BIX-01294

Name: BIX-01294
Brand: MedChemExpress
SKU: HY-10587
Rating: 5.0 (25 reviews)

Cat. No.: HY-10587 Purity: 98.75%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

BIX-01294 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 inhibits G9a/GLP by competing for binding with the amino acids N-terminal of the substrate lysine residue. BIX-01294, a (1H-1,4-diazepin-1-yl)-quinazolin-4-yl amine derivative, induces necroptosis and autophagy. BIX-01294 has antitumor activity in recurrent tumor cells.

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

BIX-01294 Chemical Structure

CAS No. : 935693-62-2

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 164	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 164	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 96	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 149	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 280	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 447	In-stock	Estimated Time of Arrival: December 31
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200 mg		Get quote

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Based on 25 publication(s) in Google Scholar

Other Forms of BIX-01294:

BIX-01294 hydrochloride hydrate Get quote
BIX-01294 trihydrochloride Get quote

23 Publications Citing Use of MCE BIX-01294

RT-PCR

: BIX-01294 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 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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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^[2]

EHMT2/G9a/KMT1C

EHMT1/GLP/KMT1D

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	2.8 μM Compound: BIX01294	Antiproliferative activity against human A549 cells after 48 hrs by CCK8 assay Antiproliferative activity against human A549 cells after 48 hrs by CCK8 assay	[PMID: 27393948]
HeLa	IC₅₀	0.966 μM Compound: BIX-01294	Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay	[PMID: 29624387]
HepG2	IC₅₀	3.7 μM Compound: BIX01294	Antiproliferative activity against human HepG2 cells after 48 hrs by CCK8 assay Antiproliferative activity against human HepG2 cells after 48 hrs by CCK8 assay	[PMID: 27393948]
HepG2	IC₅₀	4800 nM Compound: BIX01294; 1	Cytotoxicity against human HepG2 cells after 3 days by CellTiter blue assay Cytotoxicity against human HepG2 cells after 3 days by CellTiter blue assay	[PMID: 29308121]
HL-60	IC₅₀	2.2 μM Compound: BIX01294	Antiproliferative activity against human HL60 cells after 48 hrs by CCK8 assay Antiproliferative activity against human HL60 cells after 48 hrs by CCK8 assay	[PMID: 27393948]
K562	IC₅₀	3.9 μM Compound: BIX01294	Antiproliferative activity against human K562 cells after 48 hrs by CCK8 assay Antiproliferative activity against human K562 cells after 48 hrs by CCK8 assay	[PMID: 27393948]
MCF7	EC₅₀	3.3 μM Compound: 1; BIX01294	Antiproliferative activity against human MCF7 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells incubated for 72 hrs by MTT assay	[PMID: 31627059]
MDA-MB-231	EC₅₀	2.9 μM Compound: 1; BIX01294	Antiproliferative activity against human MDA-MB-231 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells incubated for 72 hrs by MTT assay	[PMID: 31627059]
MDA-MB-231	IC₅₀	9.6 μM Compound: 133; BIX-01294	Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell viability incubated for 72 hrs by MTT assay	[PMID: 35531606]

In Vitro

BIX-01294 (2 μM; 48 h) selectively inhibits recurrent tumor cell growth^[1].
BIX-01294 (1 μM) leads to a marked increase in phosphorylation of S345 of MLKL^[1].
BIX-01294 (1 μM) significantly upregulates the canonical p53 targets Cdkn1a (p21) and Gadd45a in recurrent tumor cell lines^[1].
BIX-01294 (1 μM; 6 days) causes the reduction in H3K9me2 levels in primary and recurrent tumor cells^[1].
BIX-01294 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)^[1].
BIX-01294 (4.1 μM; for 2 days) causes around a 20% reduction, concomitant with a comparable increase in the unmodified H3K9 fragment in H3K9me2 in mouse ES cells. BIX-01294 causes pronounced reduction in H3K9me2 and a small decrease for H3K9me3 and H3K9me1 in wild-type ES cells^[2].
BIX-01294 has no inhibition of the other histone methyltransferases even at concentrations of 45 μM. BIX-01294 does not affect SUV39H1 (H320R) and PRMT1 within the tested concentration range (up to 10 μM)^[2].
BIX-01294 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 hours
Result:	Selectively inhibited recurrent tumor cell growth.

In Vivo

BIX-01294 (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

490.64

Formula

C₂₈H₃₈N₆O₂

CAS No.

935693-62-2

Appearance

Solid

Color

White to off-white

SMILES

COC1=C(OC)C=C(C(NC2CCN(CC3=CC=CC=C3)CC2)=NC(N4CCN(C)CCC4)=N5)C5=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : ≥ 110 mg/mL (224.20 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.0382 mL	10.1908 mL	20.3815 mL
5 mM	0.4076 mL	2.0382 mL	4.0763 mL
10 mM	0.2038 mL	1.0191 mL	2.0382 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.75 mg/mL (5.60 mM); Clear solution

This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.75 mg/mL (5.60 mM); Clear solution

This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.75 mg/mL (5.60 mM); Clear solution

This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 98.75%

Select Batch:

Data Sheet (283 KB) SDS (393 KB)

COA (254 KB) RP-HPLC (206 KB) MS (69 KB)

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]. Kubicek S, 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]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.0382 mL	10.1908 mL	20.3815 mL	50.9539 mL
	5 mM	0.4076 mL	2.0382 mL	4.0763 mL	10.1908 mL
	10 mM	0.2038 mL	1.0191 mL	2.0382 mL	5.0954 mL
	15 mM	0.1359 mL	0.6794 mL	1.3588 mL	3.3969 mL
	20 mM	0.1019 mL	0.5095 mL	1.0191 mL	2.5477 mL
	25 mM	0.0815 mL	0.4076 mL	0.8153 mL	2.0382 mL
	30 mM	0.0679 mL	0.3397 mL	0.6794 mL	1.6985 mL
	40 mM	0.0510 mL	0.2548 mL	0.5095 mL	1.2738 mL
	50 mM	0.0408 mL	0.2038 mL	0.4076 mL	1.0191 mL
	60 mM	0.0340 mL	0.1698 mL	0.3397 mL	0.8492 mL
	80 mM	0.0255 mL	0.1274 mL	0.2548 mL	0.6369 mL
	100 mM	0.0204 mL	0.1019 mL	0.2038 mL	0.5095 mL

BIX-01294 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BIX-01294935693-62-2BIX01294BIX 01294Histone MethyltransferaseAutophagyH3K9me2H3K9me3recurrentMLKLp53Cdkn1ap21Gadd45aSUV39H1(H320R)PRMT1Inhibitorinhibitorinhibit

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BIX-01294

Customer Review

Other Forms of BIX-01294:

BIX-01294 Related Antibodies

23 Publications Citing Use of MCE BIX-01294

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Histone Methyltransferase Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

BIX-01294 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

BIX-01294 Related Classifications

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