Synonym
JLK6; JLK 6; JLK-6; JCP-251; JCP 251; JCP251
IUPAC/Chemical Name
7-Amino-4-chloro-3-methoxy-isocoumarin
InChi Key
AMDGKLWVCUXONP-UHFFFAOYSA-N
InChi Code
InChI=1S/C10H8ClNO3/c1-14-10-8(11)6-3-2-5(12)4-7(6)9(13)15-10/h2-4H,12H2,1H3
SMILES Code
O=C1OC(OC)=C(Cl)C2=C1C=C(N)C=C2
Purity
>95% (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
>3 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
2934.99.03.00
Biological target:
Inhibitor of γ-secretase-mediated βAPP processing.
In vitro activity:
To investigate the effect of JLK6 on notch1 expression, cells were treated with JLK6, and a Western blot assay was performed to analyze Notch1 expression in the treated and untreated cells. According to the observations, the Notch 1 expression was significantly suppressed in the cells treated with JLK6 (figure 2f). The expression of Notch1 associated proteins including Jag5, Hes1, and Hes 1 were also significantly reduced in the samples treated with the JLK6, Notch1 inhibitor (Figure 2h). RT-qPCR showed similar results (Figure 2g-I).
Reference: Bioengineered. 2022 Apr;13(4):8396-8411. https://pubmed.ncbi.nlm.nih.gov/35383529/
|
Solvent |
mg/mL |
mM |
comments |
| Solubility |
| DMSO |
26.3 |
116.47 |
|
| DMSO:PBS (pH 7.2) (1:5) |
0.2 |
0.71 |
|
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
225.63
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. Liu M, Zhong W, Li C, Su W. Fluoxetine attenuates apoptosis in early brain injury after subarachnoid hemorrhage through Notch1/ASK1/p38 MAPK signaling pathway. Bioengineered. 2022 Apr;13(4):8396-8411. doi: 10.1080/21655979.2022.2037227. PMID: 35383529; PMCID: PMC9162017.
2. Nascimento MT, Franca M, Carvalho AM, Amorim CF, Peixoto F, Beiting D, Scott P, Carvalho EM, Carvalho LP. Inhibition of gamma-secretase activity without interfering in Notch signalling decreases inflammatory response in patients with cutaneous leishmaniasis. Emerg Microbes Infect. 2021 Dec;10(1):1219-1226. doi: 10.1080/22221751.2021.1932608. PMID: 34009107; PMCID: PMC8676695.
In vitro protocol:
1. Liu M, Zhong W, Li C, Su W. Fluoxetine attenuates apoptosis in early brain injury after subarachnoid hemorrhage through Notch1/ASK1/p38 MAPK signaling pathway. Bioengineered. 2022 Apr;13(4):8396-8411. doi: 10.1080/21655979.2022.2037227. PMID: 35383529; PMCID: PMC9162017.
2. Nascimento MT, Franca M, Carvalho AM, Amorim CF, Peixoto F, Beiting D, Scott P, Carvalho EM, Carvalho LP. Inhibition of gamma-secretase activity without interfering in Notch signalling decreases inflammatory response in patients with cutaneous leishmaniasis. Emerg Microbes Infect. 2021 Dec;10(1):1219-1226. doi: 10.1080/22221751.2021.1932608. PMID: 34009107; PMCID: PMC8676695.
1: Peuchmaur M, Lacour MA, Sévalle J, Lisowski V, Touati-Jallabe Y, Rodier F, Martinez J, Checler F, Hernandez JF. Further characterization of a putative serine protease contributing to the γ-secretase cleavage of β-amyloid precursor protein. Bioorg Med Chem. 2013 Feb 15;21(4):1018-29. doi: 10.1016/j.bmc.2012.11.045. Epub 2012 Dec 5. PubMed PMID: 23294826.
2: Bihel F, Quéléver G, Lelouard H, Petit A, Alvès da Costa C, Pourquié O, Checler F, Thellend A, Pierre P, Kraus JL. Synthesis of new 3-alkoxy-7-amino-4-chloro-isocoumarin derivatives as new beta-amyloid peptide production inhibitors and their activities on various classes of protease. Bioorg Med Chem. 2003 Jul 17;11(14):3141-52. PubMed PMID: 12818677.
