SirReal2
SirReal2 Basic information
- Product Name:
- SirReal2
- Synonyms:
-
- SirReal2
- Acetamide,2-[(4,6-dimethyl-2-pyrimidinyl)thio]-N-[5-(1-naphthalenylmethyl)-2-thiazolyl]-
- 2-[(4,6-Dimethyl-2-pyrimidinyl)thio]-N-[5-(1-naphthalenylmethyl)-2-thiazolyl]acetamide
- 2-(4,6-dimethylpyrimidin-2-yl)sulfanyl-N-[5-(naphthalen-1-ylmethyl)-1,3-thiazol-2-yl]acetamide
- SirReal2 >=98% (HPLC)
- Sirtuin,Inhibitor,inhibit,SirReal2,SirReal 2,SirReal-2
- 2-((4,6-Dimethylpyrimidin-2-yl)thio)-N-(5-(naphthalen-1-ylmethyl)thiazol-2-yl)acetamide
- SirReal2, 10 mM in DMSO
- CAS:
- 709002-46-0
- MF:
- C22H20N4OS2
- MW:
- 420.55
- Mol File:
- 709002-46-0.mol
SirReal2 Chemical Properties
- 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
SirReal2 Usage And Synthesis
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
References
[1] TOBIAS RUMPF. Selective Sirt2 inhibition by ligand-induced rearrangement of the active site.[J]. Nature Communications, 2015: 6263. DOI: 10.1038/ncomms7263
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