2. Metabolic Enzyme/Protease Stem Cell/Wnt
  3. Microsomal Triglyceride Transfer Protein (MTP) Smo Hedgehog LDLR
  4. 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.

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LAB687

LAB687 Chemical Structure

CAS No. : 256397-11-2

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LAB687 Related Antibodies

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Description

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[1][2][3].

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.

LAB687 Related Antibodies
Molecular Weight

468.47

Formula

C26H23F3N2O3
CAS No.
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.
Purity & Documentation
References
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LAB687 Related Classifications

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Help & FAQs
  • 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.

Keywords:

LAB687256397-11-2LAB 687LAB-687Microsomal Triglyceride Transfer Protein (MTP)SmoHedgehogLDLRSmoothenedLow-density lipoprotein receptormicrosomal triglyceride transfer proteinhedgehog dependent cancersdifferential scanning calorimetryHep G2 cellsmouse Smoothened receptorHedgehog signaling pathwaypowder X-ray diffractionapoB secretionpolymorphic screeninghuman Smoothened receptorInhibitorinhibitorinhibit

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