1. Stem Cell/Wnt
  2. Smo
  3. MRT-83

MRT-83 

Cat. No.: HY-18287 Purity: >98.0%
Handling Instructions

MRT-83 is a potent antagonist of Smo, with an IC50 in the nanomolar range. MRT-83 also blocks Hedgehog (Hh) signaling.

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

MRT-83 Chemical Structure

MRT-83 Chemical Structure

CAS No. : 1263131-92-5

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Description

MRT-83 is a potent antagonist of Smo, with an IC50 in the nanomolar range. MRT-83 also blocks Hedgehog (Hh) signaling.

IC50 & Target

Smo[1].

In Vitro

MRT-83 displays full antagonist properties with an IC50 (~3 nM) for inhibiting ShhN (3 nM)-induced proliferation of rat GCPs. MRT-83 also blocks SAG (0.01 μM)-induced proliferation of GCPs (IC50 ~6 nM). MRT-83 blocks BC binding to HEK-hSmo cells in a dose-dependent manner with an IC50 of 4.6 nM. MRT-83 abrogates BC binding to cells expressing mouse Smo with an IC50 of 14 nM, which is in good correlation with its IC50 in the Shh-light2 and alkaline phosphatase assays[1].

In Vivo

Animals treated with ShhN in the presence of MRT-83 are as healthy as those of the other groups but up-regulation of Ptc transcription in the SVZ of these animals is no longer observed in agreement with a complete inhibition of ShhN-mediated effects (8.7±2.4 Ptc+ cells/section, n=9) and is not different from vehicle-mediated effects. MRT-83 but not MRT-36 antagonizes the up-regulation of Ptc transcription induced by ShhN in vivo in the SVZ of the LV[1].

Molecular Weight

538.59

Formula

C₃₁H₃₀N₄O₅

CAS No.

1263131-92-5

SMILES

COC1=C(OC)C(OC)=CC(C(NC(NC2=CC(NC(C3=CC=C(C4=CC=CC=C4)C=C3)=O)=C(C)C=C2)=N)=O)=C1

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
References
Animal Administration
[1]

Mice[1]
Four groups of six animals received 5 μL of 45% 2-hydroxypropyl-β-cyclodextrin PBS solution containing 0.9 μg of ShhN alone or in the presence of MRT-83 (200 ng) or MRT-36 (110 ng). A control group receive 5 μL of 45% 2-hydroxypropyl-β-cyclodextrin solution alone. All groups are analyzed 48 h after the injection[1]

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

References

Purity: >98.0%

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MRT-83
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