Chaetocin
Tocris Bioscience, part of Bio-Techne | Catalog # 4504
SUV39H1 inhibitor
Product Description
Chaetocin is a histone methyltransferase SUV39H1 inhibitor (IC50 values are 0.8, 2.5 and 3 μM for dSU(VAR)3-9, mouse G9a and Neurospora crassa DIM5, respectively). Induces apoptosis in myeloma cell lines in vitro; exhibits antiproliferative activity in a mouse myeloma model in vivo.Chaetocin potently inhibits cell proliferation and colony formation in a wide range of cancer cell lines (IC50 of 2-10 nM) and inhibits tumor growth by deregulating HIF-1α-mediated angiogenesis. Sensitizes glioblastoma multiforme cells to pro-apoptotic agents.
Chaetocin is also an inhibitor of the oxidative stress remediation enzyme thioredoxin reductase (TrxR), and so induces oxidative stress.
In addition, Chaetocin promotes osteogenic differentiation through modulating Wnt/Beta-catenin signaling in mesenchymal stem cells. Chaetocin treatment increased osteogenic ability and reduced adipogenic ability.
Product Specifications
Molecular Weight
696.84
Formula
C30H28N6O6S4
Storage
Store at -20°C
Purity
≥95% (HPLC)
Chemical Name
(3S,3'S,5aR,5aR,10bR,10'bR,11aS,11'aS)-2,2',3,3',5a,5'a,6,6'-octahydro-3,3'-bis(hydroxymethyl)-2,2'-dimethyl-[10b,10'b(11H,11'H)-bi3,11a-epidithio-11aH-pyrazinopyrrolo[2,3-b]indole]-1,1',4,4'-tetrone
CAS Number
28097-03-2
PubChem ID
161591
InChI Key
PZPPOCZWRGNKIR-UHFFFAOYSA-N
SMILES
[H][C@]12NC3=C(C=CC=C3)[C@]1(C[C@]13SS[C@](CO)(N(C)C1=O)C(=O)N23)[C@]12C[C@]34SS[C@](CO)(N(C)C3=O)C(=O)N4[C@@]1([H])NC1=C2C=CC=C1
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 6.97 | 10 |
Preparing Stock Solutions
for Chaetocin
The following data is based on the product molecular weight 696.84
Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 14.35 mL | 71.75 mL | 143.50 mL |
| 0.5 mM | 2.87 mL | 14.35 mL | 28.70 mL |
| 1 mM | 1.44 mL | 7.18 mL | 14.35 mL |
| 5 mM | 0.29 mL | 1.44 mL | 2.87 mL |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
- Liang Chaetocin Promotes Osteogenic Differentiation via Modulating Wnt/Beta-Catenin Signaling in Mesenchymal Stem Cells. Stem Cells Int. 2021 PMID: 33628276
- Nakajima Inhibition of the HDAC/Suv39/G9a pathway restores the expression of DNA damage-dependent major histocompatibility complex class I-related chain A and B in cancer cells. Oncol Rep. 2017 PMID: 28677817
- Ozyerli-Goknar The fungal metabolite chaetocin is a sensitizer for pro-apoptotic therapies in glioblastoma. Cell Death Dis 2019 PMID: 31772153
- Greiner Reply to "Chaetocin is a nonspecific inhibitor of histone lysine methyltransferases". Nat.Chem.Biol. 2013 PMID: 23416388
- Cherblanc Chaetocin is a nonspecific inhibitor of histone lysine methyltransferases. Nat.Chem.Biol. 2013 PMID: 23416387
- Greiner Identification of a specific inhibitor of the histone methyltransferase SU(VAR)3-9. Nat.Chem.Biol. 2005 PMID: 16408017
- Isham Chaetocin: a promising new antimyeloma agent with in vitro and in vivo activity mediated via imposition of oxidative stress. Blood 2007 PMID: 17090648
Product Specific Notices for Chaetocin
For research use only
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