KKL-10
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MedKoo CAT#: 555140

CAS#: 952849-76-2

Description: KKL-10 is an antimicrobial agent. KKL-10 exhibited exceptional antimicrobial activity against both attenuated and fully virulent strains of F. tularensis in vitro and during ex vivo infection. Addition of KKL-10 to macrophages or liver cells at any time after infection by F. tularensis prevented further bacterial proliferation. When macrophages were stimulated with the proinflammatory cytokine gamma interferon before being infected by F. tularensis, addition of KKL-10 reduced intracellular bacteria by >99%, indicating that the combination of cytokine-induced stress and a nonfunctional ribosome rescue pathway is fatal to F. tularensis. KKL-10 is a good lead compound for antibiotic development.


Chemical Structure

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KKL-10
CAS# 952849-76-2

Theoretical Analysis

MedKoo Cat#: 555140
Name: KKL-10
CAS#: 952849-76-2
Chemical Formula: C14H10BrN3O2S
Exact Mass: 362.97
Molecular Weight: 364.217
Elemental Analysis: C, 46.17; H, 2.77; Br, 21.94; N, 11.54; O, 8.79; S, 8.80

Price and Availability

Size Price Availability Quantity
100mg USD 550 2 Weeks
200mg USD 950 2 Weeks
500mg USD 1850 2 Weeks
1g USD 2950 2 Weeks
2g USD 5250 2 Weeks
Bulk inquiry

Synonym: KKL-10; KKL 10; KKL10.

IUPAC/Chemical Name: 5-bromo-N-(5-(p-tolyl)-1,3,4-oxadiazol-2-yl)thiophene-2-carboxamide

InChi Key: QKSDWSBGDVYRKQ-UHFFFAOYSA-N

InChi Code: InChI=1S/C14H10BrN3O2S/c1-8-2-4-9(5-3-8)13-17-18-14(20-13)16-12(19)10-6-7-11(15)21-10/h2-7H,1H3,(H,16,18,19)

SMILES Code: O=C(C1=CC=C(Br)S1)NC2=NN=C(C3=CC=C(C)C=C3)O2

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: Bacteria require at least one pathway to rescue ribosomes stalled at the ends of mRNAs. The primary pathway for ribosome rescue is trans-translation, which is conserved in >99% of sequenced bacterial genomes. Some species also have backup systems, such as ArfA or ArfB, which can rescue ribosomes in the absence of sufficient trans-translation activity. Small-molecule inhibitors of ribosome rescue have broad-spectrum antimicrobial activity against bacteria grown in liquid culture.

Product Data:
Biological target: KKL-10 is a small-molecule ribosome rescue inhibitor with broad-spectrum antimicrobial activity against bacteria.
In vitro activity: The inhibitors KKL-10 and KKL-40 exhibited exceptional antimicrobial activity against both attenuated and fully virulent strains of F. tularensis in vitro and during ex vivo infection. Addition of KKL-10 or KKL-40 to macrophages or liver cells at any time after infection by F. tularensis prevented further bacterial proliferation. Reference: Antimicrob Agents Chemother. 2016 May 23;60(6):3276-82. https://pubmed.ncbi.nlm.nih.gov/26953190/
In vivo activity: TBD

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 2.9 7.93

Preparing Stock Solutions

The following data is based on the product molecular weight 364.22 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. Goralski TD, Dewan KK, Alumasa JN, Avanzato V, Place DE, Markley RL, Katkere B, Rabadi SM, Bakshi CS, Keiler KC, Kirimanjeswara GS. Inhibitors of Ribosome Rescue Arrest Growth of Francisella tularensis at All Stages of Intracellular Replication. Antimicrob Agents Chemother. 2016 May 23;60(6):3276-82. doi: 10.1128/AAC.03089-15. PMID: 26953190; PMCID: PMC4879415.
In vitro protocol: 1. Goralski TD, Dewan KK, Alumasa JN, Avanzato V, Place DE, Markley RL, Katkere B, Rabadi SM, Bakshi CS, Keiler KC, Kirimanjeswara GS. Inhibitors of Ribosome Rescue Arrest Growth of Francisella tularensis at All Stages of Intracellular Replication. Antimicrob Agents Chemother. 2016 May 23;60(6):3276-82. doi: 10.1128/AAC.03089-15. PMID: 26953190; PMCID: PMC4879415.
In vivo protocol: TBD

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