EHop-016

製品コードS7319 バッチS731902

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₂₅H₃₀N₆O

分子量

430.55

CAS No.

1380432-32-5

Solubility (25°C)*

体外

DMSO

86 mg/mL (199.74 mM)

Water

Insoluble

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

Clear solution	5% DMSO 1 95% Corn oil	0.45mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 9 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	0.75mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 15 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	EHop-016 is a specific Rac GTPase inhibitor with IC50 of 1.1 μM for Rac1 in MDA-MB-435 and MDA-MB-231 cells, equally potent inhibition for Rac3.
in vitro	Rac inhibition by EHop-016 increases the activity of the closely related Rho GTPase RhoA by a compensatory mechanism. In MDA-MB-435 cells, EHop-016 (2-5 μM) inhibits association of active Vav2 with Rac1(G15A) mutant fusion protein, and reduces Rac-regulated cell functions including lamellipodia formation and cell migration. In addition, EHop-016 inhibits cell viability of MDA-MB-435 cells with IC50 of 10 μM. ^[1] EHop-016 also inhibits KITD814V-induced growth in SM and AML patients-derived cells. ^[2]
in vivo	Treatment of KITD814V-bearing cells with EHop-016 significantly enhances the survival of leukemic mice. ^[2]

プロトコル(参考用のみ)

キナーゼアッセイ	Rac Activity Assays
キナーゼアッセイ	Rac activity is determined from lysates of the MDA-MB-435 and MDA-MB-231 human metastatic cancer cell lines. Cancer cells in culture medium (DMEM, 10% FBS, pH 7.5) are treated with vehicle (0.1% DMSO) or varying concentrations of EHop-016 (0–10 μM) for 24 h. Rac1 activity is determined using the G-LISA Rac1 activation assay kit.
細胞アッセイ	細胞株	MDA-MB-231, MDA-MB-435, or MCF-10A cells
	濃度	~10 μM
	反応時間	24 hours
	実験の流れ	MDA-MB-231, MDA-MB-435, or MCF-10A mammary epithelial cells are incubated in vehicle (0.1% DMSO) or varying concentrations of EHop-016 (0–10 μM) for 24 h. Cell viability is measured using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide cell survival and proliferation kit according to the manufacturer's instructions.
動物実験	動物モデル	KITD814V-bearing mice.
	投薬量	2.5 μM
	投与方法	KITD814V-bearing 32D cells with EHop-016 are administered by i.v. injection.

参考

カスタマーフィードバック

: , , Cell Death Dis, 2015, 6:e1751.

: Data from [Data independently produced by , , Biochem Pharmacol, 2016, 105:42-54.]

: Data from [Data independently produced by , , Exp Cell Res, 2017, 361(1):112-125]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Vav proteins do not influence dengue virus replication but are associated with induction of phospho-ERK, IL-6, and viperin mRNA following DENV infection in vitro [ Microbiol Spectr, 2024, 12(1):e0239123]	PubMed: 38054722
Sigma-1 receptor-regulated efferocytosis by infiltrating circulating macrophages/microglial cells protects against neuronal impairments and promotes functional recovery in cerebral ischemic stroke [ Theranostics, 2023, 13(2):543-559]	PubMed: 36632219
Loss of Dnmt3a impairs hematopoietic homeostasis and myeloid cell skewing via the PI3Kinase pathway [ JCI Insight, 2023, 8(9)e163864]	PubMed: 36976647
Loss of Dnmt3a impairs hematopoietic homeostasis and myeloid cell skewing via the PI3Kinase pathway [ JCI Insight, 2023, 8(9)e163864]	PubMed: 36976647
ATM inhibition drives metabolic adaptation via induction of macropinocytosis [ J Cell Biol, 2023, 222(1)e202007026]	PubMed: 36399181
Activation of the mevalonate pathway in response to anti-cancer treatments drives glioblastoma recurrences through activation of Rac-1 [ bioRxiv, 2023, 2023.07.23.550205]	PubMed: 37546917
Non-muscle myosin II isoforms orchestrate substrate stiffness sensing to promote cancer cell contractility and migration [ Cancer Lett, 2022, 524:245-258]	PubMed: 34715250
Gas6 Promotes Microglia Efferocytosis and Suppresses Inflammation Through Activating Axl/Rac1 Signaling in Subarachnoid Hemorrhage Mice [ Transl Stroke Res, 2022, 10.1007/s12975-022-01099-0]	PubMed: 36324028
LncRNA RP11-214F16.8 drives breast cancer tumorigenesis via a post-translational repression on NISCH expression [ Cell Signal, 2022, S0898-6568(22)00031-6]	PubMed: 35108640
Farnesyl pyrophosphate is a new danger signal inducing acute cell death [ PLoS Biol, 2021, 19(4):e3001134]	PubMed: 33901180

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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