GSK2837808A

Name: GSK2837808A
Brand: MedChemExpress
SKU: HY-100681
Rating: 5.0 (43 reviews)

製品番号: HY-100681 純度: 99.24%: Data Sheet SDS COA 取扱説明書
FAQs
Technical Support

GSK2837808A is a potent and selective lactate dehydrogenase A (LDHA) inhibitor with IC₅₀s of 2.6 and 43 nM for hLDHA and hLDHB, respectively.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号 : 1445879-21-9

容量	価格（税別）	在庫状況	数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 197	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 197	在庫あり	Estimated Time of Arrival: December 31
Solid
1 mg	$50	在庫あり	Estimated Time of Arrival: December 31
2 mg	$70	在庫あり	Estimated Time of Arrival: December 31
5 mg	$138	在庫あり	Estimated Time of Arrival: December 31
10 mg	$220	在庫あり	Estimated Time of Arrival: December 31
25 mg	$420	在庫あり	Estimated Time of Arrival: December 31
50 mg	$580	在庫あり	Estimated Time of Arrival: December 31
100 mg	$820	在庫あり	Estimated Time of Arrival: December 31
200 mg		お問い合わせ
500 mg		お問い合わせ

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* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 43 publication(s) in Google Scholar

Other Forms of GSK2837808A:

GSK2837808A (Standard) お問い合わせ

顧客検証

Cell Proliferation/Viability Assay

Flow Cytometry

Bio/Physico-chemical Assay

Cell Imaging/Staining

: GSK2837808A purchased from MedChemExpress. Usage Cited in: Cell Metab. 2025 Apr 1;37(4):903-919.e10. [Abstract]; FACS quantification of STAR-based CSC percentage in TPO3 and TPO4 treated with LDHA inhibitor GSK2837808A (GSK, 100 µM, 3 days).

: GSK2837808A purchased from MedChemExpress. Usage Cited in: Gastroenterology. 2024 Jan 24:S0016-5085(24)00064-7. [Abstract]; Phase-contrast images of dysplastic organoids treated with dimethyl sulfoxide (DMSO; vehicle), GSK2837808A (LDH inhibitor; 10 μM), 6-aminonicotinamide (G6PD inhibitor; 50 μM), telaglenastat (GLS1 inhibitor; 1 μM) for 3 days.

: GSK2837808A purchased from MedChemExpress. Usage Cited in: J Ethnopharmacol. 2023 May 23:308:116271.; The conditioned media (CM) from hypoxia-treated NRK-52 E cells reduce the expression of FN, COL-Ⅰ, α-SMA and PCNA proteins in NRK-49 F cells after SSR (Shen Shuai II Recipe) and (or) GSK (GSK2837808A) treatment.

: GSK2837808A purchased from MedChemExpress. Usage Cited in: Nat Commun. 2020 Jun 22;11(1):3162. [Abstract]; Proliferation of HepG2 cells with HULC knockdown (left panel) or overexpression (right panel) was measured with a CCK8 assay. For rescue experiments, HepG2-HULC cells were treated by FGFR1 inhibitor PD 166866 (2.5 μM), PKM2 activator DASA-58 (30 μM), or LDHA inhibitor GSK2837808A (10 μM), respectively.

: GSK2837808A purchased from MedChemExpress. Usage Cited in: Nat Commun. 2020 Jul 9;11(1):3427. [Abstract]; Chondrocytes were treated with IL-1β (10 ng/mL) in the presence of GSK2837808A (10 μM), oxamate (10 mM) or FX11 (40 μM) for 24 hours for supernatant lactic acid measurement.

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製品説明

GSK2837808A is a potent and selective lactate dehydrogenase A (LDHA) inhibitor with IC₅₀s of 2.6 and 43 nM for hLDHA and hLDHB, respectively.

IC₅₀ & Target

IC50: 2.6 nM (hLDHA), 43 nM (hLDHB)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
A673	IC₅₀	>57 3 Compound: 2; GSK 2837808A	Cytotoxicity against human A673 cells after 48 hrs by CellTiter-Glo assay Cytotoxicity against human A673 cells after 48 hrs by CellTiter-Glo assay	[PMID: 29120638]
A673	IC₅₀	0.84 3 Compound: 2; GSK 2837808A	Cytotoxicity against human A673 cells assessed as long term cell growth inhibition measured every 4 hrs for 120 hrs by incucyte zoom live cell analysis Cytotoxicity against human A673 cells assessed as long term cell growth inhibition measured every 4 hrs for 120 hrs by incucyte zoom live cell analysis	[PMID: 29120638]
A673	IC₅₀	> 57 3 Compound: 2; GSK 2837808A	Cytotoxicity against human A673 cells after 48 hrs by CellTiter-Glo assay Cytotoxicity against human A673 cells after 48 hrs by CellTiter-Glo assay	[PMID: 29120638]
A673	IC₅₀	0.84 3 Compound: 2; GSK 2837808A	Cytotoxicity against human A673 cells assessed as long term cell growth inhibition measured every 4 hrs for 120 hrs by incucyte zoom live cell analysis Cytotoxicity against human A673 cells assessed as long term cell growth inhibition measured every 4 hrs for 120 hrs by incucyte zoom live cell analysis	[PMID: 29120638]
A673	IC₅₀	0.84 3 Compound: 2; GSK 2837808A	Cytotoxicity against human A673 cells assessed as long term cell growth inhibition measured every 4 hrs for 120 hrs by incucyte zoom live cell analysis Cytotoxicity against human A673 cells assessed as long term cell growth inhibition measured every 4 hrs for 120 hrs by incucyte zoom live cell analysis	[PMID: 29120638]
A673	IC₅₀	> 57 3 Compound: 2; GSK 2837808A	Cytotoxicity against human A673 cells after 48 hrs by CellTiter-Glo assay Cytotoxicity against human A673 cells after 48 hrs by CellTiter-Glo assay	[PMID: 29120638]
MIA PaCa-2	IC₅₀	1.37 3 Compound: 2; GSK 2837808A	Cytotoxicity against human MIAPaCa2 cells assessed as long term cell growth inhibition measured every 4 hrs for 120 hrs by incucyte zoom live cell analysis Cytotoxicity against human MIAPaCa2 cells assessed as long term cell growth inhibition measured every 4 hrs for 120 hrs by incucyte zoom live cell analysis	[PMID: 29120638]
MIA PaCa-2	IC₅₀	28.4 3 Compound: 2; GSK 2837808A	Cytotoxicity against human MIAPaCa2 cells after 48 hrs by CellTiter-Glo assay Cytotoxicity against human MIAPaCa2 cells after 48 hrs by CellTiter-Glo assay	[PMID: 29120638]
MIA PaCa-2	IC₅₀	1.37 3 Compound: 2; GSK 2837808A	Cytotoxicity against human MIAPaCa2 cells assessed as long term cell growth inhibition measured every 4 hrs for 120 hrs by incucyte zoom live cell analysis Cytotoxicity against human MIAPaCa2 cells assessed as long term cell growth inhibition measured every 4 hrs for 120 hrs by incucyte zoom live cell analysis	[PMID: 29120638]
MIA PaCa-2	IC₅₀	1.37 3 Compound: 2; GSK 2837808A	Cytotoxicity against human MIAPaCa2 cells assessed as long term cell growth inhibition measured every 4 hrs for 120 hrs by incucyte zoom live cell analysis Cytotoxicity against human MIAPaCa2 cells assessed as long term cell growth inhibition measured every 4 hrs for 120 hrs by incucyte zoom live cell analysis	[PMID: 29120638]
MIA PaCa-2	IC₅₀	28.4 3 Compound: 2; GSK 2837808A	Cytotoxicity against human MIAPaCa2 cells after 48 hrs by CellTiter-Glo assay Cytotoxicity against human MIAPaCa2 cells after 48 hrs by CellTiter-Glo assay	[PMID: 29120638]
MIA PaCa-2	IC₅₀	28.4 3 Compound: 2; GSK 2837808A	Cytotoxicity against human MIAPaCa2 cells after 48 hrs by CellTiter-Glo assay Cytotoxicity against human MIAPaCa2 cells after 48 hrs by CellTiter-Glo assay	[PMID: 29120638]

体外実験

GSK2837808A rapidly and profoundly inhibits lactate production rates in multiple cancer cell lines including hepatocellular and breast carcinomas. The potency of GSK2837808A across 30 cancer cell lines with different LDHA and LDHB expression levels ranges from 400 nM to no effect (EC₅₀ reported as 30 μM). GSK2837808A potency does not correlate with LDHA, LDHB, or the total LDH expression levels. GSK2837808A inhibits lactate production in hypoxia but at higher concentrations than in normoxia (EC₅₀=10 μM). It also reduces ECAR with EC₅₀=10 μM. LDH inhibition by GSK2837808A alters multiple metabolic pathways in Snu398 cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

体内実験

Clearance following IV infusion of GSK2837808A at 0.25 mg/kg is shown to be 69 mL/minute/kg in rats, which exceeds the animal liver blood flow. Oral dosing of GSK2837808A at 50 mg/kg in rats or 100 mg/kg in mice results in blood compound levels at or below the detection limit of 2.5 ng/mL^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

649.62

分子式

C₃₁H₂₅F₂N₅O₇S

CAS 番号

1445879-21-9

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(O)C1=CC(OC2=CC(F)=CC(F)=C2)=CC(NC3=C(S(=O)(NC4CC4)=O)C=NC5=CC(C6=CN=C(OC)N=C6OC)=CC=C35)=C1

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶剤 & 溶解度

体外:

DMSO : 50 mg/mL (76.97 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.5394 mL	7.6968 mL	15.3936 mL
5 mM	0.3079 mL	1.5394 mL	3.0787 mL
10 mM	0.1539 mL	0.7697 mL	1.5394 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (3.85 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

純度とドキュメンテーション

純度: 99.24%

Select Batch:

データシート (281 KB) SDS (393 KB)

COA (257 KB) HNMR (285 KB) RP-HPLC (252 KB) LCMS (96 KB)

取扱説明書 (2659 KB)

参考文献

[1]. Billiard J, et al. Quinoline 3-sulfonamides inhibit lactate dehydrogenase A and reverse aerobic glycolysis in cancer cells. Cancer Metab. 2013 Sep 6;1(1):19. [Content Brief]

細胞実験 ^[1]	Sixty thousand Snu398 cells per well are plated in 6-well tissue culture plates in RPMI-1640 medium supplemented with 2.5% charcoal-stripped FBS. Cells are allowed to attach overnight and then DMSO control or the indicated doses of LDHA inhibitor dissolved in DMSO are added directly to the wells. After 4 to 8 days of incubation in the indicated oxygen conditions, adherent cells are trypsinized, counted, and had their viability assessed by the trypan-blue exclusion method using the Vi-Cell XR Cell Viability Analyzer^[1]. MedChemExpress (MCE) はこれらの方法の精度を確認していません。こちらは参照専用です。
動物実験 ^[1]	Mice: GSK2837808A is administered to male CD mice or male Sprague-Dawley rats orally or by intravenous (IV) infusion over 120 minutes into a femoral vein. Arterial blood samples are collected over time and GSK2837808A concentration is determined by liquid chromatography (LC)/MS/MS analysis^[1]. MedChemExpress (MCE) はこれらの方法の精度を確認していません。こちらは参照専用です。
参考文献	[1]. Billiard J, et al. Quinoline 3-sulfonamides inhibit lactate dehydrogenase A and reverse aerobic glycolysis in cancer cells. Cancer Metab. 2013 Sep 6;1(1):19. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.5394 mL	7.6968 mL	15.3936 mL	38.4840 mL
	5 mM	0.3079 mL	1.5394 mL	3.0787 mL	7.6968 mL
	10 mM	0.1539 mL	0.7697 mL	1.5394 mL	3.8484 mL
	15 mM	0.1026 mL	0.5131 mL	1.0262 mL	2.5656 mL
	20 mM	0.0770 mL	0.3848 mL	0.7697 mL	1.9242 mL
	25 mM	0.0616 mL	0.3079 mL	0.6157 mL	1.5394 mL
	30 mM	0.0513 mL	0.2566 mL	0.5131 mL	1.2828 mL
	40 mM	0.0385 mL	0.1924 mL	0.3848 mL	0.9621 mL
	50 mM	0.0308 mL	0.1539 mL	0.3079 mL	0.7697 mL
	60 mM	0.0257 mL	0.1283 mL	0.2566 mL	0.6414 mL

GSK2837808A Related Classifications

Molarity Calculator
Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量		濃度		体積		分子量 *
	=		×		×

The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）	×	体積 _（開始）	=	濃度 _（終了）	×	体積 _（終了）
	×		=		×
C1		V1		C2		V2

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GSK2837808A1445879-21-9Lactate DehydrogenaseLDHInhibitorinhibitorinhibit

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GSK2837808A

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Other Forms of GSK2837808A:

GSK2837808A 関連抗体

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おすすめ

•関連スクリーニングライブラリ:

•関連小分子:

•関連タンパク質:

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純度とドキュメンテーション

参考文献

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GSK2837808A 関連抗体

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

GSK2837808A Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

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