hSMG-1 inhibitor 11j

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

Cat. No.: HY-124719 Purity: 99.82%: Data Sheet
COA

SDS
Handling Instructions
FAQs
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.

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

CAS No. : 1402452-15-6

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Customer Review

Based on 14 publication(s) in Google Scholar

14 Publications Citing Use of MCE hSMG-1 inhibitor 11j

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.

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Biological Activity
Purity & Documentation
References
Customer Review

Description

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]

In Vitro

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.

Molecular Weight

566.07

Formula

C₂₇H₂₈ClN₇O₃S

CAS No.

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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)

Solvent & Solubility

In Vitro:

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)

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: ≥ 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.

Purity & Documentation

Purity: 99.82%

Select Batch:

Data Sheet (272 KB) SDS (252 KB)

COA (245 KB) LCMS (92 KB)

Handling Instructions (2659 KB)

References

[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