WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 574767
CAS#: 321695-57-2
Description: L-002 is an inhibitor of p300 histone acyltransferase (KAT3B). L-002 also inhibits acetylation of histones and p53 and suppresses STAT3 activation. In vivo, L-002 potently suppressed tumor growth of TNBC cell line MDA-MB-468 xenografts.
MedKoo Cat#: 574767
Name: L-002
CAS#: 321695-57-2
Chemical Formula: C15H15NO5S
Exact Mass: 321.0671
Molecular Weight: 321.347
Elemental Analysis: C, 56.07; H, 4.71; N, 4.36; O, 24.89; S, 9.98
Synonym: L-002, L 002, L002; p300/CBP Inhibitor VI; NSC 764414
IUPAC/Chemical Name: 2,6-dimethyl-2,5-cyclohexadiene-1,4-dione 4-[O-[(4-methoxyphenyl)sulfonyl]oxime]
InChi Key: VEWFTYOFWIXCIO-UHFFFAOYSA-N
InChi Code: InChI=1S/C15H15NO5S/c1-10-8-12(9-11(2)15(10)17)16-21-22(18,19)14-6-4-13(20-3)5-7-14/h4-9H,1-3H3
SMILES Code: COC1=CC=C(S(O/N=C2C=C(C)C(C(C)=C\2)=O)(=O)=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: >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: 2934.99.9001
| Biological target: | L002 is a potent, cell permeable, reversible and specific acetyltransferase p300 (KAT3B) inhibitor with an IC50 of 1.98 μM. |
| In vitro activity: | Among the NCI-60 panel of cancer cell lines, leukemia and lymphoma cell lines were extremely sensitive to L002, whereas it is toxic to only a limited number of cell lines derived from solid tumors. Notably, breast cancer cell lines, especially those derived from TNBC, were highly susceptible to L002. Reference: Mol Cancer Ther. 2013 May;12(5):610-20. https://pubmed.ncbi.nlm.nih.gov/23625935/ |
| In vivo activity: | Treatment of hypertensive mice with ATp300-specific small molecule inhibitor L002 or C646 reverses hypertension-induced left ventricular hypertrophy, cardiac fibrosis and diastolic dysfunction, without reducing elevated blood pressures. Biochemically, treatment with L002 and C646 also reverse hypertension-induced histone acetylation and myofibroblast differentiation in murine ventricles. Reference: J Cell Mol Med. 2019 Apr;23(4):3026-3031. https://pubmed.ncbi.nlm.nih.gov/30710427/ |
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMF | 30.0 | 93.36 | |
| DMSO | 52.17 | 162.34 | |
| DMSO:PBS (pH 7.2) (1:2) | 0.25 | 0.78 | |
| Ethanol | 2.5 | 7.78 |
The following data is based on the product molecular weight 321.347 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. Rai R, Verma SK, Kim D, Ramirez V, Lux E, Li C, Sahoo S, Wilsbacher LD, Vaughan DE, Quaggin SE, Ghosh AK. A novel acetyltransferase p300 inhibitor ameliorates hypertension-associated cardio-renal fibrosis. Epigenetics. 2017;12(11):1004-1013. doi: 10.1080/15592294.2017.1370173. Epub 2017 Dec 6. PMID: 28933600; PMCID: PMC5788418. 2. Yang H, Pinello CE, Luo J, Li D, Wang Y, Zhao LY, Jahn SC, Saldanha SA, Chase P, Planck J, Geary KR, Ma H, Law BK, Roush WR, Hodder P, Liao D. Small-molecule inhibitors of acetyltransferase p300 identified by high-throughput screening are potent anticancer agents. Mol Cancer Ther. 2013 May;12(5):610-20. doi: 10.1158/1535-7163.MCT-12-0930. Epub 2013 Apr 26. Erratum in: Mol Cancer Ther. 2013 Aug;12(8):1688. Chase, Peter [added]. PMID: 23625935; PMCID: PMC3651759. 3. Rai R, Sun T, Ramirez V, Lux E, Eren M, Vaughan DE, Ghosh AK. Acetyltransferase p300 inhibitor reverses hypertension-induced cardiac fibrosis. J Cell Mol Med. 2019 Apr;23(4):3026-3031. doi: 10.1111/jcmm.14162. Epub 2019 Feb 1. PMID: 30710427; PMCID: PMC6433695. 4. Rai R, Verma SK, Kim D, Ramirez V, Lux E, Li C, Sahoo S, Wilsbacher LD, Vaughan DE, Quaggin SE, Ghosh AK. A novel acetyltransferase p300 inhibitor ameliorates hypertension-associated cardio-renal fibrosis. Epigenetics. 2017;12(11):1004-1013. doi: 10.1080/15592294.2017.1370173. Epub 2017 Dec 6. PMID: 28933600; PMCID: PMC5788418. |
| In vitro protocol: | 1. Rai R, Verma SK, Kim D, Ramirez V, Lux E, Li C, Sahoo S, Wilsbacher LD, Vaughan DE, Quaggin SE, Ghosh AK. A novel acetyltransferase p300 inhibitor ameliorates hypertension-associated cardio-renal fibrosis. Epigenetics. 2017;12(11):1004-1013. doi: 10.1080/15592294.2017.1370173. Epub 2017 Dec 6. PMID: 28933600; PMCID: PMC5788418. 2. Yang H, Pinello CE, Luo J, Li D, Wang Y, Zhao LY, Jahn SC, Saldanha SA, Chase P, Planck J, Geary KR, Ma H, Law BK, Roush WR, Hodder P, Liao D. Small-molecule inhibitors of acetyltransferase p300 identified by high-throughput screening are potent anticancer agents. Mol Cancer Ther. 2013 May;12(5):610-20. doi: 10.1158/1535-7163.MCT-12-0930. Epub 2013 Apr 26. Erratum in: Mol Cancer Ther. 2013 Aug;12(8):1688. Chase, Peter [added]. PMID: 23625935; PMCID: PMC3651759. |
| In vivo protocol: | 1. Rai R, Sun T, Ramirez V, Lux E, Eren M, Vaughan DE, Ghosh AK. Acetyltransferase p300 inhibitor reverses hypertension-induced cardiac fibrosis. J Cell Mol Med. 2019 Apr;23(4):3026-3031. doi: 10.1111/jcmm.14162. Epub 2019 Feb 1. PMID: 30710427; PMCID: PMC6433695. 2. Rai R, Verma SK, Kim D, Ramirez V, Lux E, Li C, Sahoo S, Wilsbacher LD, Vaughan DE, Quaggin SE, Ghosh AK. A novel acetyltransferase p300 inhibitor ameliorates hypertension-associated cardio-renal fibrosis. Epigenetics. 2017;12(11):1004-1013. doi: 10.1080/15592294.2017.1370173. Epub 2017 Dec 6. PMID: 28933600; PMCID: PMC5788418. |
1. Yang, H., Pinello, C.E., Luo, J., et al. Small-molecule inhibitors of acetyltransferase p300 identified by high-throughput screening are potent anticancer agents. Molecular Cancer Therapeutics 12(5), 610-620 (2013).
