KKL-10 | antimicrobial agent | CAS#952849-76-2

MedKoo Cat#: 555140 | Name: KKL-10

Description:

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

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

KKL-10

CAS#952849-76-2

Theoretical Analysis

MedKoo Cat#: 555140

Name: KKL-10

CAS#: 952849-76-2

Chemical Formula: C14H10BrN3O2S

Exact Mass: 362.9677

Molecular Weight: 364.22

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
100mg	USD 550.00	2 Weeks
200mg	USD 950.00	2 Weeks
500mg	USD 1,850.00	2 Weeks
1g	USD 2,950.00	2 Weeks
2g	USD 5,250.00	2 Weeks

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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

Product Data

Instruction

View handling instruction

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

	Solvent	mg/mL	mM
Solubility
	DMSO	2.9	7.93

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 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.

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:

In vivo protocol:

TBD

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.