Thiomyristoyl

Catalog No.S8245 Batch:S824501

Technical Data

Formula	C₃₄H₅₁N₃O₃S
Molecular Weight	581.85	CAS No.	1429749-41-6
Solubility (25°C)*	In vitro	DMSO	100 mg/mL (171.86 mM)
		Ethanol	100 mg/mL (171.86 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

Thiomyristoyl (TM) is a potent and specific SIRT2 inhibitor with an IC50 of 28 nM. It inhibits SIRT1 with an IC50 value of 98 μM and does not inhibit SIRT3 even at 200 μM.

Targets

SIRT2 ^[1]
(Cell-free assay)

28 nM

In vitro

Thiomyristoyl(TM) is a highly selective SIRT2 inhibitor. It cannot efficiently inhibit SIRT3, SIRT5, SIRT6, or SIRT7. In vitro, it shows great inhibition of cell viability and its cytotoxicity is relatively selective toward cancer cells. TM decreases c-Myc oncoprotein level in cancer cells, the ability of TM to decrease c-Myc abundance in different cell lines correlates with the sensitivity of the cell lines to TM^[1].

In vivo

The anticancer effect of TM correlates with its ability to decrease c-Myc level. TM has limited effects on non-cancerous cells and tumor-free mice^[1].

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines breast cancer cell lines MCF-7 Concentrations 1, 5, 10, 25, 50 μM Incubation Time 6 h Method Human MCF-7 cells are grown in DMEM media contained 10% (vol/vol) heat-inactivated fetal bovine serum and 1% penicillin-streptomycin and treated with in the presence of 200 nM TSA for 6 hr. The acetylation level of p53 protein is determined by western blot using anti-acetyl-p53 (K382) antibody. β-actin serves as a loading control.
Animal Study:^{^[1]}	Animal Models Mouse xenograft model Dosages 1.5 mg/50 μL (IP); 0.75 mg/50 μL (IT) Administration intraperitoneal (IP) or intra-tumor (IT) injections

Cell Assay:^{^[1]}

Cell lines
breast cancer cell lines MCF-7
Concentrations
1, 5, 10, 25, 50 μM
Incubation Time
6 h
Method
Human MCF-7 cells are grown in DMEM media contained 10% (vol/vol) heat-inactivated fetal bovine serum and 1% penicillin-streptomycin and treated with in the presence of 200 nM TSA for 6 hr. The acetylation level of p53 protein is determined by western blot using anti-acetyl-p53 (K382) antibody. β-actin serves as a loading control.

Animal Study:^{^[1]}

Animal Models
Mouse xenograft model
Dosages
1.5 mg/50 μL (IP); 0.75 mg/50 μL (IT)
Administration
intraperitoneal (IP) or intra-tumor (IT) injections

References

[1] Jing H, et al. Cancer Cell. 2016, 29(3):297-310.

Selleck's Thiomyristoyl has been cited by 6 publications

VRK1 Kinase Activity Modulating Histone H4K16 Acetylation Inhibited by SIRT2 and VRK-IN-1 [ Int J Mol Sci, 2023, 24(5)4912]	PubMed: 36902348
Effects of Dimerization on the Deacylase Activities of Human SIRT2 [ Biochemistry, 2023, 10.1021/acs.biochem.3c00381]	PubMed: 37966275
Deacetylation of ATG4B promotes autophagy initiation under starvation [ Sci Adv, 2022, 8(31):eabo0412]	PubMed: 35921421
Sirt2 Inhibition Enhances Metabolic Fitness and Effector Functions of Tumor-Reactive T Cells [ Cell Metab, 2020, 32(3):420-436.e12]	PubMed: 32768387
SIRT1 inhibitors mitigate radiation-induced GI syndrome by enhancing intestinal-stem-cell survival [ Cancer Lett, 2020, 501:20-30]	PubMed: 33359449
A novel role of SIRT2 in regulating gap junction communications via connexin-43 in bovine cumulus-oocyte complexes. [ J Cell Physiol, 2020, 10.1002]	PubMed: 32039484

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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