hSMG-1 inhibitor 11j

Name: hSMG-1 inhibitor 11j
Brand: MedChemExpress
SKU: HY-124719
Rating: 5.0 (14 reviews)

製品番号: HY-124719 純度: 99.82%: Data Sheet SDS COA 取扱説明書
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Technical Support

hSMG-1 inhibitor 11j, a pyrimidine derivative, is a potent and selective inhibitor of hSMG-1, with an IC₅₀ of 0.11 nM. hSMG-1 inhibitor 11j exhibits >455-fold selectivity for hSMG-1 over mTOR (IC₅₀=50 nM), PI3Kα/γ (IC₅₀=92/60 nM) and CDK1/CDK2 (IC₅₀=32/7.1 μM). hSMG-1 inhibitor 11j can be used for the research of 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。

CAS 番号 : 1402452-15-6

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 623	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 623	在庫あり	Estimated Time of Arrival: December 31
Solid
1 mg	$200	在庫あり	Estimated Time of Arrival: December 31
5 mg	$500	在庫あり	Estimated Time of Arrival: December 31
10 mg	$850	在庫あり	Estimated Time of Arrival: December 31
25 mg	$1400	在庫あり	Estimated Time of Arrival: December 31
50 mg	$2000	在庫あり	Estimated Time of Arrival: December 31
100 mg	$3000	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

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* 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 14 publication(s) in Google Scholar

顧客検証

RT-PCR

Gel Electrophoresis

Cell Imaging/Staining

: hSMG-1 inhibitor 11j purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Jul 1;16(1):5828. [Abstract]; Violin plot comparing the expression changes of NMD transcripts across different groups of m⁶A levels in DMSO and hSMG-1 inhibitor 11j (SMG1i) (300 nM; 4 h) treated HEK293T cells.

: hSMG-1 inhibitor 11j purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Jul 1;16(1):5828. [Abstract]; Comparing the expression changes for misprocessed isoforms with their counterpart protein-coding transcripts, respectively, in DMSO and hSMG-1 inhibitor 11j (SMG1i, 300 nM; 4 h) treated HEK293T cells. The results demonstrate that inhibiting SMG1 using the hSMG-1 inhibitor 11j (SMG1i) selectively blocks the NMD pathway.

: hSMG-1 inhibitor 11j purchased from MedChemExpress. Usage Cited in: Cell Rep. 2025 Jul 17;44(8):115985. [Abstract]; Agarose gels of RT-PCR products for PEs in DHX9, RPS9, TRA2A, SRSF2, and SRSF6 in A704 cells treated with DMSO, mTORi, or hSMG-1 inhibitor 11j (SMG1i, 300 nM; 24 h), each with quantification of three biological replicates.

: hSMG-1 inhibitor 11j purchased from MedChemExpress. Usage Cited in: Pharm Biol. 2025 Dec;63(1):645-662. [Abstract]; Bright field images of human colonoids were taken after exposure to the indicated treatments, with observations made at 0 and 2 h following forskolin treatment. Colonoids were pre-treated for an hour with α,β-dehydromonacolin K (20 µM) with or without hSMG-1 inhibitor 11j (SMG1i) (1 µM) (scale bar = 500 µm). The results showed that the inhibitory effect of α,β-dehydromonacolin K on forskolin-induced fluid secretion was significantly diminished in the presence of the SMG1 inhibitor (hSMG-1 inhibitor 11j (SMG1i)).

: hSMG-1 inhibitor 11j purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Aug 8;14(1):4760. [Abstract]; Elevated transcript expression levels of two PTC-containing transcript isoforms of TP53 upon NMD inhibition by hSMG-1 inhibitor 11j (SMG1i, 300 nM, 4 h) in HCC1599 cells, as indicated by RT-PCR analysis. The 689-bpproduct corresponds to the predominant novel transcript isoform containing a retained intron, while the 170-bpproduct corresponds to a second, minor novel transcript isoform using a novel 3’ splice site. GAPDH was usedas the loading control for RT-PCR. Western blot analysis of phosphorylated UPF1 (pUPF1) was used to measureNMD activity, and β-actin was used as the loading control for Western blot. Each RT-PCR or Western blot wasrepeated twice and yielded consistent results.

PI3K アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

mTOR アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

mTOR mTORC1 mTORC2

GSK-3 アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

GSK-3 GSK-3α GSK-3β

CDK アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

生物活性
純度とドキュメンテーション
参考文献
カスタマーレビュー

製品説明

IC₅₀ & Target^[1]

hSMG-1

0.11 nM (IC₅₀)

mTOR

50 nM (IC₅₀)

PI3Kγ

60 nM (IC₅₀)

PI3Kα

92 nM (IC₅₀)

GSKα

260 (IC₅₀)

GSKβ

330 (IC₅₀)

CDK2

7.1 μM (IC₅₀)

CDK1

32 μM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	0.00011 μM Compound: 11j	Inhibition of human recombinant SMG1 expressed in HEK293 cells using GST-tagged p53 as substrate after 1 hr by DELFIA assay Inhibition of human recombinant SMG1 expressed in HEK293 cells using GST-tagged p53 as substrate after 1 hr by DELFIA assay	[PMID: 23021994]
MDA-MB-468	IC₅₀	75 nM Compound: 11j	Cytotoxicity against human MDA-MB-468 cells Cytotoxicity against human MDA-MB-468 cells	[PMID: 23021994]

体外実験

hSMG-1 inhibitor 11j (0.3-3 μM; 6 h) significantly reduces UPF1 phosphorylation at 0.3 μM, and eliminates it at 1 μM in MDA 361 cells^[1].
hSMG-1 inhibitor 11j inhibits MDA468 cell proliferation, with an IC₅₀ of 75 nM^[1].

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

分子量

566.07

分子式

C₂₇H₂₈ClN₇O₃S

CAS 番号

1402452-15-6

Appearance

Solid

Color

White to yellow

SMILES

O=S(C1=CC(NC2=NC=CC(C3=CC(C4=CC=C(NC(NC)=O)C=C4)=NC=C3)=N2)=CC=C1Cl)(N(CC)CC)=O

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

溶剤 & 溶解度

体外:

DMSO : 80 mg/mL (141.33 mM; Need ultrasonic; 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	1.7666 mL	8.8328 mL	17.6657 mL
5 mM	0.3533 mL	1.7666 mL	3.5331 mL
10 mM	0.1767 mL	0.8833 mL	1.7666 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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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: ≥ 6 mg/mL (10.60 mM); Clear solution

This protocol yields a clear solution of ≥ 6 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (60.0 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.

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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

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: 99.82%

Select Batch:

データシート (272 KB) SDS (252 KB)

COA (245 KB) LCMS (92 KB)

取扱説明書 (2659 KB)

参考文献

[1]. Gopalsamy A, et, al. Identification of pyrimidine derivatives as hSMG-1 inhibitors. Bioorg Med Chem Lett. 2012 Nov 1;22(21):6636-41. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	1.7666 mL	8.8328 mL	17.6657 mL	44.1641 mL
	5 mM	0.3533 mL	1.7666 mL	3.5331 mL	8.8328 mL
	10 mM	0.1767 mL	0.8833 mL	1.7666 mL	4.4164 mL
	15 mM	0.1178 mL	0.5889 mL	1.1777 mL	2.9443 mL
	20 mM	0.0883 mL	0.4416 mL	0.8833 mL	2.2082 mL
	25 mM	0.0707 mL	0.3533 mL	0.7066 mL	1.7666 mL
	30 mM	0.0589 mL	0.2944 mL	0.5889 mL	1.4721 mL
	40 mM	0.0442 mL	0.2208 mL	0.4416 mL	1.1041 mL
	50 mM	0.0353 mL	0.1767 mL	0.3533 mL	0.8833 mL
	60 mM	0.0294 mL	0.1472 mL	0.2944 mL	0.7361 mL
	80 mM	0.0221 mL	0.1104 mL	0.2208 mL	0.5521 mL
	100 mM	0.0177 mL	0.0883 mL	0.1767 mL	0.4416 mL