BIX-01294 trihydrochloride

Name: BIX-01294 trihydrochloride
Brand: MedChemExpress
SKU: HY-108239
Rating: 5.0 (25 reviews)

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BIX-01294 trihydrochloride is a reversible and highly selective G9a and GLP Histone Methyltransferase inhibitor, with IC₅₀s of of 1.7 μM and 0.9 μM, respectively. BIX-01294 trihydrochloride inhibits G9a/GLP by competing for binding with the amino acids N-terminal of the substrate lysine residue. BIX-01294 trihydrochloride, a (1H-1,4-diazepin-1-yl)-quinazolin-4-yl amine derivative, induces necroptosis and autophagy. BIX-01294 trihydrochloride has antitumor activity in recurrent tumor cells.

For research use only. We do not sell to patients.

BIX-01294 trihydrochloride Chemical Structure

CAS No. : 1392399-03-9

Size	Price	Stock	Quantity
5 mg	USD 96	Get quote 3 - 4 weeks 2 - 3 weeks 2 - 3 weeks	Estimated Time of Arrival: December 31
10 mg	USD 149	Get quote 3 - 4 weeks 2 - 3 weeks 2 - 3 weeks	Estimated Time of Arrival: December 31
25 mg	USD 290	Get quote 3 - 4 weeks 2 - 3 weeks 2 - 3 weeks	Estimated Time of Arrival: December 31
50 mg	USD 447	Get quote 3 - 4 weeks 2 - 3 weeks 2 - 3 weeks	Estimated Time of Arrival: December 31
100 mg	USD 670	Get quote 3 - 4 weeks 2 - 3 weeks 2 - 3 weeks	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Based on 25 publication(s) in Google Scholar

Other Forms of BIX-01294 trihydrochloride:

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BIX-01294 hydrochloride hydrate Get quote

23 Publications Citing Use of MCE BIX-01294 trihydrochloride

RT-PCR

: BIX-01294 trihydrochloride purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2018 Aug 17;37(1):196. [Abstract]; The relative mRNA levels of Ki67 and PCNA in primary CRC cells responding to rhIL-33 (100 ng/mL) incubation and/ or indicated inhibitors (SB203580, 10 μg/mL; PD98059, 20 μg/mL; SP600125, 10 μg/mL; BIX01294, 2 μM; 5Aza, 10 μM; SC560, 0.1 μg/mL; celecoxib, 20 μg/mL) for 24 h.

: BIX-01294 trihydrochloride purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2017 Apr 6;8(4):e2726. [Abstract]; Upper and middle panels: WB detection of H3K9me2 and G9A in PC9 and A549 cells treated with 0, 1, 2.5, 5 or 10 μM BIX-01294. The total level of histone H3 and actin serve as loading controls. Lower panel: WB detection of the total (T-) level of and phosphorylated (P-) ERK kinase in PC9 and A549 cells treated with 0, 1, 5 or 10 μM BIX-01294. GAPDH serves as the loading control

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•Related Small Molecules:

•Related Proteins:

View All Histone Methyltransferase Isoform Specific Products:

View All Isoforms

EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

IC50: 2.7 μM (G9a in DELFIA assay)^[2]
IC50: 1.9 μM for G9a and 0.7 μM for GLP^[5]

In Vitro

BIX-01294 (2 μM; 48 h) trihydrochloride selectively inhibits recurrent tumor cell growth^[1].
BIX-01294 (1 μM) trihydrochloride leads to a marked increase in phosphorylation of S345 of MLKL^[1].
BIX-01294 (1 μM) trihydrochloride significantly upregulates the canonical p53 targets Cdkn1a (p21) and Gadd45a in recurrent tumor cell lines^[1].
BIX-01294 (1 μM; 6 days) trihydrochloride causes the reduction in H3K9me2 levels in primary and recurrent tumor cells^[1].
BIX-01294 trihydrochloride leads to necroptotic cell death in recurrent tumor cells. Necrostatin-1 (30 μM) partially reverses cell death induced by BIX-01294 (750 nM; 24 h) trihydrochloride^[1].
BIX-01294 (4.1 μM; for 2 days) trihydrochloride causes around a 20% reduction, concomitant with a comparable increase in the unmodified H3K9 fragment in H3K9me2 in mouse ES cells. BIX-01294 trihydrochloride causes pronounced reduction in H3K9me2 and a small decrease for H3K9me3 and H3K9me1 in wild-type ES cells^[2].
BIX-01294 trihydrochloride has no inhibition of the other histone methyltransferases even at concentrations of 45 μM. BIX-01294 trihydrochloride does not affect SUV39H1 (H320R) and PRMT1 within the tested concentration range (up to 10 μM)^[2].
BIX-01294 trihydrochloride inhibits G9a in an uncompetitive manner with S-adenosyl-methionine (SAM)^[2].
BIX-01294 (1 µg/mL) causes reduction in the BrdU incorporation of fetal PASMCs. BIX-01294 treatment decreases the PASMCs migration induced by PDGF^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[1]

Cell Line:	Primary or recurrent tumor cells
Concentration:	2 μM
Incubation Time:	48 h
Result:	Selectively inhibited recurrent tumor cell growth.

In Vivo

BIX-01294 trihydrochloride (10 mg/kg; IP; three times a week for 2 weeks) significantly reduces tumor growth and tumor burden in recurrent tumor cells. Primary tumor growth is not inhibited^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female MMTV-rtTA;TetO-Her2/neu (MTB;TAN) and TetO-Her2/neu (TAN) mice with recurrent or primary tumor cells^[1]
Dosage:	10 mg/kg
Administration:	IP; three times a week for 2 weeks
Result:	Significantly reduced tumor growth and tumor burden in recurrent tumor cells. Primary tumor growth was not inhibited. Slowed the growth of orthotopic recurrent tumors in athymic nude recipients.

Molecular Weight

600.02

Formula

C₂₈H₄₁Cl₃N₆O₂

CAS No.

1392399-03-9

SMILES

CN(CCC1)CCN1C2=NC(C=C(OC)C(OC)=C3)=C3C(NC4CCN(CC5=CC=CC=C5)CC4)=N2.Cl.Cl.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Nathaniel W Mabe, et al. G9a Promotes Breast Cancer Recurrence through Repression of a Pro-inflammatory Program. Cell Rep. 2020 Nov 3;33(5):108341. [Content Brief]

[2]. Stefan Kubicek, et al. Reversal of H3K9me2 by a small-molecule inhibitor for the G9a histone methyltransferase. Mol Cell. 2007 Feb 9;25(3):473-81. [Content Brief]

[3]. Yang Q, et al. BIX-01294 treatment blocks cell proliferation, migration and contractility in ovine foetal pulmonary arterial smooth muscle cells. Cell Prolif. 2012 Aug;45(4):335-44. [Content Brief]

[4]. Iwona Anna Ciechomska, et al. BIX01294, an inhibitor of histone methyltransferase, induces autophagy-dependent differentiation of glioma stem-like cells. Sci Rep [Content Brief]

[5]. Yanqi Chang, et al.Structural basis for G9a-like protein lysine methyltransferase inhibition by BIX-01294. Nat Struct Mol Biol. 2009 Mar;16(3):312-7. [Content Brief]