Histone Lysine Methyltransferase Inhibitor An HMTase inhibitor known as BIX-01294 Trihydrochloride

Histone Lysine Methyltransferase Inhibitor (CAS 935693-62-2 (hydrate))

Histone Lysine Methyltransferase Inhibitor | CAS 935693-62-2 (hydrate) is rated 5.0 out of 5 by 1.
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Synonym: BIX-01294
Application: An HMTase inhibitor known as BIX-01294 Trihydrochloride
CAS Number: 935693-62-2 (hydrate)
Purity: >97%
Molecular Weight: 600
Molecular Formula: C28H38N6O2 3HCl
* Refer to Certificate of Analysis for lot specific data (including water content).
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Histone Lysine Methyltransferase Inhibitor (BIX-01294) is a G9a (histone lysine methyltransferase (HMTase)) inhibitor, specifically shown to inhibit the G9a-mediated generation of H3K9me2 (histone H3 lysine 9 dimethylation), not competitive with the S-adenosyl-methionine cofactor. Levels of H3K9me2 are restored with removal of BIX-01294. This molecule allows transient modulation of HMTase behavior, providing a tool for studying consequent effects on gene expression and chromatin organization. Histone Lysine Methyltransferase Inhibitor is an inhibitor of EHMT.


References

1. Kubicek, Stefan., et al., 2007. Reversal of H3K9me2 by a small-molecule inhibitor for the G9a histone methyltransferase. Molecular cell. 25(3): 473-81. PMID: 17289593
2. Shi, Yan., et al., 2008. A combined chemical and genetic approach for the generation of induced pluripotent stem cells. Cell stem cell. 2(6): 525-8. PMID: 18522845
3. Huangfu, Danwei., et al., 2008. Induction of pluripotent stem cells by defined factors is greatly improved by small-molecule compounds. Nature biotechnology. 26(7): 795-7. PMID: 18568017

Physical State :
Solid
Solubility :
Soluble in water (100 mM), DMSO (5 mg/ml), and ethanol.
Storage :
Store at -20° C
Refractive Index :
n20D ~1.63 (Predicted)
IC50 :
G9a : IC50 = 0.11 µM (human); G9a-like protein: IC50 = 0.7 µM; EHMT: IC50 = 0.7 µM (human); G9a histone lysine methyltransferase: IC50 = 1.7 µM; GLP-catalyzed H3K9me3 : IC50 = 38 µM
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
25150857
MDL Number :
MFCD16618384
SMILES :
CN1CCCN(CC1)C2=NC3=CC(=C(C=C3C(=N2)NC4CCN(CC4)CC5=CC=CC=C5)OC)OC

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Certificate of Analysis

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Histone Lysine Methyltransferase Inhibitor  Product Citations

See how others have used Histone Lysine Methyltransferase Inhibitor. Click on the entry to view the PubMed entry .

Citations 1 to 1 of 1 total

PMID: # 27022024  Perez, RE. et al. 2016. J. Biol. Chem. 291: 10131-47.

Citations 1 to 1 of 1 total

How is this manufactured – synthetically or has an animal/human been used to obtain the chemical? We need to know to get the correct customs form for importation to Australia.

Asked by: AnitaP
Thank you for your question. Each lot of this chemical comes with a lot-specific Certificate Of Analysis. You may request a lot-specific Certificate Of Analysis on our website. Alternatively, please contact your local distributor or our Technical Service Department to inquire about the source information for the biochemical.
Answered by: Tech Service
Date published: 2019-02-11
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Rated 5 out of 5 by from Shi et al Shi et al. (PubMed ID 18522845) used Histone Lysine Methyltransferase Inhibitor (BIX-01294) to inhibit G9a histone methyltrasferase and found this to improve reprograming efficiency in neural progenitor cells transduced with Oct3/4-Klf4. -SCBT Publication Review
Date published: 2015-04-27
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