Hesperadin hydrochloride
Based on 12 publication(s) in Google Scholar
Hesperadin hydrochloride is an ATP competitive indolinone inhibitor of Aurora A and B. Hesperadin hydrochloride inhibits Aurora B with an IC50 of 250 nM.
For research use only. We do not sell to patients.
- Formula: C29H33ClN4O3S
- Molecular Weight:553.12
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications Citing Use of MedChemExpress (MCE) Hesperadin hydrochloride
More- Nat Commun. 2025 Sep 29;16(1):8598. [Abstract]
- Adv Sci (Weinh). 2025 Mar;12(11):e2414518. [Abstract]
- Adv Sci (Weinh). 2022 Oct 30;e2205091. [Abstract]
- Cell Commun Signal. 2025 Oct 2;23(1):409. [Abstract]
- Sci Signal. 2025 Feb 18;18(874):eadg4626. [Abstract]
- Antioxid Redox Signal. 2025 Jan;42(1-3):115-132. [Abstract]
- Int J Mol Sci. 2025 Aug 20;26(16):8052. [Abstract]
- Sci Rep. 2021 Jan 27;11(1):2283. [Abstract]
- Brain Res Bull. 2021 Dec:177:31-38. [Abstract]
- Behav Neurol. 2020 Feb 3:2020:2476861. [Abstract]
- Exp Cell Res. 2021 Sep 1;406(1):112741. [Abstract]
- bioRxiv. 2024 May 31.
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WB
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Cell Proliferation/Viability Assay
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In Vivo Efficacy Study
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IHC
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Cell Proliferation/Viability Assay
All Aurora Kinase Isoforms
MoreAll Parasite Isoforms
More
Biological Activity
Description
IC50 & Target
[1]|
Aurora B 250 nM (IC50) |
In Vitro
Hesperadin (10-100 nM) inhibits the Aurora kinase-1 (TbAUK1)-mediated phosphoryation of trypanosome histone H3 (TbH3) in a dose dependent manner, with an IC50 of 40 nM[1].
Hesperadin (0.01-10 μM; 24 or 48 hours) inhibits growth of bloodstream forms (BF) and procyclic forms (PF) cultures[1].
Hesperadin (100-200 nM; 24-72 hours) alters cell morphology and inhibits cell cycle progression similar to the RNAi knockdown of TbAUK1[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:M110 cells
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Concentration:0.01, 0.1, 1, 10 μM
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Incubation Time:24 hours or 48 hours
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Result:Inhibiting growth of BF cultures with an IC50 of 50 nM, while the inhibition of PF growth required approximately 11-fold more Hesperadin, with an IC50 of 550 nM.
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Cell Line:M110 cells
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Concentration:100, 200 nM
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Incubation Time:24, 48, 72 hours
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Result:Had a strong effect on cell growth and mitotic progression at 100-200 nM.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:6-week-old female nude mice injected GBM cells[2]
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Dosage:20 mg/kg/d
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Administration:I.v. injection
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Result:Increased the survival of xenograft mice models.
Chemical Information
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Molecular Weight 553.12
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Formula C29H33ClN4O3S
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SMILES
O=C1NC2=CC=C(C=C2/C1=C(NC3=CC=C(C=C3)CN4CCCCC4)\C5=CC=CC=C5)NS(CC)(=O)=O.[H]Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (12)
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Journal Impact Factor
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Most Recent
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Nat Commun
Cytoplasmic TRIM24 promotes colorectal cancer cell proliferation by activating Wnt/β-catenin signaling. [Abstract]2025 Sep 29;16(1):8598. PMID: 41022821
Hesperadin hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Sep 29;16(1):8598. [Abstract]
Cytosolic (Cyto) and nuclear (Nuc) fractions derived from DLD1 and SW620 cells stimulated with 20 μM of Hesperadin for 8 h were immunoblotted for indicated proteins. PARP1 and Caspase-3 served as loading controls and nuclear/cytosolic markers, respectively. Shown are the representative results from three independent experiments. Hesperadin treatment accelerated TRIM24 translocation to the nucleus and attenuated β-catenin accumulation in the cytosol and its nuclear distribution.
Hesperadin hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Sep 29;16(1):8598. [Abstract]
DLD1, SW620, RKO, and SW1643 cells were grown in the absence or presence of Hesperadin at the indicated concentrations for 7 days, then fixed and stained for colony-formation assessment. The colony formation assays revealed that Hesperadin markedly suppressed the proliferation of DLD1 and SW620 cells.
Hesperadin hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Sep 29;16(1):8598. [Abstract]
Upper: A schematic diagram of the experimental timeline for the subcutaneous xenograft assay (n = 4 mice per group). Bottom: The tumor growth curve of the mice subcutaneously injected with DLD1 or SW1643 cells after intraperitoneal administration of Hesperadin (2.5 mg/kg; once every other day, for a total of 9 times) or PBS. Representative pictures of tumors dissected from mice at day 24 post-implantation. Scale bar, 1 cm. The results showed that Hesperadin administration showed no impact on tumor growth in mice inoculated with SW1643 cells, it significantly suppressed tumor growth in mice inoculated with DLD1 cells.
Hesperadin hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Sep 29;16(1):8598. [Abstract]
Left: Tumor tissues collected from mice subcutaneously injected with DLD1 or SW1643 cells after intraperitoneal administration of Hesperadin (2.5 mg/kg; once every other day, for a total of 9 times) or PBS were subjected to PCNA staining, with nuclei counterstained by hematoxylin. Scale bar, 50 µm. Right: PCNA staining intensity was quantified in randomly selected fields (n = 5, 6, 8, and 6 for the four histograms, respectively) using ImageJ with the H-DAB color deconvolution vector, and relative intensity was calculated after normalization to the PBS control group. Immunohistochemical staining of PCNA indicated that Hesperadin administration inhibited cell proliferation in tumors formed by DLD1 cells but not in those by SW1643 cells.
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Adv Sci (Weinh)
Ischemic Area-Targeting and Self-Monitoring Nanoprobes Ameliorate Myocardial Ischemia/Reperfusion Injury by Scavenging ROS and Counteracting Cardiac Inflammation. [Abstract]2025 Mar;12(11):e2414518. PMID: 39840521
Hesperadin hydrochloride purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Mar;12(11):e2414518. [Abstract]
Evaluation of the synergistic treatment efficacy of diselenide bonds and Hesperadin (0.07 µg/mL; 16 h).
Hesperadin hydrochloride purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Mar;12(11):e2414518. [Abstract]
Effects of different treatments on apoptosis of AC16 cells subjected to OGD/R. Hesperadin (0.07 µg/mL; 16 h).
Hesperadin hydrochloride purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Mar;12(11):e2414518. [Abstract]
Hesperadin (0.3556 mg/kg; i.v.; once daily) contributed to some improvement of cardiac function, including an increase in LVEF and LVFS as well as a decrease in LVDd, LVDs, and left ventricular end‐systolic volume (LVESV) in myocardial ischemia/reperfusion injury (MIRI) mice.
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Adv Sci (Weinh)
N6 -Methyladenosine-Modified CBX1 Regulates Nasopharyngeal Carcinoma Progression Through Heterochromatin Formation and STAT1 Activation. [Abstract]2022 Oct 30;e2205091. PMID: 36310139 -
Cell Commun Signal
2025 Oct 2;23(1):409. PMID: 41039590 -
Sci Signal
Sustained chromosomal passenger complex activity preserves the pluripotency of human embryonic carcinoma cells. [Abstract]2025 Feb 18;18(874):eadg4626. PMID: 40136047 -
Antioxid Redox Signal
CARD11-BCL10-MALT1 complex-dependent MALT1 activation facilitates myocardial oxidative stress in doxorubicin-treated mice via enhancing k48-linked ubiquitination of Nrf2. [Abstract]2025 Jan;42(1-3):115-132. PMID: 38814831 -
Int J Mol Sci
STK26 Promotes the Stabilization of ATF6 to Facilitate the Progression of Colorectal Cancer. [Abstract]2025 Aug 20;26(16):8052. PMID: 40869379 -
Sci Rep
Depletion of Survivin suppresses docetaxel-induced apoptosis in HeLa cells by facilitating mitotic slippage. [Abstract]2021 Jan 27;11(1):2283. PMID: 33504817 -
Brain Res Bull
MST4 attenuates NLRP3 inflammasome-mediated neuroinflammation and affects the prognosis after intracerebral hemorrhage in mice. [Abstract]2021 Dec:177:31-38. PMID: 34534636 -
Behav Neurol
MST4 Kinase Inhibitor Hesperadin Attenuates Autophagy and Behavioral Disorder via the MST4/AKT Pathway in Intracerebral Hemorrhage Mice. [Abstract]2020 Feb 3:2020:2476861. PMID: 32089749
Hesperadin hydrochloride purchased from MedChemExpress. Usage Cited in: Behav Neurol. 2020 Feb 3:2020:2476861. [Abstract]
Administration of Hesperadin influences endogenous expression of MST4, pAKT, AKT, and LC3 12 h following ICH. Representative western blot bands for MST4, pAKT, AKT, and LC3 expression in sham and ICH mice 12 h following ICH.
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Exp Cell Res
RNA-binding protein RNPC1 acts as an oncogene in gastric cancer by stabilizing aurora kinase B mRNA. [Abstract]2021 Sep 1;406(1):112741. PMID: 34302858 -
Purity & Documentation
References
[1]. Neal J, et, al. 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. [Content Brief]
[2]. Wahafu A, et, al. Targeting Aurora kinase B attenuates chemoresistance in glioblastoma via a synergistic manner with temozolomide. Pathol Res Pract. 2019 Nov; 215(11): 152617. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)