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
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
N-Bromosuccinimide Price
- 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
- Product number
- 24199
- Product name
- Hesperadin
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $49
- Updated
- 2024/03/01
- Product number
- 24199
- Product name
- Hesperadin
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $202
- Updated
- 2024/03/01
- Product number
- 24199
- Product name
- Hesperadin
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $310
- Updated
- 2024/03/01
- Product number
- 24199
- Product name
- Hesperadin
- Purity
- ≥98%
- Packaging
- 25mg
- Price
- $711
- Updated
- 2024/03/01
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
Hesperadin Suppliers
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View Lastest Price from Hesperadin manufacturers
- Product
- Hesperadin 422513-13-1
- Price
- US $1.00/g
- Min. Order
- 1g
- Purity
- 99%
- Supply Ability
- 1ton
- Release date
- 2020-01-10