT treatment increased vascular density and reduced the expression of SMA and GJA5, indicating delayed arterial development.	Nat Commun. 2017 Dec 15;8(1):2149.
Kunming mice	Focal cerebral ischemia/reperfusion injury model	Intraperitoneal injection	5 mL/kg	Single dose, lasting 14 days	DAPT significantly improved neurobehavioral scores and relieved neuronal morphological damage in mice with cerebral ischemia/reperfusion injury. DAPT decreased the number of glial fibrillary acidic protein- and Notch1-positive cells in the right prefrontal cortex, reduced the number of apoptotic cells, and downregulated Hes1 and Hes5 protein expression.	Neural Regen Res. 2019 Mar;14(3):452-461
Mice	Snail1 LOF mutant mice	Subcutaneous injection	100 mg/kg	Injected at E7.5, E8.5 and E9.5, embryos dissected at E10.5	To evaluate the rescue effect of DAPT on vascular defects in Snail1 LOF mutant mice. Results showed that DAPT partially restored vascular remodeling and branching in Snail1 LOF mutants.	Nat Commun. 2014 Jun 4;5:3998

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.

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

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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

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
HT29	0.5-75 μM	Growth Inhibition Assay	12/24/48 h	inhibits the cell growth in a concentration manner	25257945
MG63	100 μM	Function Assay	24 h	desensitizes the cell line to cisplatin treatment	24894297
Saos-2	100 μM	Function Assay	24 h	desensitizes the cell line to cisplatin treatment	24894297
SHG-44	0.5-10 μM	Growth Inhibition Assay	1-5 d	inhibits the cell viability at the optimal concentration of 1 μM	25063285
U251	2 μM	Growth Inhibition Assay	48 h	strengthens t-AUCB-induced cell growth suppression	24793313
U251	2 μM	Function Assay	48 h	blocks t-AUCB-induced activation of the p38 MAPK/MAPKAPK2/Hsp27 pathway and inhibits expression of NICD1	24793313
U87	2 μM	Growth Inhibition Assay	48 h	strengthens t-AUCB-induced cell growth suppression	24793313
U87	2 μM	Function Assay	48 h	blocks t-AUCB-induced activation of the p38 MAPK/MAPKAPK2/Hsp27 pathway and inhibits expression of NICD1	24793313

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