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| | 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 | | EINECS: | | | Product Categories: | | | 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 | | InChI | 1S/C22H20N4OS2/c1-14-10-15(2)25-22(24-14)28-13-20(27)26-21-23-12-18(29-21)11-17-8-5-7-16-6-3-4-9-19(16)17/h3-10,12H,11,13H2,1-2H3,(H,23,26,27) | | InChIKey | MENNDDDTIIZDDN-UHFFFAOYSA-N | | SMILES | CC1=NC(SCC(NC2=NC=C(S2)CC3=CC=CC4=C3C=CC=C4)=O)=NC(C)=C1 |
| WGK Germany | WGK 3 | | Storage Class | 11 - Combustible Solids |
| | 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 |
| | SirReal2 Preparation Products And Raw materials |
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