An inhibitor of G9a histone methyltransferase
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Isomer(s)
42901TM2-115
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BIX01294 (hydrochloride hydrate)

Item No. 13124

Technical Information
Formal Name
2-(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-6,7-dimethoxy-N-[1-(phenylmethyl)-4-piperidinyl]-4-quinazolinamine, trihydrochloride, hydrate
CAS Number
1808255-64-2
Molecular Formula
C28H38N6O2 • 3HCl [XH2O]
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
DMSO: 5 mg/mlWater: 10 mg/ml
λmax
212, 247, 333, 346 nm
SMILES
COC(C(OC)=C1)=CC2=C1C(NC3CCN(CC4=CC=CC=C4)CC3)=NC(N5CCCN(C)CC5)=N2.Cl.Cl.Cl.O
InChi Code
InChI=1S/C28H38N6O2.3ClH.H2O/c1-32-12-7-13-34(17-16-32)28-30-24-19-26(36-3)25(35-2)18-23(24)27(31-28)29-22-10-14-33(15-11-22)20-21-8-5-4-6-9-21;;;;/h4-6,8-9,18-19,22H,7,10-17,20H2,1-3H3,(H,29,30,31);3*1H;1H2
InChi Key
BZOWJAYUMMHCDW-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    BIX01294 (hydrochloride hydrate) is a selective inhibitor of G9a HMTase (IC50 = 1.7 μM).1 It less effectively inhibits the HMTase G9a-like protein (GLP; IC50 = 38 μM) and has no effect on other known HMTases.1 BIX01294 has been used in combination with the calcium channel activator BayK8644 to facilitate the generation of induced pluripotent stem cells from somatic cells in vitro.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Kubicek, S., O'Sullivan, R.J., August, E.M., et alReversal of H3K9me2 by a small-molecule inhibitor for the G9a histone methyltransferase. Mol. Cell 25, 473-481 (2007).

    2. Shi, Y., Desponts, C., Do, J.T., et alInduction of pluripotent stem cells from mouse embryonic fibroblasts by Oct4 and Klf4 with small-molecule compounds. Cell Stem Cell 3(5), 568-574 (2008).