| Identification | Back Directory | [Name]
SirReal2 | [CAS]
709002-46-0 | [Synonyms]
SirReal2
SirReal2 >=98% (HPLC)
2-[(4,6-Dimethyl-2-pyrimidinyl)thio]-N-[5-(1-naphthalenylmethyl)-2-thiazolyl]acetamide
Acetamide,2-[(4,6-dimethyl-2-pyrimidinyl)thio]-N-[5-(1-naphthalenylmethyl)-2-thiazolyl]-
2-(4,6-dimethylpyrimidin-2-yl)sulfanyl-N-[5-(naphthalen-1-ylmethyl)-1,3-thiazol-2-yl]acetamide | [Molecular Formula]
C22H20N4OS2 | [MDL Number]
MFCD04173051 | [MOL File]
709002-46-0.mol | [Molecular Weight]
420.55 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: 3 mg/ml; DMSO:PBS(pH 7.2) (1:2): 0.3 mg/ml | [form ]
A crystalline solid | [color ]
Off-white to light yellow |
| Hazard Information | Back Directory | [Description]
Sirtuins (SIRTs) represent a distinct class of trichostatin A-insensitive lysyl-deacetylases (class III HDACs). SIRT2 deacetylates histone H4 and α-tubulin and functions as a regulator of cell cycle progression, a determinant of myelination, a modulator of autophagy, and a suppressor of brain inflammation. SirReal2 is an aminothiazole that acts as a SIRT-rearranging ligand to selectively inhibit SIRT2 (IC50 = 140 nM). SirReal2 is >1,000-fold more potent at inhibiting the activity of SIRT2 than that of SIRT1 or SIRT3-6. This compound has been shown to be active in HeLa cells by significantly increasing α-tubulin acetylation. | [Uses]
SirReal2 is an aminothiazole that is a potent and selective Sirt2 inhibitor. | [in vivo]
SirReal2 (4 mg/kg, i.p., every 3 days for 28 days) combined with VS-5584 (4mg/kg, i.p., every 3 days for 28 days) leads to an extension of the survival time of mice and exhibits significant anti-tumor effects[3].
SirReal2 (50 mg/kg, i.p., every 3 days for 19 days) inhibits the expression of SIRT2, resumes NK cell tumor infltration and suppresses melanoma progression in WT mice[4].
| Animal Model: | mouse tumor xenograft model[3] | | Dosage: | 4 mg/kg | | Administration: | i.p., every 3 days for 28 days | | Result: | Restrained the growth of subcutaneous xenografts combined with VS-5584 in vivo. |
| [IC 50]
SIRT2: 140 nM (IC50) | [storage]
Store at -20°C |
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