AB284522

Aromatase (CYP19A) Inhibitor Screening Kit (Fluorometric)

Be the first to review this product! 리뷰 제출

(0 출판물)

Aromatase Inhibitor Screening Kit ab284522 enables rapid screening of drugs and other small molecules for compound-Aromatase interaction in a reliable, high-throughput fluorescence-based assay.

Individual kit components also available for purchase with a minimum order of 20 units. Contact us to discuss your needs.

대체 명칭 보기

ARO1, CYAR, CYP19, CYP19A1, Aromatase, CYPXIX, Cytochrome P-450AROM, Cytochrome P450 19A1, Estrogen synthase

3 이미지

Functional Studies - Aromatase (CYP19A) Inhibitor Screening Kit (Fluorometric) (AB284522)

FuncS

Supplier Data

Functional Studies - Aromatase (CYP19A) Inhibitor Screening Kit (Fluorometric) (AB284522)

Functional Studies - Aromatase standard curve.

Aromatase Substrate metabolite fluorescence standard curve. One mole of fluorescence standard corresponds to the metabolism of one mole of Aromatase Substrate.

FuncS

Supplier Data

Functional Studies - Aromatase (CYP19A) Inhibitor Screening Kit (Fluorometric) (AB284522)

Functional Studies - Reaction kinetics of recombinant human aromatase.

Reaction kinetics of recombinant human aromatase enzyme at 37°C in the presence and absence of the indicated aromatase inhibitors. The solvent control reaction contained assay buffer with 0.2% acetonitrile.

FuncS

Supplier Data

Functional Studies - Aromatase (CYP19A) Inhibitor Screening Kit (Fluorometric) (AB284522)

Functional studies - Dose-response curves for various aromatase ligands.

Dose-response curves for various aromatase ligands of differing structural and mechanistic classes. The potent competitive inhibitor letrozole, the mechanism-based irreversible inhibitor exemestane, the phytoestrogen-like synthetic flavonoid α-naphthoflavone and the antifungal ketoconazole (a competitive inhibitor of several CYP isoforms) are plotted in the graph. For dose-response curves, percent activity was calculated for each concentration of inhibitor by comparison to activity of reactions containing no inhibitor. For each inhibitor, IC₅₀ values were derived by 4-parameter logistic curve fitting with each point representing the mean ± SEM of at least four replicates. Assays were performed according to the kit protocol.

주요 정보

검출 방식

Fluorescent

샘플 타입

Inhibitor compounds

분석 유형

Enzyme activity

결과 유형

Quantitative

분석 플랫폼

Microplate reader, Fluorescence microscope

style

left-column

style

left-column

Reactivity 정보

{ "title": "Reactivity Data", "filters": { "stats": ["", "Reactivity", "Dilution Info", "Notes"] }, "values": { "Enzyme activity assay": { "reactivity":"TESTED_AND_REACTS", "dilution-info":"", "notes":"<p></p>" } } }

style

left-column

제품 세부 정보

The Aromatase Inhibitor Screening Kit (ab284522) (K984) enables rapid screening of drugs and other small molecules for compound-Aromatase interaction in a reliable, high-throughput fluorescence-based assay. The assay utilizes a fluorogenic substrate that is converted into a highly fluorescent metabolite detected in the visible range (Ex/Em = 488/527 nm), ensuring a high signal-to-background ratio with little interference by autofluorescence. The kit contains a complete set of reagents sufficient for performing 100 reactions in a 96-well plate format.

Other Notes
This product was previously called K984 Biovision Aromatase (CYP19A) Inhibitor Screening Kit (Fluorometric). Biovision was acquired by Abcam in 2021.

The Safety Datasheet for this product has been updated for certain countries. Please check the current version in the Support and downloads section.

style

left-column

제품 구성

{ "values": { "100Test": { "sellingSize": "100 Test", "publicAssetCode":"ab284522-100Test", "assetComponentDetails": [ { "size":"1 x 1 Vial", "name":"Beta-NADP Stock", "number":"AB284522-CMP05", "productcode":"" }, { "size":"1 x 1 Vial", "name":"Aromatase Inhibitor", "number":"AB284522-CMP02", "productcode":"" }, { "size":"1 x 100 mL", "name":"Aromatase Assay Buffer", "number":"AB284522-CMP01", "productcode":"" }, { "size":"1 x 1 Vial", "name":"Aromatase Substrate", "number":"AB284522-CMP03", "productcode":"" }, { "size":"1 x 1 Vial", "name":"100X NADPH Generating System II", "number":"AB284522-CMP06", "productcode":"" }, { "size":"1 x 50 µL", "name":"Aromatase Fluorescence Standard", "number":"AB284522-CMP04", "productcode":"" }, { "size":"2 x 1 Vial", "name":"Recombinant Human Aromatase", "number":"AB284522-CMP07", "productcode":"" } ] } } }

style

left-column

특성 및 보관 정보

배송 시 보관 조건

Blue Ice

적절한 단기 보관 조건

-20°C

적절한 장기 보관 조건

-20°C

보관 정보

-20°C

style

left-column

추가 정보

This supplementary information is collated from multiple sources and compiled automatically.

Aromatase also known as CYP19A is an enzyme responsible for the conversion of androgens into estrogens. It is a member of the cytochrome P450 superfamily and has a molecular mass of approximately 58 kDa. Aromatase is mainly expressed in the gonads brain adipose tissue and placenta. The activity of this enzyme is important for estrogen biosynthesis which is especially important in postmenopausal women where adipose tissue becomes an important estrogen source.

Biological function summary

The enzyme catalyzes the aromatization of androgens aiding in the production of estrogens like estradiol. This process is essential for maintaining estrogen levels in the human body. Aromatase operates as a monomer and does not form part of any larger complex. The balance of androgens and estrogens maintained by aromatase activity plays a significant role in reproductive functions and other physiological processes.

Pathways

Aromatase enzyme activity plays a pivotal role in the steroidogenesis pathway which involves the biosynthesis of steroid hormones. It is also a part of the estrogen signaling pathway interacting with other proteins like estrogen receptors. These pathways help regulate gene expression and are important in processes such as cell proliferation and differentiation linking aromatase function to broader metabolic and developmental effects.

Aromatase has a significant role in conditions such as hormone receptor-positive breast cancer and endometriosis. In breast cancer increased aromatase activity elevates estrogen levels promoting cancer cell growth. Anti-aromatase drugs like aromatase inhibitors target this enzyme to lower estrogen production. Additionally defects in aromatase activity can lead to disorders like aromatase deficiency resulting in an imbalance in sex hormone levels. Understanding its function aids in the development of therapies targeting proteins like the estrogen receptor which interacts with products of aromatase activity.

style

left-column

제품 프로토콜

style

left-column

타겟 정보

A cytochrome P450 monooxygenase that catalyzes the conversion of C19 androgens, androst-4-ene-3,17-dione (androstenedione) and testosterone to the C18 estrogens, estrone and estradiol, respectively (PubMed : 27702664, PubMed : 2848247). Catalyzes three successive oxidations of C19 androgens : two conventional oxidations at C19 yielding 19-hydroxy and 19-oxo/19-aldehyde derivatives, followed by a third oxidative aromatization step that involves C1-beta hydrogen abstraction combined with cleavage of the C10-C19 bond to yield a phenolic A ring and formic acid (PubMed : 20385561). Alternatively, the third oxidative reaction yields a 19-norsteroid and formic acid. Converts dihydrotestosterone to delta1,10-dehydro 19-nordihydrotestosterone and may play a role in homeostasis of this potent androgen (PubMed : 22773874). Also displays 2-hydroxylase activity toward estrone (PubMed : 22773874). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (CPR; NADPH-ferrihemoprotein reductase) (PubMed : 20385561, PubMed : 22773874).

See full target information CYP19A1

style

left-column

style

left-column

websiteProtocolBooklet

style

right-column

Product promise

저희는 고품질 시약으로 고객님의 연구를 서포트하고자 최선을 다하고 있으며, 모든 단계에서 함께 하겠습니다. 만약 제품이 기대한 성능을 보이지 않을 경우에도 Product Promise로 보호받으실 수 있습니다.

자세한 내용은 이용 약관을 확인해 주세요.

Please note: All products are 'FOR RESEARCH USE ONLY. NOT FOR USE IN DIAGNOSTIC OR THERAPEUTIC PROCEDURES'.

For licensing inquiries, please contact partnerships@abcam.com

Aromatase (CYP19A) Inhibitor Screening Kit (Fluorometric)

Functional Studies - Aromatase (CYP19A) Inhibitor Screening Kit (Fluorometric) (AB284522)

Functional Studies - Aromatase (CYP19A) Inhibitor Screening Kit (Fluorometric) (AB284522)

Functional Studies - Aromatase (CYP19A) Inhibitor Screening Kit (Fluorometric) (AB284522)

주요 정보

검출 방식

샘플 타입

분석 유형

결과 유형

분석 플랫폼

보완 제품

Assay Kits

Primary Antibodies

Secondary Antibodies

Assay Kits

Reactivity 정보

제품 세부 정보

제품 구성

특성 및 보관 정보

배송 시 보관 조건

적절한 단기 보관 조건

적절한 장기 보관 조건

보관 정보

추가 정보

Biological function summary

Pathways

제품 프로토콜

타겟 정보

Product promise