SPS8I1 | CAS#383907-43-5 | SETD8 inhibitor

MedKoo Cat#: 562811 | Name: SPS8I1

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Description:

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

SPS8I1, also known as DA3003-1, is an inhibitor of SETD8 with cellular activity. It also acts as a Cdc25 phosphatase inhibitor.

Chemical Structure

SPS8I1

CAS#383907-43-5

Theoretical Analysis

MedKoo Cat#: 562811

Name: SPS8I1

CAS#: 383907-43-5

Chemical Formula: C15H16ClN3O3

Exact Mass: 321.0880

Molecular Weight: 321.76

Elemental Analysis: C, 55.99; H, 5.01; Cl, 11.02; N, 13.06; O, 14.92

Price and Availability

Size	Price	Availability
5mg	USD 280.00	2 weeks
10mg	USD 500.00	2 weeks
25mg	USD 775.00	2 weeks

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Related CAS #

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Synonym

SPS8I1; SPS-8I1; SPS 8I1; DA3003-1; DA3003 1; DA30031; NSC-663284; NSC 663284; NSC663284;

IUPAC/Chemical Name

6-Chloro-7-(2-morpholin-4-yl-ethylamino)quinoline-5,8-dione

InChi Key

BMKPVDQDJQWBPD-UHFFFAOYSA-N

InChi Code

InChI=1S/C15H16ClN3O3/c16-11-13(18-4-5-19-6-8-22-9-7-19)15(21)12-10(14(11)20)2-1-3-17-12/h1-3,18H,4-9H2

SMILES Code

O=C(C(Cl)=C1NCCN2CCOCC2)C3=C(N=CC=C3)C1=O

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 and ethanol

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

View handling instruction

Biological target:

SPS8I1 is a potent, selective inhibitor of Cdc25 dual specificity phosphatases (Ki values are 29, 95 and 89 nM for human Cdc25A, Cdc25B2 and Cdc25C respectively); > 20- and > 450-fold selective over VHR and PTP1B phosphatases respectively. SPS8I1 blocks proliferation of a range of human tumor cell lines (IC50 = 0.2 - 35 μM).

In vitro activity:

SPS8I1 inhibited Cdc25 phosphatases in vitro in an irreversible, time-dependent manner and arrested cells in the G1 and G2/M phases of the cell cycle. SPS8I1 directly inhibited Cdc25B activity in cells. SPS8I1 rapidly generated intracellular reactive oxygen species. After in vitro treatment with SPS8I1, there was sulfonic acid formation on the catalytic cysteine of Cdc25B Reference: Mol Pharmacol. 2005 Dec;68(6):1810-20. https://pubmed.ncbi.nlm.nih.gov/16155209/

In vivo activity:

To be determined

	Solvent	mg/mL	mM
Solubility
	DMSO	16.1	50.00
	Ethanol	16.1	50.00

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 321.76 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. Brisson M, Nguyen T, Wipf P, Joo B, Day BW, Skoko JS, Schreiber EM, Foster C, Bansal P, Lazo JS. Redox regulation of Cdc25B by cell-active quinolinediones. Mol Pharmacol. 2005 Dec;68(6):1810-20. doi: 10.1124/mol.105.016360. Epub 2005 Sep 9. PMID: 16155209. 2. Lazo JS, Aslan DC, Southwick EC, Cooley KA, Ducruet AP, Joo B, Vogt A, Wipf P. Discovery and biological evaluation of a new family of potent inhibitors of the dual specificity protein phosphatase Cdc25. J Med Chem. 2001 Nov 22;44(24):4042-9. doi: 10.1021/jm0102046. PMID: 11708908.

In vitro protocol:

In vivo protocol: