BRM/BRG1 ATP Inhibitor-1

Name: BRM/BRG1 ATP Inhibitor-1
Brand: MedChemExpress
SKU: HY-119374
Rating: 5.0 (40 reviews)

製品番号: HY-119374 純度: 99.72%: Data Sheet SDS COA 取扱説明書
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BRM/BRG1 ATP Inhibitor-1 (compound 14) is an orally active allosteric dual brahma homolog (BRM)/SWI/SNF related matrix associated actin dependent regulator of chromatin subfamily A member 2 (SMARCA2) and brahma related gene 1 (BRG1)/SMARCA4 ATPase activity inhibitor, both IC₅₀s are below 0.005 µM. BRM/BRG1 ATP Inhibitor-1 has anticancer activity.

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研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号 : 2270879-17-7

容量	価格（税別）	在庫状況	数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 605	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 605	在庫あり	Estimated Time of Arrival: December 31
Solid
5 mg	$550	在庫あり	Estimated Time of Arrival: December 31
10 mg	$825	在庫あり	Estimated Time of Arrival: December 31
25 mg	$1450	在庫あり	Estimated Time of Arrival: December 31
50 mg	$2100	在庫あり	Estimated Time of Arrival: December 31
100 mg	$2950	在庫あり	Estimated Time of Arrival: December 31
200 mg		お問い合わせ
500 mg		お問い合わせ

or バルクお問い合わせ

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 40 publication(s) in Google Scholar

顧客検証

Bio/Physico-chemical Assay

: BRM/BRG1 ATP Inhibitor-1 purchased from MedChemExpress. Usage Cited in: Cell. 2025 Aug 7;188(16):4424-4440.e17. [Abstract]; Line plots compared four proteomic analyses on MCF7 cells treated with the BAF inhibitor BRM/BRG1 ATP Inhibitor-1 (BRM014) (1 μM; 20 min). The drug target SMARCA4/2 (BRG1/BRM) and selected chromatin organizers were highlighted, with particularly significant changes in the photo-crosslinked DNA interactome.

: BRM/BRG1 ATP Inhibitor-1 purchased from MedChemExpress. Usage Cited in: Nature. 2024 Apr;628(8007):442-449. [Abstract]; BRM/BRG1 ATP Inhibitor-1 (BRM014) (1 μM; 2 h), a small molecule inhibitor that is specific for the SWI/SNF ATPases SMARCA4 and SMARCA2³⁴, largely rescued the effect of DCAF5 knockdown.

: BRM/BRG1 ATP Inhibitor-1 purchased from MedChemExpress. Usage Cited in: Nature. 2024 Dec;636(8043):745-754. [Abstract]; The BAF inhibitor BRM/BRG1 ATP Inhibitor-1 (BRM014) (10 μM; 30 min) reduced the average TF occupancy per enhancer and the TF binding distribution per molecule.

: BRM/BRG1 ATP Inhibitor-1 purchased from MedChemExpress. Usage Cited in: Cell. 2024 May 9:S0092-8674(24)00451-3. [Abstract]; Western blot of SMARCA4 and STAT1 in B16F10 cells treated with vehicle or BRM/BRG1 ATP Inhibitor-1 (BRM014) (30 nM–3 μM; 72 h).

: BRM/BRG1 ATP Inhibitor-1 purchased from MedChemExpress. Usage Cited in: Nature. 2023 Jun;618(7963):180-187. [Abstract]; BRM/BRG1 ATP Inhibitor-1 (BRM014) (1 μM; 90 min), a SMARCA4 ATPase inhibitor, significantly reduced the accessible regions in control Smarce1-MD(R42A) cells.

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参考文献
カスタマーレビュー

製品説明

IC₅₀ & Target

IC50: ﹤0.005 µM (BRM, BRG1)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
SBC-5	EC₅₀	> 10 μM Compound: 14	Antiproliferative activity against human SBC5 cells assessed as cell growth inhibition after 6 days by celltiter-glo luminescent cell viability assay Antiproliferative activity against human SBC5 cells assessed as cell growth inhibition after 6 days by celltiter-glo luminescent cell viability assay	[PMID: 30339381]

体外実験

BRM/BRG1 ATP Inhibitor-1 (compound 14) (0-10 μM, 5 days) can inhibit the proliferation of cancer cells^[1].
BRM/BRG1 ATP Inhibitor-1 inhibits KRT80 gene expression in H1299 cells with the AAC₅₀ (absolute AC₅₀) value of 0.01 μM and in RERF-LC-AI cells with an AAC₅₀ value of 0.01 μM^[1].

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

Cell Proliferation Assay^[1]

Cell Line:	SKMEL5 melanoma cells and SBC-5 small cell carcinoma
Concentration:	0-10 μM
Incubation Time:	5 days
Result:	Inhibited the proliferation of SKMEL5 cells with an AAC₅₀ (absolute AC₅₀) value of 0.004 μM and of SBC-5 cells with the AAC₅₀more than 10 μM.

体内実験

BRM/BRG1 ATP Inhibitor-1 (compound 14) (oral administration, 7.5 or 20 mg/kg, everyday, 3 weeks) can inhibit tumor growth and inhibit KRT80 expression in a dose-dependent manner^[1].

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

Animal Model:	Female athymic nude mice with RERF-LC-AI tumor xenografts^[1]
Dosage:	7.5 mg/kg, 20 mg/kg
Administration:	Oral administration; everyday; 3 weeks
Result:	Inhibited tumor growth by 21% and 55% at doses of 7.5 mg/kg and 20 mg/kg, respectively. Inhibited KRT80 expression by up to 90% at 20 mg/kg for 7 hours after administration.

分子量

318.27

分子式

C₁₁H₉F₃N₄O₂S

CAS 番号

2270879-17-7

Appearance

Solid

Color

White to off-white

SMILES

FC1=CC(NC(NC2=CC(C(F)F)=NS2)=O)=C(CO)C=N1

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶剤 & 溶解度

体外:

DMSO : 200 mg/mL (628.40 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.1420 mL	15.7099 mL	31.4199 mL
5 mM	0.6284 mL	3.1420 mL	6.2840 mL
10 mM	0.3142 mL	1.5710 mL	3.1420 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)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

体内:

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: ≥ 2.08 mg/mL (6.54 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (6.54 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (6.54 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 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.

純度とドキュメンテーション

純度: 99.72%

Select Batch:

データシート (276 KB) SDS (252 KB)

COA (249 KB) HNMR (273 KB) LCMS (96 KB)

取扱説明書 (2659 KB)

参考文献

[1]. Papillon JPN, et al. Discovery of Orally Active Inhibitors of Brahma Homolog (BRM)/SMARCA2 ATPase Activity for the Treatment of Brahma Related Gene 1 (BRG1)/SMARCA4-Mutant Cancers. J Med Chem. 2018 Nov 21;61(22):10155-10172 [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	3.1420 mL	15.7099 mL	31.4199 mL	78.5497 mL
	5 mM	0.6284 mL	3.1420 mL	6.2840 mL	15.7099 mL
	10 mM	0.3142 mL	1.5710 mL	3.1420 mL	7.8550 mL
	15 mM	0.2095 mL	1.0473 mL	2.0947 mL	5.2366 mL
	20 mM	0.1571 mL	0.7855 mL	1.5710 mL	3.9275 mL
	25 mM	0.1257 mL	0.6284 mL	1.2568 mL	3.1420 mL
	30 mM	0.1047 mL	0.5237 mL	1.0473 mL	2.6183 mL
	40 mM	0.0785 mL	0.3927 mL	0.7855 mL	1.9637 mL
	50 mM	0.0628 mL	0.3142 mL	0.6284 mL	1.5710 mL
	60 mM	0.0524 mL	0.2618 mL	0.5237 mL	1.3092 mL
	80 mM	0.0393 mL	0.1964 mL	0.3927 mL	0.9819 mL
	100 mM	0.0314 mL	0.1571 mL	0.3142 mL	0.7855 mL