2. Metabolic Enzyme/Protease
  3. Cytochrome P450
  4. GW273297X

GW273297X is a selective CYP27A1 inhibitor. GW273297X blocks 27-hydroxycholesterol biosynthesis and sterol product formation in human macrophages. GW273297X reduces cancer cells colonization by inhibiting pro-metastatic effects of 27-hydroxycholesterol. GW273297X can be used for the researches of cancer and metabolic disease, such as breast cancer.

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

GW273297X

GW273297X Chemical Structure

CAS No. : 1713317-28-2

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GW273297X Related Antibodies

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View All Cytochrome P450 Isoform Specific Products:

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CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A CYP3A4 CYP17A1

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Description

GW273297X is a selective CYP27A1 inhibitor. GW273297X blocks 27-hydroxycholesterol biosynthesis and sterol product formation in human macrophages. GW273297X reduces cancer cells colonization by inhibiting pro-metastatic effects of 27-hydroxycholesterol. GW273297X can be used for the researches of cancer and metabolic disease, such as breast cancer[1][2].

IC50 & Target[1]

CYP27A1

 

In Vitro

GW273297X (1 μM; 24 h) potently inhibits CYP27A1 enzyme activity in PMA-differentiated THP-1 human macrophage-like cells[2].
GW273297X (1 μM; 24 h) potently inhibits CYP27A1 enzyme activity in PMA (HY-18739)-differentiated THP-1 human macrophage-like cells when cholesterol is used as substrate[2].
GW273297X (1 μM; 24 h) potently and nearly completely inhibits CYP27A1 enzyme activity in primary human monocyte-derived macrophages (HMDMs)[2].

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

GW273297X Related Antibodies
In Vivo

GW273297X (100 mg/kg; s.c.; daily; 28 days) attenuates high-fat diet-induced lung metastatic colonization by E0771 breast cancer cells in ovariectomized humanized APOE3 mice[1].
GW273297X (100 mg/kg; s.c.; daily; 5 days) reduces early-stage lung metastatic colonization by Met1 and E0771 breast cancer cells in naive wild-type mice[1].

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

Animal Model: Humanized APOE3 with E0771-iRFP cells (ovariectomized female, ~6 weeks of age at ovariectomy)[1]
Dosage: 100 mg/kg
Administration: s.c.; daily; 28 days
Result: Attenuated the increased lung metastatic burden induced by the high-fat diet, as measured by relative fluorescence of iRFP-expressing tumor cells.
Animal Model: wild-type with Met1 and E0771 breast cancer cells (naive)[1]
Dosage: 100 mg/kg
Administration: s.c.; daily; 5 days
Result: Reduced the number of Met1 metastatic colonies in the lungs, as measured by relative fluorescence of iRFP-expressing tumor cells.
Reduced lung metastatic colonization by E0771 cells; this effect was reversed by co-pretreatment with exogenous 27-hydroxycholesterol.
Molecular Weight

444.69

Formula

C29H48O3
CAS No.
SMILES

C[C@@]12[C@]3([H])[C@]([C@@H](C[C@]1([H])CC(OC)(CC2)OC)O)([H])[C@@]4([H])[C@](CC3)([C@H](CC4)[C@H](C)CCCCC#C)C
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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GW273297X 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:

GW273297X1713317-28-2G297XCytochrome P450CYPs27-hydroxycholesterolhuman macrophagesCYP27A1atherosclerosisE0771 breast cancer cellsmammary tumor cellsTHP-1 human macrophage-like cellsprimary human monocyte-derived macrophagesbreast cancermiceInhibitorinhibitorinhibit

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