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United States

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製品番号: HY-182987

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SMARCA2/SMARCA4 ligand-1

SMARCA2/SMARCA4 ligand-1 is a SMARCA2/SMARCA4 ligand with K_D values of 1.2 and 10.3 nM. SMARCA2/SMARCA4 ligand-1 binds SMARCA2/4 bromodomain via hydrogen bonds with asparagine and tyrosine residues, and a salt bridge with a glutamate residue. SMARCA2/SMARCA4 ligand-1 shows antiproliferative activity against cancer cells. SMARCA2/SMARCA4 ligand-1 can be used for the research of cancer, such as smarca4 mutant nonsmall cell lung cancer.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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。

分子式: C₂₀H₁₇BrN₄O
分子量:409.28

保管条件:

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

Data Sheet (271 KB)

SMARCA2/SMARCA4 ligand-1 構造式

価格（税別）

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性

製品説明

IC₅₀ & Target

^[1]

SMARCA2

1.2 nM (Kd)

SMARCA4

10.3 nM (Kd)

SMARCA2

98.5 nM (IC₅₀)

SMARCA4

285 nM (IC₅₀)

PBRM1

SWI/SNF Complex アイソフォーム固有の製品をすべて表示 :

体外実験

SMARCA2/SMARCA4 ligand-1 (Compound 4p) potently binds to purified SMARCA2 bromodomain with an IC₅₀ of 95.8 nM^[1].
SMARCA2/SMARCA4 ligand-1 binds to purified SMARCA4 bromodomain with potency with an IC₅₀ of 285 nM^[1].
SMARCA2/SMARCA4 ligand-1(0.064-200 μM) binds to purified SMARCA2 bromodomain with a K_d of 1.2 nM^[1].
SMARCA2/SMARCA4 ligand-1 (0.625-10 μM) binds to purified SMARCA4 bromodomain with a K_d of 10.3 nM^[1].
SMARCA2/SMARCA4 ligand-1 demonstrates high stability in aqueous solutions at pH 1 and pH 7 and in cell culture medium, retaining >99% purity over 24 h^[1].
SMARCA2/SMARCA4 ligand-1 (compound 4p) shows antiproliferative activity in NCI-H1568 and HEK-293 cells with IC₅₀ values of 13.94 and 11.76 μM^[1].
SMARCA2/SMARCA4 ligand-1 (20 μM; 2 h) rescues SMARCA2 and PBRM1 in NCI-H1568 cells, confirming target engagement dependency of the PROTAC effect^[1].

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

Western Blot Analysis^[1]

Cell Line:

NCI-H1568
Concentration:

20 μM
Incubation Time:

2 h (pre-incubation); 2 h (PROTAC 14 treatment)
Result:

Effectively restored SMARCA2 and PBRM1 protein levels reduced by PROTAC 14 (HY-183007) treatment.

Related Protocols :

Cell Viability Determination by MTT Colorimetric Assay

化学情報

分子量 409.28
分子式 C₂₀H₁₇BrN₄O
SMILES

O=C1[N-][N+]2=CC3=CC=C(C=C3C=C2C4=CC=CC(Br)=C14)N5CCNCC5
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

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

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (271 KB)
COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[1]. Zhang S, et al. N-Iminopyridinium Ylides as Chemically Stable Pharmacophores Enabling Targeted Degradation of SMARCA Proteins[J]. JACS Au, 2026.

Calculators

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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MOQ

Minimum order quantity

100 mg

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