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MedKoo Cat#: 530669 | Name: GSK2837808A
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

GSK2837808A is a potent, selective lactate dehydrogenase A (LDHA) inhibitor (IC50 values are 1.9 and 14 nM for LDHA and LDHB respectively).

Chemical Structure

GSK2837808A
GSK2837808A
CAS#1445879-21-9

Theoretical Analysis

MedKoo Cat#: 530669

Name: GSK2837808A

CAS#: 1445879-21-9

Chemical Formula: C31H25F2N5O7S

Exact Mass: 649.1443

Molecular Weight: 649.63

Elemental Analysis: C, 57.32; H, 3.88; F, 5.85; N, 10.78; O, 17.24; S, 4.94

Price and Availability

Size Price Availability Quantity
50mg USD 750.00 2 Weeks
100mg USD 1,350.00 2 Weeks
200mg USD 1,950.00 2 Weeks
500mg USD 3,450.00 2 Weeks
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Related CAS #
No Data
Synonym
GSK2837808A; GSK-2837808A; GSK 2837808A; GSK2837808; GSK-2837808; GSK 2837808.
IUPAC/Chemical Name
3-[[3-[(cyclopropylamino)sulfonyl]-7-(2,4-dimethoxy-5-pyrimidinyl)-4-quinolinyl]amino]-5-(3,5-difluorophenoxy)-benzoic acid
InChi Key
RZBCPMYJIARMGV-UHFFFAOYSA-N
InChi Code
InChI=1S/C31H25F2N5O7S/c1-43-29-25(14-35-31(37-29)44-2)16-3-6-24-26(9-16)34-15-27(46(41,42)38-20-4-5-20)28(24)36-21-7-17(30(39)40)8-22(13-21)45-23-11-18(32)10-19(33)12-23/h3,6-15,20,38H,4-5H2,1-2H3,(H,34,36)(H,39,40)
SMILES Code
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
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
GSK2837808A is a potent and selective lactate dehydrogenase A (LDHA) inhibitor with IC50s of 2.6 and 43 nM for hLDHA and hLDHB, respectively
In vitro activity:
The cell apoptosis were demonstrated by TUNEL staining and Annexin V/PI double staining. A potent and specific inhibitor of LDHA, GSK2837808A, was administrated to suppress the activity of LDHA and detect the potential efficacy on HAS2. LDHA inhibition impaired active LDHA performance, suppressed the glucose uptake and decreased lactate concentration. Furthermore, GSK2837808A reversed the occurrence of low ratio of ATP/AMP, high level of Adenosine Monophosphate-activated Protein Kinase (AMPK) activation, disturbed HAS2 synthesis and hyaluronic acid (HA) production by inhibiting LDHA. The cellular viability and cell cycle were not affected by GSK2837808A at the working concentration. In conclusion, Targeting LDHA using its specific suppressant GSK2837808A impeded lactate secretion and contributed to HAS2 and HA synthesis in TMJOA SFs, providing the vital role of LDHA associated with TMJOA pathogenesis and a novel therapeutic approach for TMJOA. Reference: Bone. 2020 Dec;141:115584. https://pubmed.ncbi.nlm.nih.gov/32795674/
In vivo activity:
TBD
Solvent mg/mL mM
Solubility
DMSO 73.7 113.51
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 649.63 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Li HM, Guo HL, Xu C, Liu L, Hu SY, Hu ZH, Jiang HH, He YM, Li YJ, Ke J, Long X. Inhibition of glycolysis by targeting lactate dehydrogenase A facilitates hyaluronan synthase 2 synthesis in synovial fibroblasts of temporomandibular joint osteoarthritis. Bone. 2020 Dec;141:115584. doi: 10.1016/j.bone.2020.115584. Epub 2020 Aug 11. PMID: 32795674. 2. Qi CL, Huang ML, Zou Y, Yang R, Jiang Y, Sheng JF, Kong YG, Tao ZZ, Feng HY, Hua QQ, Bu LH, Chen SM. The IRF2/CENP-N/AKT signaling axis promotes proliferation, cell cycling and apoptosis resistance in nasopharyngeal carcinoma cells by increasing aerobic glycolysis. J Exp Clin Cancer Res. 2021 Dec 10;40(1):390. doi: 10.1186/s13046-021-02191-3. PMID: 34893086; PMCID: PMC8662847.
In vitro protocol:
1. Li HM, Guo HL, Xu C, Liu L, Hu SY, Hu ZH, Jiang HH, He YM, Li YJ, Ke J, Long X. Inhibition of glycolysis by targeting lactate dehydrogenase A facilitates hyaluronan synthase 2 synthesis in synovial fibroblasts of temporomandibular joint osteoarthritis. Bone. 2020 Dec;141:115584. doi: 10.1016/j.bone.2020.115584. Epub 2020 Aug 11. PMID: 32795674. 2. Qi CL, Huang ML, Zou Y, Yang R, Jiang Y, Sheng JF, Kong YG, Tao ZZ, Feng HY, Hua QQ, Bu LH, Chen SM. The IRF2/CENP-N/AKT signaling axis promotes proliferation, cell cycling and apoptosis resistance in nasopharyngeal carcinoma cells by increasing aerobic glycolysis. J Exp Clin Cancer Res. 2021 Dec 10;40(1):390. doi: 10.1186/s13046-021-02191-3. PMID: 34893086; PMCID: PMC8662847.
In vivo protocol:
TBD
1: Merk A, Bartesaghi A, Banerjee S, Falconieri V, Rao P, Davis MI, Pragani R, Boxer MB, Earl LA, Milne JL, Subramaniam S. Breaking Cryo-EM Resolution Barriers to Facilitate Drug Discovery. Cell. 2016 Jun 16;165(7):1698-707. doi: 10.1016/j.cell.2016.05.040. Epub 2016 May 26. PubMed PMID: 27238019; PubMed Central PMCID: PMC4931924.

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