Splitomicin | CAS#5690-03-9 | HDAC inhibitor

Splitomicin
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 406571

CAS#: 5690-03-9

Description: Splitomicin is a cell-permeable lactone derived from naphthol and known to be a potent selective inhibitor of Sir2 (silent information regulator 2) and HDAC. Splitomicin inhibits the NAD+-dependent deacetylase activity of Sir2 in vitro. It increases the levels of cyclic AMP by inhibiting the activity of cyclic AMP phosphodiesterase, interferes with mobilization of intracellular Ca+2 and ATP release.

Chemical Structure

Splitomicin

CAS# 5690-03-9

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 406571
Name: Splitomicin
CAS#: 5690-03-9
Chemical Formula: C13H10O2
Exact Mass: 198.07
Molecular Weight: 198.220
Elemental Analysis: C, 78.77; H, 5.09; O, 16.14

Price and Availability

Size	Price	Availability
1mg	USD 200	2 Weeks
5mg	USD 415	2 Weeks
10mg	USD 575	2 Weeks
25mg	USD 900	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: Splitomicin

IUPAC/Chemical Name: 1H-benzo[f]chromen-3(2H)-one

InChi Key: ISFPDBUKMJDAJH-UHFFFAOYSA-N

InChi Code: InChI=1S/C13H10O2/c14-13-8-6-11-10-4-2-1-3-9(10)5-7-12(11)15-13/h1-5,7H,6,8H2

SMILES Code: O=C1CCC2=C3C=CC=CC3=CC=C2O1

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Product Data:

Product Data

Instruction:

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Biological target:	Splitomicin is a Sir2p histone deacetylase activity inhibitor, displaying higher activity in vivo (minimal inhibitory concentration = 0.49 µM) than in vitro (IC50 = 60 µM). Splitomicin has diverse effects on mammalian cells.
In vitro activity:	Targeting SIRT1 activity, with compounds such as splitomicin, during embryonic stem (ES) cell differentiation could be a promising strategy to improve the efficiency of hematopoietic lineage differentiation. The inhibitors nicotinamide and splitomicin enhanced the production of hematopoietic progenitors and mildly upregulated erythroid and myeloid-specific gene expression. Notably, splitomicin treatment led to an increase in the percentage of erythroid and myeloid lineage cells. Reference: Int J Stem Cells. 2019 Mar 30;12(1):21-30. https://pubmed.ncbi.nlm.nih.gov/30836727/
In vivo activity:	To be determined

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMF	15.0	75.67
	DMSO	20.0	100.90
	Ethanol	15.0	75.67

Preparing Stock Solutions

The following data is based on the product molecular weight 198.22 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:	1. Park JA, Park S, Park WY, Han MK, Lee Y. Splitomicin, a SIRT1 Inhibitor, Enhances Hematopoietic Differentiation of Mouse Embryonic Stem Cells. Int J Stem Cells. 2019 Mar 30;12(1):21-30. doi: 10.15283/ijsc18040. PMID: 30836727; PMCID: PMC6457709. 2. Liu FC, Day YJ, Liou JT, Yu HP, Liao HR. Splitomicin inhibits fMLP-induced superoxide anion production in human neutrophils by activate cAMP/PKA signaling inhibition of ERK pathway. Eur J Pharmacol. 2012 Aug 5;688(1-3):68-75. doi: 10.1016/j.ejphar.2012.05.006. Epub 2012 May 23. PMID: 22634165.
In vitro protocol:	1. Park JA, Park S, Park WY, Han MK, Lee Y. Splitomicin, a SIRT1 Inhibitor, Enhances Hematopoietic Differentiation of Mouse Embryonic Stem Cells. Int J Stem Cells. 2019 Mar 30;12(1):21-30. doi: 10.15283/ijsc18040. PMID: 30836727; PMCID: PMC6457709. 2. Liu FC, Day YJ, Liou JT, Yu HP, Liao HR. Splitomicin inhibits fMLP-induced superoxide anion production in human neutrophils by activate cAMP/PKA signaling inhibition of ERK pathway. Eur J Pharmacol. 2012 Aug 5;688(1-3):68-75. doi: 10.1016/j.ejphar.2012.05.006. Epub 2012 May 23. PMID: 22634165.
In vivo protocol:	To be determined

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1: Liu FC, Day YJ, Liou JT, Yu HP, Liao HR. Splitomicin inhibits fMLP-induced superoxide anion production in human neutrophils by activate cAMP/PKA signaling inhibition of ERK pathway. Eur J Pharmacol. 2012 Aug 5;688(1-3):68-75. doi: 10.1016/j.ejphar.2012.05.006. Epub 2012 May 23. PubMed PMID: 22634165.

2: Freitag M, Schemies J, Larsen T, El Gaghlab K, Schulz F, Rumpf T, Jung M, Link A. Synthesis and biological activity of splitomicin analogs targeted at human NAD(+)-dependent histone deacetylases (sirtuins). Bioorg Med Chem. 2011 Jun 15;19(12):3669-77. doi: 10.1016/j.bmc.2011.01.026. Epub 2011 Jan 22. PubMed PMID: 21315612.

3: Liu FC, Liao CH, Chang YW, Liou JT, Day YJ. Splitomicin suppresses human platelet aggregation via inhibition of cyclic AMP phosphodiesterase and intracellular Ca++ release. Thromb Res. 2009 Jun;124(2):199-207. doi: 10.1016/j.thromres.2009.02.013. Epub 2009 Mar 26. PubMed PMID: 19327818.

4: Neugebauer RC, Uchiechowska U, Meier R, Hruby H, Valkov V, Verdin E, Sippl W, Jung M. Structure-activity studies on splitomicin derivatives as sirtuin inhibitors and computational prediction of binding mode. J Med Chem. 2008 Mar 13;51(5):1203-13. doi: 10.1021/jm700972e. Epub 2008 Feb 13. PubMed PMID: 18269226.

5: Posakony J, Hirao M, Stevens S, Simon JA, Bedalov A. Inhibitors of Sir2: evaluation of splitomicin analogues. J Med Chem. 2004 May 6;47(10):2635-44. PubMed PMID: 15115404.

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