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Hesperadin

Product Name
Hesperadin
CAS No.
422513-13-1
Chemical Name
Hesperadin
Synonyms
CS-408;Hesperadin;Hesperadine;Hesperadin, >=98%;Hesperadin USP/EP/BP;Hesperadin hydrochloride;Hesperadin (This product is unavailable in the U.S.);Hesperadin Hesperadine;(Z)-N-(2-Oxo-3-(phenyl((4-(piperidin-1-ylmethyl)phenyl)amino)methylene)indolin-5-yl)ethanesulf;(Z)-N-(2-oxo-3-(phenyl(4-(piperidin-1-ylmethyl)phenylamino)methylene)indolin-5-yl)ethanesulfonamide
CBNumber
CB12537545
Molecular Formula
C29H32N4O3S
Formula Weight
516.65
MOL File
422513-13-1.mol
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Hesperadin Property

Melting point:
228 °C
Density 
1.326
storage temp. 
Refrigerator
solubility 
DMSO, Methanol
form 
Solid
pka
9.14±0.20(Predicted)
color 
Yellow
CAS DataBase Reference
422513-13-1
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
375680
Product name
Hesperadin - CAS 422513-13-1 - Calbiochem
Purity
Hesperadin primarily used in Inhibition.
Packaging
5mg
Price
$280
Updated
2024/03/01
Cayman Chemical
Product number
24199
Product name
Hesperadin
Purity
≥98%
Packaging
1mg
Price
$49
Updated
2024/03/01
Cayman Chemical
Product number
24199
Product name
Hesperadin
Purity
≥98%
Packaging
5mg
Price
$202
Updated
2024/03/01
Cayman Chemical
Product number
24199
Product name
Hesperadin
Purity
≥98%
Packaging
10mg
Price
$310
Updated
2024/03/01
Cayman Chemical
Product number
24199
Product name
Hesperadin
Purity
≥98%
Packaging
25mg
Price
$711
Updated
2024/03/01
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Hesperadin Chemical Properties,Usage,Production

Description

Hesperadin is a multi-kinase inhibitor. It inhibits human Aurora kinase B (IC50 = 250 nM) and its T. brucei homolog Aurora kinase-1 (IC50 = 40 nM) in in vitro kinase assays. Hesperadin (1 μM) inhibits AMPK, LCK, MKK1, MAPKAP-K1, CHK1, and PHK in a panel of 25 kinases. It also inhibits MEKK2 in ATPase and transphosphorylation assays with IC50s of 60 and 34 nM, respectively. Hesperadin (50-100 nM) induces polyploidy and defects in cytokinesis and spindle assembly as well as inhibits proliferation of HeLa cells and overrides mitotic arrest induced by paclitaxel or monastrol . Hesperadin also induces toxicity in HepG2 cells with a toxic concentration (TC50) value of less than 0.2 μM. It inhibits replication of clinical isolates of influenza A and B viruses with EC50s ranging from 0.22 to 2.21 μM in a plaque formation assay. Hesperadin inhibits the growth of T. brucei, L. major promastigotes and amastigotes, and P. falciparum with EC50 values ranging from 0.01 to 2.37 μM, but has less activity against T. cruzi (EC50 = 39 μM).

Uses

Hesperadin phosphorylates human mitotic protein complexes that control physiological changes within the cell to allow for proper and successful chromosome segregation. It also targets aurora kinases in cancer treatment, affecting the chromosomes’ regulation during mitosis.

Definition

ChEBI: An oxindole that is indolin-2-one which is substituted at position 5 by an (ethylsulfonyl)nitrilo group and at position 2 by a methylidene group, which is itself substituted by a phenyl group and a [4-(piperidin-1-ylmethyl)phenyl]amino group. An Aurora B k nase inhibitor, it is used to inhibit chromosome alignment and segregation.

References

[1]jetton n1, rothberg kg, hubbard jg, wise j, li y, ball hl, ruben l. the cell cycle as a therapeutic target against trypanosoma brucei: hesperadin inhibits aurora kinase-1 and blocks mitotic progression in bloodstream forms. mol microbiol. 2009 apr;72(2):442-58. doi: 10.1111/j.1365-2958.2009.06657.x. epub 2009 mar 6.
[2]hauf s1, cole rw, laterra s, zimmer c, schnapp g, walter r, heckel a, van meel j, rieder cl, peters jm. the small molecule hesperadin reveals a role for aurora b in correcting kinetochore-microtubule attachment and in maintaining the spindle assembly checkpoint. j cell biol. 2003 apr 28;161(2):281-94. epub 2003 apr 21.

Hesperadin Preparation Products And Raw materials

Raw materials

Preparation Products

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Hesperadin Suppliers

Canada 1 China 85 Europe 1 India 3 Japan 1 The Netherlands 1 United Kingdom 3 United States 15 Global 110
Novachemistry
Tel
44-20819178-90 02081917890
Fax
(0)2080432064
Email
info@novachemistry.com
Country
United Kingdom
ProdList
4381
Advantage
58
Tocris Bioscience
Tel
--
Fax
--
Email
customerservice@tocris.co.uk
Country
United Kingdom
ProdList
5726
Advantage
77
Sequoia Research Products Ltd.
Tel
--
Fax
--
Email
sales@seqchem.com
Country
United Kingdom
ProdList
3113
Advantage
69
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View Lastest Price from Hesperadin manufacturers

Career Henan Chemical Co
Product
Hesperadin 422513-13-1
Price
US $1.00/g
Min. Order
1g
Purity
99%
Supply Ability
1ton
Release date
2020-01-10

422513-13-1, HesperadinRelated Search:

ZM 447439 MK-5108 (VX-689) Aurora A Inhibitor I MG-132 MLN8054 Barasertib (AZD1152-HQPA)

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  • (Z)-N-(2-Oxo-3-(phenyl((4-(piperidin-1-ylmethyl)phenyl)amino)methylene)indolin-5-yl)ethanesulf
  • N-[(3Z)-2-Oxo-3-(phenyl{[4-(1-piperidinylmethyl)phenyl]amino}methylen)-2,3-dihydro-1H-indol-5-yl]ethansulfonamid
  • Hesperadin (This product is unavailable in the U.S.)
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  • 422513-13-1
  • Inhibitor
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