1. Immunology/Inflammation
  2. Galectin
  3. GB1841

GB1841 is an orally active and selective galectin inhibitor with human galectin-1 Kd of 0.027 μM, human galectin-3 Kd of 0.14 μM, mouse galectin-1 Kd of 0.034 μM and mouse galectin-3 Kd of 1.170 μM. GB1841 can be used for the research of lung cancer.

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

GB1841

GB1841 Chemical Structure

CAS No. : 2573135-33-6

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Description

GB1841 is an orally active and selective galectin inhibitor with human galectin-1 Kd of 0.027 μM, human galectin-3 Kd of 0.14 μM, mouse galectin-1 Kd of 0.034 μM and mouse galectin-3 Kd of 1.170 μM. GB1841 can be used for the research of lung cancer[1].

IC50 & Target[1]

Galectin-1

0.027 μM (Kd)

Galectin-3

0.14 μM (Kd)

In Vitro

GB1841 potently binds human galectin-1 (Kd 0.027 μM), human galectin-3 (Kd 0.14 μM), and human galectin-4C (Kd 0.25 μM); it also [1].
GB1841 potently binds mouse galectin-1 (Kd 0.034 μM) and mouse galectin-3 (Kd 1.170 μM)[1].
GB1841 reduces A549 human lung adenocarcinoma cell viability by 62% at 90 μM[1].

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

In Vivo

GB1841 (30 mg/kg; p.o.; b.i.d. for 3 days) achieves free plasma levels sufficient for mouse galectin-1 inhibition for over 24 h, with a >90-fold therapeutic window relative to cell toxicity[1].

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

Animal Model: C57BL/6 (female, 17−19 g, syngeneic implantation of LL/2 lung cancer cells)[1]
Dosage: 30 mg/kg
Administration: p.o.; b.i.d. for 3 days
Result: Achieved free plasma Cmax levels of 1 μM.
Remained above the mouse galectin-1 Kd (0.034 μM) for over 24 h.
Did not reach levels above the mouse galectin-3 Kd (1.170 μM).
Demonstrated a >90-fold therapeutic window compared to cell toxicity levels (62% viability reduction at 90 μM in A549 cells).
Molecular Weight

559.84

Formula

C18H16BrClN6O4S2

CAS No.
SMILES

O[C@@H]1[C@H](N2C=C(C3=NC(Cl)=CS3)N=N2)[C@@H](OC)[C@@H](SC4=C(C#N)N=CC(Br)=C4)O[C@@H]1CO

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Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
References
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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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GB1841
Cat. No.:
HY-183582
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