GSK-LSD1 2HCl

Alias: GSK-LSD1 dihydrochloride; GSK-LSD1; GSK-LSD 1; GSK-LSD-1; GSK-LSD1 2HCl; GSK-LSD1 (trans-racemic) dihydrochloride; GSK-LSD1 HCl;
Cat No.:V0376 Purity: ≥98%
GSK-LSD1 2HCl, thedihydrochloride salt of GSK-LSD1 (GSK-LSD-1), is an irreversible, potent and selectiveinhibitor ofLysine (K) -specific demethylase 1A (LSD1) with antineoplastic activity.
GSK-LSD1 2HCl Chemical Structure CAS No.: 1821798-25-7
Product category: Histone Demethylase
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
2mg
5mg
10mg
25mg
50mg
100mg
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Other Forms of GSK-LSD1 2HCl:

  • GSK-LSD1 dihydrochloride
  • GSK-LSD1
  • GSK-LSD1 hydrochloride
  • GSK-LSD1
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

GSK-LSD1 2HCl, the dihydrochloride salt of GSK-LSD1 (GSK-LSD-1), is an irreversible, potent and selective inhibitor of Lysine (K) -specific demethylase 1A (LSD1) with antineoplastic activity. It inhibits LSD1 with an IC50 of 16 nM, and shows > 1000 fold selectivity for LSD1 over other closely related FAD dependent enzymes such as LSD2, MAO-A, and MAO-B. It displays potent in vitro antiproliferative activity and high in vivo antitumor efficacy.

Biological Activity I Assay Protocols (From Reference)
ln Vitro

In vitro activity: GSK-LSD1 induces gene expression changes in cancer cell lines with average EC50 of < 5 nM and inhibits cancer cell line growth with average EC50 of < 5 nM.


Kinase Assay: GSK-LSD1 Dihydrochloride is a potent, selective and irreversible lysine specific demethylase 1 (LSD1) inhibitor with an IC50 of 16 nM.


Cell Assay: GSK-LSD1 2HCl irreversibly inhibited LSD1 with IC50 value of 16 nM and is > 1000 fold selective over LSD2, MAO-A and MAO-B, which were related to FAD utilizing enzymes. In cancer cell lines, GSK-LSD1 2HCl changed gene expression with average EC50 value < 5 nM and inhibited cells growth with average EC50 value < 5 nM. GSK-LSD1 2HCl (10 ?M) inhibited human recombinant dopamine transporter, 5-HT1A and 5-HT transporter by 39%, 49% and 74%, respectively. And no activity against other 55 recombinant receptors (GPCR, transporters, ion channels). GSK-LSD1 2HCl can be used as a chemical probe and a part of the SGC epigenetics.

ln Vivo
NA
Animal Protocol
NA
NA
References
Biochim Biophys Acta. 2017 Aug 8;1864(12):2428-2437.; http://www.thesgc.org/chemical-probes/LSD1.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C14H22CL2N2
Molecular Weight
289.243881702423
CAS #
1821798-25-7
Related CAS #
2102933-95-7 (rel-2HCl);1431367-49-5 (rel-HCl);1431368-48-7 (rel-free base);1821798-25-7 (2HCl);1431367-51-9 (HCl);1431368-50-1;
SMILES
[H]Cl.[H]Cl.C1(N[C@H]2[C@H](C3=CC=CC=C3)C2)CCNCC1
InChi Key
PJFZOGMSPBHPNS-WICJZZOFSA-N
InChi Code
InChI=1S/C14H20N2.2ClH/c1-2-4-11(5-3-1)13-10-14(13)16-12-6-8-15-9-7-12;;/h1-5,12-16H,6-10H2;2*1H/t13-,14+;;/m0../s1
Chemical Name
rel- N-[(1R,2S)-2-Phenylcyclopropyl]-4-Piperidinamine hydrochloride (1:2)
Synonyms
GSK-LSD1 dihydrochloride; GSK-LSD1; GSK-LSD 1; GSK-LSD-1; GSK-LSD1 2HCl; GSK-LSD1 (trans-racemic) dihydrochloride; GSK-LSD1 HCl;
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO:≥ 60 mg/mL
Water: N/A
Ethanol: N/A
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.4573 mL 17.2867 mL 34.5734 mL
5 mM 0.6915 mL 3.4573 mL 6.9147 mL
10 mM 0.3457 mL 1.7287 mL 3.4573 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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