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Chaetocin

Catalog No.GC14936

Inhibitor of lys9-specific HMTs

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Chaetocin Chemical Structure

Cas No.: 28097-03-2

Size Price Stock Qty
1mg
$135.00
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5mg
$405.00
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10mM (in 1mL DMSO)
$621.00
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10mg
$729.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Cell experiment [1]:

Cell lines

SKOV-3, OVCAR-3, KGN and A2780 ovarian cancer (OC) cell line

Preparation Method

The OC cells were seeded in 96-well microplates (1×104 cells/well) and incubated at 37°C overnight. Following incubation with chaetocin (0.05, 0.1, 0.25, 0.5, 0.75, 1 and 2 µM) at 37°C for 24 h,

Reaction Conditions

0.05, 0.1, 0.25, 0.5, 0.75, 1 and 2 µM for 24 hours

Applications

Chaetocin significantly inhibited the viability of SKOV-3, OVCAR-3, KGN and A2780 cells in a dose-dependent manner, with half-maximal inhibitory concentrations of 0.30, 60.66, 81.86 and 100.60 nM, respectively.

Animal experiment [2]:

Animal models

Female BALB/C nude mice

Preparation Method

Paired mice with equal tumor volume were divided into the chaetocin-treated group and the vehicle-treated group (n = 6 for each group), and then injected intraperitoneally (i.p.) daily with chaetocin (0.5 mg/kg) and the vehicle (DMSO), respectively. After 10 days of drug treatment, mice were sacrificed and the tumor were weighed.

Dosage form

Intraperitoneal injection, 0.5 mg/kg/day for 10 days

Applications

Significantly lower average tumor weight for chaetocin treatment group compared to control group

References:

[1]: Li Z, Huang L, Wei L, et al. Chaetocin induces caspase?dependent apoptosis in ovarian cancer cells via the generation of reactive oxygen species[J]. Oncology Letters, 2019, 18(2): 1915-1921.
[2]: Liao X, Fan Y, Hou J, et al. Identification of chaetocin as a potent non-ROS-mediated anticancer drug candidate for gastric cancer[J]. Journal of Cancer, 2019, 10(16): 3678.

Background

Chaetocin was reported to be a nonspecific inhibitor of histone methyl transferase (HMT) such as SUV39H1, thereby affecting gene expression [1]. Chaetocin inhibited HMT SU(VAR)3-9 with an IC50 of 0.6 µM [2].

Chaetocin significantly reduces the proliferation, cloning potential, and migration ability of the glioblastoma cell line T98G [3]. Chaetocin abrogated the maintenance of stem cell characteristics and tumor growth of bladder cancer stem cells (BCSCs) by suppressing the KMT1A-GATA3-STAT3 circuit (inhibition ratio: 80.1%) [4]. Chaetocin inhibited ovarian cancer (OC) cell proliferation, induced G2/M phase cell cycle arrest, and induced apoptosis at the concentration of 2µM (24 hours) [5]. Chaetocin inhibited cell proliferation and reduced PI3K/AKT pathway and p-AKT in gastric cancer HGC-27 cell, at the concentration of 200µM (24 hours) [6].

Chaetocin inhibited tumor growth in HGC-27 cell injected Gastric cancer mice model, by 0.5 mg/kg/day every alternate day for 24 days [6]. Chaetocin inhibited tumor progression and reduced PCNA in U87MG cell injected glioma mice model, by 0.5 mg/kg/day every alternate day for 25 days [7].

References:
[1]. Cherblanc F L, Chapman K L, Brown R, et al. Chaetocin is a nonspecific inhibitor of histone lysine methyltransferases[J]. Nature chemical biology, 2013, 9(3): 136-137.
[2]. Greiner D, Bonaldi T, Eskeland R, et al. Identification of a specific inhibitor of the histone methyltransferase SU (VAR) 3-9[J]. Nature chemical biology, 2005, 1(3): 143-145.
[3]. Sepsa A, Levidou G, Gargalionis A, et al. Emerging role of linker histone variant H1x as a biomarker with prognostic value in astrocytic gliomas. A multivariate analysis including trimethylation of H3K9 and H4K20[J]. PLoS One, 2015, 10(1): e0115101.
[4]. Yang Z, Wang H, Zhang N, et al. Chaetocin Abrogates the Self-Renewal of Bladder Cancer Stem Cells via the Suppression of the KMT1A-GATA3-STAT3 Circuit[J]. Frontiers in cell and developmental biology, 2020, 8: 424.
[5]. Li Z, Huang L, Wei L, et al. Chaetocin induces caspase?dependent apoptosis in ovarian cancer cells via the generation of reactive oxygen species[J]. Oncology Letters, 2019, 18(2): 1915-1921.
[6]. Wen C, Wang H, Wu X, et al. ROS-mediated inactivation of the PI3K/AKT pathway is involved in the antigastric cancer effects of thioredoxin reductase-1 inhibitor chaetocin[J]. Cell death & disease, 2019, 10(11): 1-16.
[7]. Dixit D, Ghildiyal R, Anto N P, et al. Chaetocin-induced ROS-mediated apoptosis involves ATM-YAP1 axis and JNK-dependent inhibition of glucose metabolism[J]. Cell death & disease, 2014, 5(5): e1212-e1212.

Chemical Properties

Cas No. 28097-03-2 SDF
Chemical Name (3S,3'S,6R,6'R,14R,14'R,16S,16'S)-3,3'-bis(hydroxymethyl)-2,2'-dimethyl-2,2',3,3',6,6',7,7'-octahydro-1H,1'H-[14,14'-bi(3,11a-epidithiopyrazino[1',2':1,5]pyrrolo[2,3-b]indole)]-1,1',4,4'(15H,15'H)-tetraone
Canonical SMILES O=C1[C@](CO)(SS2)N(C)C([C@]32N1[C@]4([H])[C@](C(C=CC=C5)=C5N4)([C@@]6(C(C=CC=C7)=C7N8)[C@@]8([H])N(C([C@](CO)(SS9)N%10C)=O)[C@]9(C6)C%10=O)C3)=O
Formula C30H28N6O6S4 M.Wt 696.84
Solubility DMSO: 25 mg/ml Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 1.435 mL 7.1752 mL 14.3505 mL
5 mM 0.287 mL 1.435 mL 2.8701 mL
10 mM 0.1435 mL 0.7175 mL 1.435 mL
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