GSK1733953A
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MedKoo CAT#: 525856

CAS#: 930470-97-6

Description: GSK1733953A, also known as DG70, a respiration inhibitor in M. tuberculosis, inhibits MenG activity with an IC50 value of 2.6 ± 0.6 μM. DG70 inhibited the final step in menaquinone biosynthesis. DG70 also inhibited oxygen utilization and ATP biosynthesis, which was reversed by external menaquinone supplementation. DG70 was bactericidal in actively replicating cultures and in a nutritionally deprived persistence model. DG70 was synergistic with the first-line TB drugs isoniazid, rifampin, and the respiratory inhibitor bedaquiline.

Chemical Structure

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GSK1733953A
CAS# 930470-97-6
Instruction

Theoretical Analysis

MedKoo Cat#: 525856
Name: GSK1733953A
CAS#: 930470-97-6
Chemical Formula: C21H17ClFNO3
Exact Mass: 385.09
Molecular Weight: 385.819
Elemental Analysis: C, 65.38; H, 4.44; Cl, 9.19; F, 4.92; N, 3.63; O, 12.44

Price and Availability

Size Price Availability Quantity
50mg USD 450 2 Weeks
100mg USD 750 2 Weeks
200mg USD 1250 2 Weeks
500mg USD 2650 2 Weeks
1g USD 4250 2 Weeks
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Related CAS #: 930470-97-6    

Synonym: GSK1733953A; GSK-1733953A; GSK 1733953A; DG70; DG-70; DG 70;

IUPAC/Chemical Name: 2-Chloro-N-(6,4"-dimethoxy-biphenyl-3-yl)-4-fluoro-benzamide

InChi Key: RWSCJEILSRMTEH-UHFFFAOYSA-N

InChi Code: InChI=1S/C21H17ClFNO3/c1-26-16-7-3-13(4-8-16)18-12-15(6-10-20(18)27-2)24-21(25)17-9-5-14(23)11-19(17)22/h3-12H,1-2H3,(H,24,25)

SMILES Code: COC1=C(C2=CC=C(OC)C=C2)C=C(NC(C3=C(Cl)C=C(F)C=C3)=O)C=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:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 385.82 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:
In vitro protocol:
In vivo protocol:

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1: Sukheja P, Kumar P, Mittal N, Li SG, Singleton E, Russo R, Perryman AL, Shrestha R, Awasthi D, Husain S, Soteropoulos P, Brukh R, Connell N, Freundlich JS, Alland D. A Novel Small-Molecule Inhibitor of the Mycobacterium tuberculosis Demethylmenaquinone Methyltransferase MenG Is Bactericidal to Both Growing and Nutritionally Deprived Persister Cells. MBio. 2017 Feb 14;8(1). pii: e02022-16. doi: 10.1128/mBio.02022-16. PubMed PMID: 28196957; PubMed Central PMCID: PMC5312080.

2. Pujari V, Rozman K, Dhiman RK, Aldrich CC, Crick DC. Mycobacterial MenG: Partial Purification, Characterization, and Inhibition. ACS Infect Dis. 2022 Dec 9;8(12):2430-2440. doi: 10.1021/acsinfecdis.2c00190. Epub 2022 Nov 23. PMID: 36417754.