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
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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Cell Line
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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
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[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
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[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] |
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.
Chemical Information
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CAS No. 256397-11-2
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Molecular Weight 468.47
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Formula C26H23F3N2O3
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
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]
[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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
LAB687 Related Classifications
Cat. No.: HY-177291
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- LAB687
- 256397-11-2
- LAB 687
- LAB-687
- Microsomal Triglyceride Transfer Protein (MTP)
- Smo
- Hedgehog
- LDLR
- microsomal triglyceride transfer protein
- hedgehog dependent cancers
- differential scanning calorimetry
- Hep G2 cells
- mouse Smoothened receptor
- Hedgehog signaling pathway
- powder X-ray diffraction
- apoB secretion
- polymorphic screening
- human Smoothened receptor
- Inhibitor
- inhibitor
- inhibit