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Cat. No.: HY-177291

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LAB687

LAB687 is a microsomal triglyceride transfer protein (MTP) inhibitor with an IC₅₀ of 0.9 nM for apolipoprotein B (apoB) secretion in HepG2 cells. LAB687 also acts as a Smoothened (Smo) antagonist, with IC₅₀ values of 2.48 μM and 3.42 μM against mouse and human Smo receptors, respectively. LAB687 reduces triglyceride and low-density lipoprotein cholesterol (LDL-C) levels, and inhibits the Hedgehog signaling pathway. LAB687 can be used in studies related to Hedgehog-dependent cancers.

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

CAS No.: 256397-11-2
Formula: C₂₆H₂₃F₃N₂O₃
Molecular Weight:468.47

Storage:

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

Data Sheet (269 KB)

LAB687 Chemical Structure

CAS No.: 256397-11-2

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- Cellular Effect
- In Vitro
Chemical Information
Protocols (1)
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

Description

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	2480 nM Compound: 2a, LAB687	Antagonist activity at mouse Smo receptor expressed in CHO cells by [3H]Hh-Ag binding assay Antagonist activity at mouse Smo receptor expressed in CHO cells by [3H]Hh-Ag binding assay	[PMID: 19091559]
CHO	IC₅₀	3420 nM Compound: 2a, LAB687	Antagonist activity at human Smo receptor expressed in CHO cells by [3H]Hh-Ag binding assay Antagonist activity at human Smo receptor expressed in CHO cells by [3H]Hh-Ag binding assay	[PMID: 19091559]
HepG2	IC₅₀	0.9 nM Compound: 2a, LAB687	Inhibition of MTP in human HepG2 cells assessed as apolipoprotein B production by ELISA Inhibition of MTP in human HepG2 cells assessed as apolipoprotein B production by ELISA	[PMID: 19091559]
TM3	IC₅₀	1200 nM Compound: 2a, LAB687	Inhibition of Hedgehog signaling pathway in mouse TM3 cells bearing pTA-8xGli-Luc reporter construct assessed as transcriptional modulation of Gli after 48 hrs by luciferase assay Inhibition of Hedgehog signaling pathway in mouse TM3 cells bearing pTA-8xGli-Luc reporter construct assessed as transcriptional modulation of Gli after 48 hrs by luciferase assay	[PMID: 19091559]

In Vitro

LAB687 (Compound 2a) binds to human and mouse Smoothened receptors, with IC₅₀ values of 3420 nM and 2480 nM, respectively^[1].
LAB687 inhibits apoB secretion in Hep G2 cells with an IC₅₀ of 0.9 nM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.

Chemical Information

CAS No. 256397-11-2
Molecular Weight 468.47
Formula C₂₆H₂₃F₃N₂O₃
SMILES

COC(N[C@@H]1CC2=CC=C(C=C2C1)NC(C(C=CC=C3C)=C3C4=CC=C(C(F)(F)F)C=C4)=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Protocols

All Cell Biology

Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (269 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Peukert S, et al. Identification and structure-activity relationships of ortho-biphenyl carboxamides as potent Smoothened antagonists inhibiting the Hedgehog signaling pathway. Bioorg Med Chem Lett. 2009;19(2):328-331. [Content Brief]

[2]. Mahavir Prashad, et al. Process Research and Development of a MTP Inhibitor: Another Case of
Disappearing Polymorphs upon Scale-up. Organic Process Research & Development 2010, 14, 878-882.

[3]. Shmeis RA, et al. A mechanistic investigation of an amorphous pharmaceutical and its solid dispersions, part I: a comparative analysis by thermally stimulated depolarization current and differential scanning calorimetry. Pharm Res. 2004;21(11):2025-2030. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

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Biological Activity
- Description
- In Vitro
Chemical Information
Protocols
Purity & Documentation
References

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LAB687