Home Metabolism P450 (e.g. CYP17) inhibitor Apigenin

연구용

Apigenin P450 (e.g. CYP17) inhibitor

제품 번호: S2262

Apigenin is a potent P450 inhibitor for CYP2C9 with Ki of 2 μM.
Apigenin P450 (e.g. CYP17) inhibitor Chemical Structure

화학 구조

분자량: 270.24

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품질 관리 (Quality Control)

배치: 순도: 99.73%
99.73

세포 배양, 처리 및 작업 농도
(Cell Culture, Treatment & Working Concentration)

세포주 분석 유형 농도 배양 시간 제형 활성 설명 PMID
mouse RAW264.7 cells Function assay Inhibition of COX2 protein expression in mouse RAW264.7 cells, IC50=0.5 μM
human H295R cells Function assay Inhibition of aromatase expressed in human H295R cells, IC50=1 μM
HEK293 FS cells Function assay Inhibition of NOX4 expressed in HEK293 FS cells assessed as H2O2 production by H2O2/Tyr/LPO assay, IC50=1.13 μM
human HeLa cells Function assay Inhibition of MRP1 transfected in human HeLa cells assessed as inhibition of [3H]LTC4 transport by rapid filtration assay, Ki=2.4 μM
human MV4-11 cells Cytotoxicity assay 72 h Cytotoxicity against human MV4-11 cells harboring FLT3 mutation after 72 hrs by tetrazolium based Ez CyTox cell viability assay, GI50=2.81 μM
human mast cells Function assay Inhibition of SYK in human mast cells assessed as reduction in mast cell degranulation, EC50=3 μM
MDCK cells Function assay Inhibition of BCRP expressed in MDCK cells using Hoechst 33342 staining, IC50=3.1 μM
human MDA-kb2 cells Function assay Antagonist activity at androgen receptor in human MDA-kb2 cells assessed as inhibition of DHT-induced luciferase activity by luciferase reporter gene assay, IC50=5.2 μM
MCF-7 MX cells Function assay Inhibition of BCRP expressed in MCF-7 MX cells using Hoechst 33342 staining, IC50=5.9 μM
mouse RAW264.7 cells Function assay 24 h Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced nitrite accumulation after 24 hrs by Griess reagent method, IC50=6.7 μM
human H9 cells Function assay 3 days Antiviral activity against HIV1 3B infected in human H9 cells assessed as inhibition of viral replication after 3 days by p24 antigen capture assay, EC50=9 μM
HEK293 cells Function assay 24 h Agonist activity at mouse PPARgamma expressed in HEK293 cells co-expressing with Gal4 reporter vector after 24 hrs by dual-luciferase reporter assay, EC50=24.9 μM
mouse 26-L5 cells Proliferation assay 72 h Antiproliferative activity against mouse 26-L5 cells after 72 hrs by MTT assay, EC50=25 μM
human RS4:11 cells Cytotoxicity assay 72 h Cytotoxicity against human RS4:11 cells harboring wild type FLT3 after 72 hrs by tetrazolium based Ez CyTox cell viability assay, GI50=27.9 μM
mouse B16-BL6 cells Proliferation assay 72 h Antiproliferative activity against mouse B16-BL6 cells after 72 hrs by MTT assay, EC50=31.6 μM
human H9 cells Cytotoxicity assay 3 days Cytotoxicity against human H9 cells after 3 days, IC50=35 μM
human HT1080 cells Proliferation assay 72 h Antiproliferative activity against human HT1080 cells after 72 hrs by MTT assay, IC
MDCK cells Cytotoxicity assay Cytotoxicity against MDCK cells by MTT assay, CC50=39.59 μM
mouse L929 cells Function assay 15 mins Potentiation of recombinant human TNF-alpha-induced cytotoxicity of mouse L929 cells assessed as survivality preincubated for 15 mins before TNFalpha addition measured after 24 hrs by crystal violet staining
human THP1 cells Function assay 20 uM 1 h Inhibition of NOX2 in human THP1 cells assessed as downregulation of TPA-induced CD36 mRNA expression at 20 uM incubated for 1 hr prior to TPA challenge measured after 24 hrs by RT-PCR analysis
MDA-MB-231 cells Function assay 5 uM Inhibition of PMA-stimulated NF-kappaB signaling (unknown origin) expressed in MDA-MB-231 cells at 5 uM incubated for 16 hrs by luciferase reporter gene assay
클릭하여 더 많은 세포주 실험 데이터 보기

화학 정보, 보관 및 안정성 (Chemical Information, Storage & Stability)

분자량 270.24 화학식

C15H10O5

보관 (수령일로부터)
CAS 번호 520-36-5 SDF 다운로드 원액 보관

용해도 (Solubility)

In vitro
배치:

DMSO : 54 mg/mL (199.82 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

몰농도 계산기

질량 농도 부피 분자량
희석 계산기 분자량 계산기

In vivo
배치:

생체 내 제형 계산기 (투명한 용액)

1단계: 아래 정보 입력 (권장: 실험 중 손실을 고려하여 추가 동물 포함)

mg/kg g μL

2단계: 생체 내 제형 입력 (이것은 계산기일 뿐 제형이 아닙니다. 용해도 섹션에 생체 내 제형이 없는 경우 먼저 당사에 문의하십시오.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

계산 결과:

작업 농도: mg/ml;

DMSO 원액 준비 방법: mg 약물 사전 용해 μL DMSO ( 원액 농도 mg/mL, 농도가 해당 약물 배치의 DMSO 용해도를 초과하는 경우 먼저 당사에 문의하십시오. )

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가μL PEG300, 혼합하고 투명하게 한 다음 추가μL Tween 80, 혼합하고 투명하게 한 다음 추가 μL ddH2O, 혼합하고 투명하게 합니다.

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가 μL 옥수수 기름, 혼합하고 투명하게 합니다.

참고: 1. 다음 용매를 추가하기 전에 액체가 투명한지 확인하십시오.
2. 용매를 순서대로 추가해야 합니다. 다음 용매를 추가하기 전에 이전 추가에서 얻은 용액이 투명한 용액인지 확인해야 합니다. 와동, 초음파 또는 뜨거운 물 중탕과 같은 물리적 방법을 사용하여 용해를 도울 수 있습니다.

작용 메커니즘 (Mechanism of Action)

특징
Much more potent than kaempferol and myricetin in CT-L inhibition.
Targets/IC50/Ki
CYP2C9
2 μM(Ki)
시험관 내(In vitro)
Apigenin inhibits PKC by competing with adenosine triphosphate (ATP). This compound also reduces the level of TPA-stimulated phosphorylation of cellular proteins and inhibits TPA-induced c-jun and c-fos expression. It exhibits the reverting effect on the transformed morphology of v-H-ras transformed NIH3T3 cells. It has been shown to possess anti-mutagenic properties in a setting of nitropyrene-induced genotoxicity in Chinese hamster ovary cells. This chemical suppresses of LPS-induced cyclooxygenase-2 and nitric oxide synthase-2 activity and expression in mouse macrophages. It has been reported to inhibit protein kinase C activity, mitogen-activated protein kinase (MAPK), transformation of C3HI mouse embryonic fibroblasts and downstream oncogenes in v-Ha-ras-transformed NIH3T3 cells. This compound blocks peroxisome proliferation-regulated kinase (ERK), a MAPK in isolated hepatocytes. It has further been shown to down-regulate the expression of the Na+/Ca2+-exchanger, a protein important for calcium extrusion in neonatal rat cardiac myocytes. It induces a reversible G2/M and G0/G1 arrest by inhibiting p34 (cdc2) kinase activity, accompanied by increased p53 protein stability in epidermal cells and fibroblasts. It is also effective in inhibiting TNFα-induced intracellular adhesion molecule-1 upregulation in cultured human endothelial cells. It inhibits the expression of HIF-1α and VEGF via the PI3K/Akt/p70S6K1 and HDM2/p53 pathways in human ovarian cancer cells. It inhibits differentiation by suppressing MAPK signal transduction and reducing API transcription factor level in human keratinocytes. This compound also inhibits proliferating of human keratinocytes.
생체 내(In vivo)
Apigenin down-regulates production of IL-4 in ovalbumin-immunized BALB/C mice. This compound inhibits melanoma lung metastases by impairing interaction of tumor cells with endothelium. It is shown to cause a significant increase in uterine weight and overall uterine concentration of estrogen receptor (ER)-α in female mice (64) and also suppresses prostate and breast cancer cell growth through estrogen receptor β1. This chemical suppresses the levels of IGF-I in prostate tumor xenografts and increases levels of IGFBP-3, a binding protein that sequesters IGF-I in vascular circulation. This compound (12.5 mg/kg) increases cell proliferation in the dentate gyrus of hippocampus of adult mice.
참조
  • [4] https://pubmed.ncbi.nlm.nih.gov/19441930/
  • [5] https://pubmed.ncbi.nlm.nih.gov/25859163/
  • [6] https://pubmed.ncbi.nlm.nih.gov/24067903/

적용 분야 (Applications)

방법 바이오마커 이미지 PMID
Western blot MHC / MHC2A / MHC2B / MyoD CXCR4 CDK1 / Cyclin B1 / p21
S2262-WB1
29108230
Immunofluorescence E-caherin / Vimentin Snail
S2262-IF1
27203387
Growth inhibition assay Cell viability
S2262-viability1
23224239