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HS-173

Catalog No. T2308 CAS 1276110-06-5

Synonyms: HS 173, HS173

HS-173 is an effective PI3Kα inhibitor (IC50: 0.8 nM).

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

HS-173, CAS 1276110-06-5

Pack Size	Availability	Price/USD
1 mg	In stock	$ 34.00
2 mg	In stock	$ 48.00
5 mg	In stock	$ 77.00
10 mg	In stock	$ 137.00
25 mg	In stock	$ 286.00
50 mg	In stock	$ 441.00
100 mg	In stock	$ 573.00
1 mL * 10 mM (in DMSO)	In stock	$ 84.00

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Purity: 99.47%

Purity: 99.33%

Biological Description

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Storage & Solubility Information

Description	HS-173 is an effective PI3Kα inhibitor (IC50: 0.8 nM).
Targets&IC50	PI3Kα:0.8 nM
In vitro	By inhibiting the PI3K/Akt signaling pathway, HS-173 significantly slows down the progression of liver fibrosis in vivo. It also reduces angiogenesis in mice.
In vivo	In vitro studies reveal that HS-173 can induce apoptosis by affecting cell cycle distribution and activating caspases, while also inhibiting VEGF-induced angiogenesis. When combined with sorafenib, HS-173 exhibits synergistic anticancer effects in pancreatic cancer cells. Additionally, HS-173 demonstrates significant anti-proliferative activity in T47D, SK-BR3, and MCF7 cells (IC50: 0.6/1.5/7.8 μM), and fully inhibits the PI3K pathway in cancer cell lines (Hep3B and SkBr3).
Kinase Assay	PI3-Kinase assay: The PI3K assay is performed using the Kinase-Glo Max luminescent kinase assay kit which quantifies the amount of ADP produced by the PI3K reaction. In brief, an active PI3K (100 ng) is preincubated with compound for 5 min in kinase reaction buffer (25 mM MOPS [pH 7.0], 5 mM MgCl2, and 1 mM EGTA) and 10 μg l-α-phosphatidylinositol (PI). Before addition of PI, it is sonicated with sonication buffer (25 mM MOPS [pH 7.0], 1 mM EGTA) in water for 20 min for allowing miscelle formation. Then reaction is started by the addition of 10 μM ATP and ran for 180 min. To terminate kinase reaction, same volume of Kinase-Glo Max buffer is added. After 10 min, the plates are then read on a GloMax plate reader for luminescence detection.
Cell Research	Cell viability is performed by a MTT assay. Briefly, T47D cells are plated in 96-well plates for 24 h. Then, the medium is removed and cells were treated with either DMSO as a control or various concentrations of inhibitors. The final concentration of DMSO in the medium was ≤0.1% (v/v). After the cells are incubated for 48 h, 20 μL MTT solution (5 mg/mL) is added to each well for another 4 h at 37 °C. The formazan crystals that formed are dissolved in DMSO (100 μL/well) by constant shaking for 5 min. The plate is then read on a microplate reader at 540 nm. Three replicate wells are used for each analysis. The median inhibitory concentration (IC50, defined as the drug concentration at which cell growth is inhibited by 50%) is assessed from the dose?response curves. To assess the effect of compounds on cell proliferation, T47D cells are cultured with compound (0.1?100 μM) for 48 h before MTT analysis.(Only for Reference)

Synonyms	HS 173, HS173
Molecular Weight	422.46
Formula	C21H18N4O4S
CAS No.	1276110-06-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 78 mg/mL (184.6 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. Kim O, et al. J Med Chem. 2011, 54(7), 2455-2466. 2. Lee H, et al. Cancer Lett. 2013, 328(1), 152-159. 3. Yun SM, et al. Cancer Lett. 2013, 331(2), 250-261. 4. Son MK, et al. Sci Rep. 2013, 3, 3470.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Kinase Inhibitor Library Stem Cell Differentiation Compound Library Bioactive Compounds Library Max Neural Regeneration Compound Library Neuronal Differentiation Compound Library Anti-Cancer Metabolism Compound Library Anti-Pancreatic Cancer Compound Library Antioxidant Compound Library Anti-Colorectal Cancer Compound Library

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

HS-173 1276110-06-5 Apoptosis PI3K/Akt/mTOR signaling PI3K HS 173 Phosphoinositide 3-kinase HS173 Inhibitor inhibit inhibitor

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