GSK2807 Trifluoroacetate

SKU: orb1309603

Description

GSK2807 Trifluoroacetate is a potent and selective SMYD3 inhibitor that competes with S-adenosylmethionine (SAM), exhibiting a Ki of 14 nM and an IC50 of 130 nM. This compound is a valuable chemical probe for studying SMYD3's role in oncology and epigenetics, supporting both in vitro biochemical assays and in vivo cancer model research.

Research Area

Epigenetics & Chromatin

Key Properties

• CAS Number: 2245255-66-5
• MW: 566.53
• Purity: 99.95%
• Formula: C₂₁H₃₃F₃N₈O₇
• SMILES: OC(=O)C(F)(F)F.CN(C)CCCN(CC[C@H](N)C(O)=O)C[C@H]1O[C@H]([C@H](O)[C@@H]1O)n1cnc2c(N)ncnc12
• Target: Histone Methyltransferase
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.53 mM);H2O:50 mg/mL (88.26 mM)

Bioactivity

• Target IC50:
  SMYD3:130 nM|SMYD3:14 nM (ki)
• In Vitro:
  GSK2807, a potent and selective, SAM-competitive inhibitor of SMYD3 (Ki = 14 nM). A high-resolution crystal structure reveals that GSK2807 bridges the gap between the SAM-binding pocket and the substrate lysine tunnel of SMYD3. GSK2807 is 24-fold selective for SMYD3 in comparison with the closely related enzyme SMYD2 (Ki=14±6 nM and 345±36 nM, respectively) .

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, Inhibitor, GSK 2807, GSK 2807 Trifluoroacetate, GSK-2807, GSK2807 Trifluoroacetate, GSK-2807 Trifluoroacetate, GSK2807, Histone Methyltransferase, HistoneMethyltransferase, SMYD3

Compound Identifiers

PubChem CID

134814505