Name: Chaetocin
Brand: Selleck Chemicals
SKU: S8068
Availability: InStock
Rating: 5 (25 reviews)

Jump to

Quality Control

Batch: Purity: 99.82%

99.82

Related Targets	HDAC JAK BET PKC PARP HIF PRMT EZH2 AMPK Histone Acetyltransferase
Other Histone Methyltransferase Inhibitors	Pinometostat (EPZ5676) 3-Deazaneplanocin A (DZNep) Hydrochloride BIX-01294 trihydrochloride EPZ004777 EPZ015666 (GSK3235025) UNC1999 EPZ005687 SGC 0946 MM-102 UNC0638

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description	PMID
A549	Cytotoxicity assay			Cytotoxicity against human A549 cells, IC50 = 0.025 μM.	20303767
Hep3b	Function assay			Inhibition of HIF-1alpha-mediated VEGF expression in human Hep3b cells by luciferase reporter gene assay, IC50 = 0.04 μM.	22305612
Hep3b	Function assay			Inhibition of HIF-1alpha-mediated VEGF secretion in human Hep3b cells by ELISA, IC50 = 0.1 μM.	22305612
Jurkat	Cytotoxicity assay		40 hrs	Cytotoxicity against human Jurkat cells after 40 hrs bioluminescence assay, IC50 = 0.6 μM.	20303767
Drosophila melanogaster SL2	Function assay	0.1 uM	5 days	Inhibition of SU(VAR)3-9 in Drosophila melanogaster SL2 cells assessed as reduction of H3K9me2 at 0.1 uM after 5 days by MALDI-TOF MS seeded at 2.5 million cells/ml density	16408017
Drosophila melanogaster SL2	Function assay	0.5 uM	5 days	Inhibition of SU(VAR)3-9 in Drosophila melanogaster SL2 cells assessed as reduction of H3K9me2 at 0.5 uM after 5 days by MALDI-TOF MS seeded at 2.5 million cells/ml density	16408017
Drosophila melanogaster SL2	Function assay	0.5 uM		Inhibition of SU(VAR)3-9 in Drosophila melanogaster SL2 cells assessed as reduction of H3K9me3 at 0.5 uM by immunostaining method	16408017
HL60	Apoptosis assay	30 uM	4 hrs	Induction of apoptosis in human HL60 cells assessed as necrotic cell death at 30 uM after 4 hrs using DAPI/PI by confocal laser microscopy analysis	20675131
HL60	Apoptosis assay	0.3 uM	4 hrs	Induction of apoptosis in human HL60 cells assessed as nuclear fragmentation at 0.3 uM after 4 hrs using DAPI/PI by confocal laser microscopy analysis	20675131
HL60	Apoptosis assay	0.3 uM	2 hrs	Induction of apoptosis in human HL60 cells assessed as activation of caspase 3 at 0.3 uM after 2 hrs by Western blot analysis	20675131
MCF7	Function assay			Inhibition of histone-lysine N-methyltransferase in human MCF7 cells assessed as decrease in methylation of RARbeta DNA by qPCR method	ChEMBL
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 25 mg/mL (35.87 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (7.18mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	696.84	Formula	C₃₀H₂₈N₆O₆S₄	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	28097-03-2	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent

Mechanism of Action

Targets/IC₅₀/Ki	dSU(VAR)3-9 0.8 μM mouse G9a 2.5 μM Neurospora crassa DIM5 3 μM
In vitro	In SL-2 Drosophila tissue culture cells, Chaetocin causes the inhibition of SU(VAR)3-9 and the number of H3 molecules dimethylated at Lys9, and also inhibits cell growth. In HepG2, Hep3B, and Huh7 human hepatoma cells, this compound inhibits HIF-1-Mediated hypoxic responses. It also potently inhibits proliferation and colony formation in a broad range of cancer cell lines with IC50 of 2-10 nM.
Kinase Assay	Methylation assays
Kinase Assay	Unless otherwise stated, reactions are performed as followed: 1 g of purified enzyme (dSU(VAR)3-9 213; GST-hSUV39H1(82-412); GST-ncDIM5(19-318) and GSTmG9a(621-1000); dPRSET7(1-691); His-SET7/9(109-366) or enzyme complex expressed in a baculoviral expression system (dE(z), dSU(Z)12, dp55, dESC) were incubated for 30 minutes with 1 g of a peptide containing the first 19 amino acids of H3 plus an additional cystein residue (ARTKQTARKSTGGKAPRKQC) in a total volume of 40μl in BC25 (10mM HEPES pH7.6, 25mM NaCl, 1mM EDTA, 10%glycerol). All enzymes except for the E(z) complex had a similar specific activity between 5-10 nmole/min/mg. For the E(z) complex, the specific activity is approximately 5-10 fold lower, which is probably due to an incomplete formation of the full complex that is required for the highest activity. As a methyl donor S-Adenosyl [methyl-3H] methionine (SAM) is present in the reaction at a final concentration of 40 M with a specific activity of 0.3Ci/mmole. Reactions are stopped by adding 1/10 volume of 100% acetic acid and the incorporation of radioactivity is measured by spotting 30 l of the reaction on P81 filter paper and subsequent scintillation counting. For the inhibitor screening, 1 l of this compound with a concentration of 10 g/l is added to each reaction. In the cases where PRSET7 or the E(z) complex is used as enzyme either recombinant nucleosomes (1 g) or recombinant H3 (1 g) respectively replaced the H3 peptide as a substrate.
In vivo	In Hepa 1c1c-7 tumor-bearing mice, Chaetocin (0.25 mg/kg, i.p.) inhibits tumor growth by deregulating HIF-1[alpha]-mediated angiogenesis. In SKOV3 tumor-bearing nude mice, this compound treatment (0.25 mg/kg, i.p.) significantly delays the tumor growth with minimal evidence of toxicities.
References	[1] https://pubmed.ncbi.nlm.nih.gov/16408017/ [2] https://pubmed.ncbi.nlm.nih.gov/21140472/ [3] https://pubmed.ncbi.nlm.nih.gov/22187030/ [4] https://pubmed.ncbi.nlm.nih.gov/36070144/

Applications

Methods	Biomarkers	Images	PMID
Western blot	Procaspase-3 / Cleaved Caspase-3 / PARP		26890137
Growth inhibition assay	Cell viability		18176557

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

Chaetocin Histone Methyltransferase inhibitor

Chemical Structure

Molecular Weight: 696.84