Syrosingopine

Synonyms: Su-3118

Syrosingopine is a dual MCT1 and MCT4 inhibitor with IC50 values of 2500nM and 40 nM in HAP1 cells, respectively.

Syrosingopine Chemical Structure

Syrosingopine Chemical Structure

CAS No. 84-36-6

Purity & Quality Control

Syrosingopine Related Products

Biological Activity

Description Syrosingopine is a dual MCT1 and MCT4 inhibitor with IC50 values of 2500nM and 40 nM in HAP1 cells, respectively.
Targets
MCT4 [1]
(in HAP1 cell)
MCT1 [1]
(in HAP1 cell)
40 nM 2500 nM
In vitro
In vitro

Syrosingopine treatment leads to high intracellular lactate levels and thereby end-product inhibition of lactate dehydrogenase by inhibiting the Lactate Transporters MCT1 and MCT4. The loss of NAD+ regeneration capacity due to combined metformin and syrosingopine treatment results in glycolytic blockade, leading to ATP depletion and cell death. <sup><a class="sref" href="#s_ref">[1]</a></sup>

Cell Research Cell lines HCT116 cells, HeLa, HAP1
Concentrations 10 μM
Incubation Time 2 h
Method

HCT116 cells are grown to 80% confluency in DMEM and pre-treated with compounds (10 μM) for 2 hours. After ishing with PBS, cytosolic depletion is performed by scraping cells and incubating with 1.9ml digitonin buffer for 30 minutes on ice.And then used for DARTS assay. For ATP and lactate measurement,HeLa and HAP1 are seeded at 15000 cells/well or 30000 cells/well. After Syrosingopine incubation, cells are ished with PBS and lysed with 22.5 μL HCl. Cell lysates are neutralized with 7.5 μL 1M Tris-base and incubated with 30 μL detection reagent. Luminescence is recorded after 1 hour and intracellular lactate concentrations determined from a standard curve.

In Vivo
In vivo

Syrosingopine treatment leads to reduced serum lactate levels significantlyn, and higher intracellular lactate from liver tumor nodules in syrosingopine-treated liver tumor model mice. <sup><a class="sref" href="#s_ref">[1]</a></sup>

Animal Research Animal Models Liver-specific Tsc1 and Pten double-knockout mice
Dosages 7.5 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 666.71 Formula

C35H42N2O11

CAS No. 84-36-6 SDF --
Smiles CCOC(=O)OC1=C(OC)C=C(C=C1OC)C(=O)OC2CC3CN4CCC5=C([NH]C6=C5C=CC(=C6)OC)C4CC3C(C2OC)C(=O)OC
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (149.99 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 5 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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