Hesperadin, CAS 422513-13-1

Hesperadin, CAS 422513-13-1, Stock 841g, Assay 98.74%, White powder, Water 0.24%, Single Impurity 0.32%.

Hesperadin

Hesperadin is an inhibitor of human Aurora B, which can prevent the phosphorylation of substrate with IC(50) of 40 nM. Growth of cultured bloodstream forms was also sensitive to Hesperadin (IC(50) of 50 nM). Hesperadin blocked nuclear division and cytokinesis but not other aspects of the cell cycle. Consequently, growth arrested cells accumulated multiple kinetoplasts, flagella and nucleoli, similar to the effects of RNAi-dependent knockdown of TbAUK1 in cultured bloodstream forms cells. Molecular models predicted high-affinity binding of Hesperadin to both conserved and novel sites in TbAUK1. Collectively, these data demonstrate that cell cycle progression is essential for infections with T. brucei and that parasite Aurora kinases can be targeted with small-molecule inhibitors. 

Product Details:

Name: Hesperadin

CAS#: 422513-13-1 (free base)

Chemical Formula: C29H32N4O3S

Exact Mass: 516.21951

Molecular Weight: 516.65

Elemental Analysis: C, 67.42; H, 6.24; N, 10.84; O, 9.29; S, 6.21

Specification:

Related CAS #: 422513-13-1 (free base); unknown (HCl)    

Synonym: Hesperadin; Hesperadine.

IUPAC/Chemical Name: (Z)-N-(2-oxo-3-(phenyl((4-(piperidin-1-ylmethyl)phenyl)amino)methylene)indolin-5-yl)ethanesulfonamide

InChi Key: GLDSKRNGVVYJAB-DQSJHHFOSA-N

InChi Code: InChI=1S/C29H32N4O3S/c1-2-37(35,36)32-24-15-16-26-25(19-24)27(29(34)31-26)28(22-9-5-3-6-10-22)30-23-13-11-21(12-14-23)20-33-17-7-4-8-18-33/h3,5-6,9-16,19,30,32H,2,4,7-8,17-18,20H2,1H3,(H,31,34)/b28-27-

SMILES Code: CCS(=O)(NC1=CC2=C(NC(/C2=C(C3=CC=CC=C3)\NC4=CC=C(CN5CCCCC5)C=C4)=O)C=C1)=O

Appearance: white 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

Certification: