Synonym
OG-L002; OGL002; OG L002
IUPAC/Chemical Name
4'-((1R,2S)-2-aminocyclopropyl)biphenyl-3-ol
InChi Key
DSOJSZXQRJGBCW-CABCVRRESA-N
InChi Code
InChI=1S/C15H15NO/c16-15-9-14(15)11-6-4-10(5-7-11)12-2-1-3-13(17)8-12/h1-8,14-15,17H,9,16H2/t14-,15+/m1/s1
SMILES Code
OC1=CC(C2=CC=C([C@@H]3[C@@H](N)C3)C=C2)=CC=C1
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
Biological target:
OG-L002 is a potent and highly selective LSD1 inhibitor with an IC50 of 0.02 μM.
In vitro activity:
As shown in Fig. 2, compound OG-L002, which is highly specific to LSD1 (IC50, ~0.02 µM), potently inhibited the expression of viral IE (ICP27 and ICP4) genes, but not cellular control genes. As shown, OG-L002 inhibited viral IE gene expression in both cells with a significantly reduced IC50 (IC50, ~10 µM in HeLa cells; IC50, ~3 µM in HFF cells) relative to the control MAOI TCP (IC50, ~1 mM). In addition, OG-L002 potently reduced viral yields (~100-fold) in comparison to control DMSO treatment.
Reference: mBio. 2013 Feb 5;4(1):e00558-12. https://pubmed.ncbi.nlm.nih.gov/23386436/
In vivo activity:
Here, this study analysed the activation by lipopolysaccaride (LPS) of primary splenocytes obtained from two different Ogg1-/- mouse strains. This study found that the induction of TNF-α expression was reduced in splenocytes (in particular macrophages) of both Ogg1-/- strains. Notably, an inhibitor of LSD1, OG-L002, reduced the induction of TNF-α mRNA in splenocytes from wild-type mice to the level observed in splenocytes from Ogg1-/- mice and had no influence in the latter cells.
Reference: DNA Repair (Amst). 2017 Oct;58:13-20. https://pubmed.ncbi.nlm.nih.gov/28843610/
|
Solvent |
mg/mL |
mM |
| Solubility |
| DMF |
50.0 |
221.94 |
| DMSO |
91.9 |
407.84 |
| DMSO:PBS (pH 7.2) (1:1) |
0.5 |
2.22 |
| Ethanol |
17.2 |
76.24 |
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
225.29
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. Tallmadge RL, Žygelytė E, Van de Walle GR, Kristie TM, Felippe MJB. Effect of a Histone Demethylase Inhibitor on Equine Herpesvirus-1 Activity In Vitro. Front Vet Sci. 2018 Mar 12;5:34. doi: 10.3389/fvets.2018.00034. PMID: 29594155; PMCID: PMC5857540.
2. Liang Y, Quenelle D, Vogel JL, Mascaro C, Ortega A, Kristie TM. A novel selective LSD1/KDM1A inhibitor epigenetically blocks herpes simplex virus lytic replication and reactivation from latency. mBio. 2013 Feb 5;4(1):e00558-12. doi: 10.1128/mBio.00558-12. PMID: 23386436; PMCID: PMC3565832.
3. Seifermann M, Ulges A, Bopp T, Melcea S, Schäfer A, Oka S, Nakabeppu Y, Klungland A, Niehrs C, Epe B. Role of the DNA repair glycosylase OGG1 in the activation of murine splenocytes. DNA Repair (Amst). 2017 Oct;58:13-20. doi: 10.1016/j.dnarep.2017.08.005. Epub 2017 Aug 12. PMID: 28843610.
In vitro protocol:
1. Tallmadge RL, Žygelytė E, Van de Walle GR, Kristie TM, Felippe MJB. Effect of a Histone Demethylase Inhibitor on Equine Herpesvirus-1 Activity In Vitro. Front Vet Sci. 2018 Mar 12;5:34. doi: 10.3389/fvets.2018.00034. PMID: 29594155; PMCID: PMC5857540.
2. Liang Y, Quenelle D, Vogel JL, Mascaro C, Ortega A, Kristie TM. A novel selective LSD1/KDM1A inhibitor epigenetically blocks herpes simplex virus lytic replication and reactivation from latency. mBio. 2013 Feb 5;4(1):e00558-12. doi: 10.1128/mBio.00558-12. PMID: 23386436; PMCID: PMC3565832.
In vivo protocol:
1. Seifermann M, Ulges A, Bopp T, Melcea S, Schäfer A, Oka S, Nakabeppu Y, Klungland A, Niehrs C, Epe B. Role of the DNA repair glycosylase OGG1 in the activation of murine splenocytes. DNA Repair (Amst). 2017 Oct;58:13-20. doi: 10.1016/j.dnarep.2017.08.005. Epub 2017 Aug 12. PMID: 28843610.
1: Tallmadge RL, Žygelytė E, Van de Walle GR, Kristie TM, Felippe MJB. Effect of a Histone Demethylase Inhibitor on Equine Herpesvirus-1 Activity In Vitro. Front Vet Sci. 2018 Mar 12;5:34. doi: 10.3389/fvets.2018.00034. PMID: 29594155; PMCID: PMC5857540.
2: Matsuoka S, Petri G, Larson K, Behnke A, Wang X, Peng M, Spagnoli S, Lohr C, Milston-Clements R, Divilov K, Jin L. Evaluation of Histone Demethylase Inhibitor ML324 and Acyclovir against Cyprinid herpesvirus 3 Infection. Viruses. 2023 Jan 5;15(1):163. doi: 10.3390/v15010163. PMID: 36680202; PMCID: PMC9863241.
3: Harancher MR, Packard JE, Cowan SP, DeLuca NA, Dembowski JA. Antiviral Properties of the LSD1 Inhibitor SP-2509. J Virol. 2020 Sep 15;94(19):e00974-20. doi: 10.1128/JVI.00974-20. PMID: 32699090; PMCID: PMC7495396.
4: Zhang Z, Aoki H, Umezawa K, Kranrod J, Miyazaki N, Oshima T, Hirao T, Miura Y, Seubert J, Ito K, Aoki S. Potential role of lipophagy impairment for anticancer effects of glycolysis-suppressed pancreatic ductal adenocarcinoma cells. Cell Death Discov. 2024 Apr 5;10(1):166. doi: 10.1038/s41420-024-01933-4. PMID: 38580661; PMCID: PMC10997792.
5: Seifermann M, Ulges A, Bopp T, Melcea S, Schäfer A, Oka S, Nakabeppu Y, Klungland A, Niehrs C, Epe B. Role of the DNA repair glycosylase OGG1 in the activation of murine splenocytes. DNA Repair (Amst). 2017 Oct;58:13-20. doi: 10.1016/j.dnarep.2017.08.005. Epub 2017 Aug 12. PMID: 28843610.
6: Liang et al (2013) A novel selective LSD1/KDM1A inhibitor epigenetically blocks herpes simplex virus lytic replication and reactivation from latency. MBio. 4 e00558 PMID: 23386436
