2. Metabolic Enzyme/Protease
  3. Lactate Dehydrogenase
  4. GSK2837808A

GSK2837808A 

Cat. No.: HY-100681 Purity: ≥99.0%
COA Handling Instructions

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

For research use only. We do not sell to patients.

GSK2837808A Chemical Structure

GSK2837808A Chemical Structure

CAS No. : 1445879-21-9

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Solution
10 mM * 1 mL in DMSO USD 214 In-stock
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10 mM * 1 mL
ready for reconstitution
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Solid
2 mg USD 70 In-stock
5 mg USD 150 In-stock
10 mg USD 250 In-stock
25 mg USD 550 In-stock
50 mg USD 990 In-stock
100 mg USD 1750 In-stock
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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 14 publication(s) in Google Scholar

Top Publications Citing Use of Products

    GSK2837808A purchased from MCE. Usage Cited in: J Ethnopharmacol. 2023 May 23.

    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.

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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]
    In Vitro

    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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    In Vivo

    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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Molecular Weight

    649.62

    Appearance

    Solid

    Formula

    C31H25F2N5O7S
    CAS No.
    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
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (76.97 mM; Need ultrasonic)

    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
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 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

    *All of the co-solvents are available by MCE.
    Purity & Documentation

    Purity: ≥99.0%

    COA (257 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [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].

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

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    This equation is commonly abbreviated as: C1V1 = C2V2

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    Keywords:

    GSK2837808A1445879-21-9Lactate DehydrogenaseLDHInhibitorinhibitorinhibit

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