L67 | CAS#325970-71-6 | DNA Ligase Inhibitor

MedKoo Cat#: 407299 | Name: L67

Description:

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

L67 is a DNA Ligase Inhibitor. L67 inhibited DNA ligases I and III. L67 is a simple competitive inhibitor with respect to nicked DNA. L67 inhibits DNA ligases I and III with IC₅₀ values of 10 μM and 10 μM.). L67 significantly increased the cytotoxicity of DNA-damaging.

Chemical Structure

L67

CAS#325970-71-6

Theoretical Analysis

MedKoo Cat#: 407299

Name: L67

CAS#: 325970-71-6

Chemical Formula: C16H14Br2N4O4

Exact Mass: 483.9382

Molecular Weight: 486.12

Elemental Analysis: C, 39.53; H, 2.90; Br, 32.87; N, 11.53; O, 13.16

Price and Availability

Size	Price	Availability
50mg	USD 150.00	Ready to ship
100mg	USD 250.00	Ready to ship
200mg	USD 450.00	Ready to ship
500mg	USD 850.00	Ready to ship
1g	USD 1,450.00	Ready to ship
2g	USD 2,450.00	Ready to ship

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Related CAS #

No Data

Synonym

L67; L-67; L 67.

IUPAC/Chemical Name

E-2-((3,5-Dibromo-4-methylphenyl)amino)-N’-(2-hydroxy-5-nitrobenzylidene)acetohydrazide

InChi Key

KFEPVFJQVOMODD-IFRROFPPSA-N

InChi Code

InChI=1S/C16H14Br2N4O4/c1-9-13(17)5-11(6-14(9)18)19-8-16(24)21-20-7-10-4-12(22(25)26)2-3-15(10)23/h2-7,19,23H,8H2,1H3,(H,21,24)/b20-7+

SMILES Code

O=C(N/N=C/C1=CC([N+]([O-])=O)=CC=C1O)CNC2=CC(Br)=C(C)C(Br)=C2

Appearance

Light yellow to yellow 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, not in water

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

Certificate of Analysis

View CoA: current batch, Lot#CRB60801

QC Data

View QC data: current batch, Lot#CRB60801

Safety Data Sheet (SDS)

View Safety Data Sheet (SDS)

Instruction

View handling instruction

Biological target:

L67 is a novel, competitive human DNA ligase inhibitor, inhibits DNA ligases I and III with IC50 of 10 μM and 10 μM.

In vitro activity:

To determine the mechanisms underlying the cytotoxicity of the LigI/III inhibitor L67, derivatives of cell lines established from cervical (HeLa, Supplementary Figure S1A), breast (MDA-MB-231) and colon (HCT116) cancers that lack mito DNA (Rho minus) were selected by growth in the presence of ethidium bromide, pyruvate and uridine. HeLa cells with abnormal mitochondria that lack mitochondrial DNA (Supplementary Figure S1A and B) were more resistant to L67 in colony forming (Fig. 1A) and cell proliferation assays (Fig. 1B) with the absence of mitochondrial DNA increasing the IC50 from 8.2 µM to 29.7 µM (Supplementary Table 1). The differential effect of L67 on HeLa and HeLa Rho minus cells was also observed when HeLa cells were grown in the media containing pyruvate and uridine (Supplementary Figure S1C). MDA-MB-231 and HCT 116 cells lacking mitochondrial DNA were also more resistant to L67 compared with their respective parental cells (Fig. 1C and D, and Supplementary Table 1), suggesting that, at lower concentrations, L67 causes cell death by targeting mitochondrial function. Reference: Cancer Res. 2016 Sep 15; 76(18): 5431–5441. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5036517/

In vivo activity:

TBD

	Solvent	mg/mL	mM
Solubility
	DMSO	21.5	44.23
	DMF	10.0	20.57
	Water	1.0	2.06

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 486.12 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. Sallmyr A, Matsumoto Y, Roginskaya V, Van Houten B, Tomkinson AE. Inhibiting Mitochondrial DNA Ligase IIIα Activates Caspase 1-Dependent Apoptosis in Cancer Cells. Cancer Res. 2016 Sep 15;76(18):5431-41. doi: 10.1158/0008-5472.CAN-15-3243. Epub 2016 Aug 8. PMID: 27503931; PMCID: PMC5036517.

In vitro protocol:

In vivo protocol:

TBD

1: Chen X, Zhong S, Zhu X, Dziegielewska B, Ellenberger T, Wilson GM, MacKerell AD Jr, Tomkinson AE. Rational design of human DNA ligase inhibitors that target cellular DNA replication and repair. Cancer Res. 2008 May 1;68(9):3169-77. doi: 10.1158/0008-5472.CAN-07-6636. PubMed PMID: 18451142; PubMed Central PMCID: PMC2734474.