InChI key
XCLPBILTRRWOIL-UHFFFAOYSA-N
SMILES string
FC(F)(F)c1ncc(nc1)N2C(c3c(c(ccc3)C(=O)NO)C2)(C)C
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
Quality Level
Biochem/physiol Actions
FT895 is a potent and highly selective HDAC11 inhibitor (IC50 = 3 nM/HDAC11, 5.6 μM/HDAC8, >10 μM/HDAC1-7, HDAC9 & HDAC10) with a deacetylase active site Zn2+-targeting hydroxamate. FT895 exhibits antiproliferation potency against myeloproliferative neoplasm (MPN) cultures (IC50 = 3.00 μM/JAK2(V617F) Ba/F3, 4.94 μM/HEL92.1.7, 6.49 μM/MPL(W515L) Ba/F3) and reduces stem-like properties of CSCs (42/62/85/100% inhibtion of H1650 Sphere formation at 0.5/1/2/5 μM).
Potent and highly selective HDAC11 inhibitor that reduces myeloproliferative neoplasm (MPN) proliferation and CSCs stem-like properties.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Se In Son et al.
ACS chemical biology, 14(7), 1393-1397 (2019-07-03)
Mammalian histone deacetylases (HDACs) are a class of enzymes that play important roles in biological pathways. Existing HDAC inhibitors target multiple HDACs without much selectivity. Inhibitors that target one particular HDAC will be useful for investigating the biological functions of
Matthew W Martin et al.
Bioorganic & medicinal chemistry letters, 28(12), 2143-2147 (2018-05-20)
N-Hydroxy-2-arylisoindoline-4-carboxamides are potent and selective inhibitors of HDAC11. The discovery, synthesis, and structure activity relationships of this novel series of inhibitors are reported. An advanced analog (FT895) displays promising cellular activity and pharmacokinetic properties that make it a useful tool
Lanzhu Yue et al.
Blood, 135(3), 191-207 (2019-11-22)
Protein acetylation is an important contributor to cancer initiation. Histone deacetylase 6 (HDAC6) controls JAK2 translation and protein stability and has been implicated in JAK2-driven diseases best exemplified by myeloproliferative neoplasms (MPNs). By using novel classes of highly selective HDAC
Namrata Bora-Singhal et al.
Scientific reports, 10(1), 4722-4722 (2020-03-15)
Non-small cell lung cancer (NSCLC) is known to have poor patient outcomes due to development of resistance to chemotherapy agents and the EGFR inhibitors, which results in recurrence of highly aggressive lung tumors. Even with recent success in immunotherapy using
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