1. Metabolic Enzyme/Protease Apoptosis NF-κB Immunology/Inflammation
  2. SHMT Apoptosis Reactive Oxygen Species (ROS)
  3. SHMT2-IN-1

SHMT2-IN-1 is a potent serine hydroxymethyltransferase 2 (SHMT2) inhibitor with an IC50 of 1.21 μM and a KD of 10.6 μM. SHMT2-IN-1 binds to the folate binding site of SHMT2. SHMT2-IN-1 also inhibits SHMT1 with an IC50 of 1.83 μM. SHMT2-IN-1 can inhibit cancer cells proliferation, migration and invasion. SHMT2-IN-1 can induce cells apoptosis and ROS production and cause G2/M phase arrest. SHMT2-IN-1 can be used for the research of cancer, such as esophageal cancer.

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

SHMT2-IN-1

SHMT2-IN-1 Chemical Structure

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Description

SHMT2-IN-1 is a potent serine hydroxymethyltransferase 2 (SHMT2) inhibitor with an IC50 of 1.21 μM and a KD of 10.6 μM. SHMT2-IN-1 binds to the folate binding site of SHMT2. SHMT2-IN-1 also inhibits SHMT1 with an IC50 of 1.83 μM. SHMT2-IN-1 can inhibit cancer cells proliferation, migration and invasion. SHMT2-IN-1 can induce cells apoptosis and ROS production and cause G2/M phase arrest. SHMT2-IN-1 can be used for the research of cancer, such as esophageal cancer[1].

IC50 & Target[1]

SHMT2

1.21 μM (IC50)

Human SHMT1

1.83 μM (IC50)

In Vitro

SHMT2-IN-1 (0.1-10 μM, 24 h) exhibits potent antiproliferative activity against esophageal cancer cells KYSE-450 and KYSE-70 with IC50 values of 1.62 μM and 1.18 μM respectively[1].
SHMT2-IN-1 (2.5-10 μM, 24 h) dose-dependently inhibits the migration and invasion of KYSE-450 and KYSE-70 cells[1].
SHMT2-IN-1 (2.5-7.5 μM, 24-72 h) induces apoptosis, ROS production and cause G2/M phase arrest in KYSE-450 and KYSE-70 cells[1].

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

Apoptosis Analysis[1]

Cell Line: KYSE-450 and KYSE-70 cells
Concentration: 2.5, 5 and 7.5 μM
Incubation Time: 72 h
Result: Increased apoptotic cells.
Upregulated Bax expression and downregulated Bcl-2, Pro-Caspase 3 and Pro-Caspase 9 expression.
Molecular Weight

558.03

Formula

C26H16ClN7O2S2

Appearance

Solid

Color

White to off-white

SMILES

N#CC1=C(N=C(N=C1C2=CC=C(C=C2)Cl)SCC3=CC=C(C=C3)C(O)=O)SC4=NN=NN4C5=CC=CC=C5

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Purity & Documentation
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  • 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.

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Product Name:
SHMT2-IN-1
Cat. No.:
HY-178432
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