GSK2837808A | CAS#1445879-21-9 |

GSK2837808A
featured

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

MedKoo CAT#: 530669

CAS#: 1445879-21-9

Description: 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

CAS# 1445879-21-9

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 530669
Name: GSK2837808A
CAS#: 1445879-21-9
Chemical Formula: C31H25F2N5O7S
Exact Mass: 649.14
Molecular Weight: 649.626
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
50mg	USD 750	2 Weeks
100mg	USD 1350	2 Weeks
200mg	USD 1950	2 Weeks
500mg	USD 3450	2 Weeks
1g	USD 5250	2 Weeks
2g	USD 8250	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

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

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	73.7	113.51

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.

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

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.

Mass

Concentration

Volume

M. Wt* g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

Dilution Calculator

Calculate the dilution required to prepare a stock solution.

Concentration 1

Volume 1

Concentration 2

Volume 2

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.

Your view history

GSK2837808A featured