Home PI3K/Akt/mTOR Antineoplastic and Immunosuppressive Antibiotics inhibitor Honokiol

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Honokiol Antineoplastic and Immunosuppressive Antibiotics inhibitor

제품 번호: S2310

Honokiol is the active principle of magnolia extract that inhibits Akt-phosphorylation and promotes ERK1/2 phosphorylation. This compound causes G0/G1 phase arrest, induces apoptosis, and autophagy via the ROS/ERK1/2 signaling pathway. It inhibits hepatitis C virus (HCV) infection. Phase 3.
Honokiol Antineoplastic and Immunosuppressive Antibiotics inhibitor Chemical Structure

화학 구조

분자량: 266.334

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품질 관리 (Quality Control)

배치: 순도: 99.96%
99.96

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

세포주 분석 유형 농도 배양 시간 제형 활성 설명 PMID
human UACC-903 cells Cytotoxicity assay Cytotoxicity against human UACC-903 cells after 72 hrs by MTS assay, IC50=5.1 μM
Vero E6 cells Function assay Antiviral activity against SARS coronavirus in Vero E6 cells assessed as inhibition of viral replication by ELISA, EC50=6.5 μM
human UACC-903 cells Cytotoxicity assay Cytotoxicity against human UACC-903 cells after 24 hrs by MTS assay, IC50=7.45 μM
human A549 cells Cytotoxicity assay Cytotoxicity against human A549 cells after 72 hrs by MTS assay, IC50=7.75 μM
human CEM cells Cytotoxicity assay Cytotoxicity against human CEM cells, IC50=10.9 μM
HEK293 cells Function assay Agonist activity at RXRalpha in HEK293 cells assessed as transcriptional activation after 48 hrs by luciferase reporter gene assay, EC50=11.8 μM
human A549 cell Cytotoxicity assay 24 h Cytotoxicity against human A549 cells after 24 hrs by MTS assay, IC50=12.51 μM
human HT-29 cells Cytotoxicity assay 72 h Cytotoxicity against human HT-29 cells after 72 hrs by MTS assay, IC50=13.24 μM
human PBM cells Cytotoxicity assay Cytotoxicity against human PBM cells, IC50=16.1 μM
Hep-G2 cells Cytotoxicity assay Cytotoxicity of compound against human liver tumor cell line (Hep-G2) was determined, IC50=16.5 μM
human HepG2 cells Proliferation assay 24 h Antiproliferative activity against human HepG2 cells after 24 hrs by MTT assay, IC50=16.5 μM
human K562 cells Proliferation assay Antiproliferative activity against human K562 cells by MTT assay, IC50=21.1 μM
Vero cells Cytotoxicity assay Cytotoxicity against Vero cells, IC50=22.5 μM
human A2780 cells Proliferation assay Antiproliferative activity against cisplatin-sensitive human A2780 cells by MTT assay, IC50=30.5 μM
human SPC-A1 cells Proliferation assay Antiproliferative activity against human SPC-A1 cells by MTT assay, IC50=36.1 μM
HUVEC cells Function assay 20 μM 24 h Antimigratory activity against human HUVEC cells at 20 uM after 24 hrs by wound-healing assay
HEK293 cells Function assay 24-48 h Agonist activity at human RXR-alpha expressed in HEK293 cells coexpressing with pCMX-beta-gal after 24 to 48 hrs by luciferase reporter gene assay
human SH-SY5Y cells Function assay 10 μM 30 mins Neuroprotective activity in human SH-SY5Y cells assessed as inhibition of CHP and TBHP-induced cell death at 10 uM incubated for 30 mins prior to challenge measured after 3 hrs by MTT assay
클릭하여 더 많은 세포주 실험 데이터 보기

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

분자량 266.334 화학식

C18H18O2

 보관 (수령일로부터)
CAS 번호 35354-74-6 SDF 다운로드 원액 보관

동의어 NSC 293100 Smiles C=CCC1=CC(=C(C=C1)O)C2=CC(=C(C=C2)O)CC=C

용해도 (Solubility)

In vitro
배치:

DMSO : 53 mg/mL (198.99 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)

Targets/IC50/Ki
Akt-phosphorylation
MEK
시험관 내(In vitro)

Honokiol shows pro-apoptotic effects in melanoma, sarcoma, myeloma, leukemia, bladder, lung, prostate, oral squamous cell carcinoma and colon cancer cell lines. This compound is effective on inducing apoptosis in SVR angiosarcoma cells. Treatment of SVR cells with this chemical causes decreased phosphorylation of MAP kinase, akt, and c-src. In addition, it potentiates TRAIL-mediated apoptosis, and its cytotoxicity is partially abrogated by neutralizing antibodies to TRAIL. This compound also has direct antiangiogenic activity, in that it blocks the phosphorylation and rac activation due to VEGF-VEGFR2 interactions. It causes apoptosis in CLL cells through activation of caspase 8, followed by caspase 9 and 3 activation. This chemical prevents interleukin-4-mediated survival of CLL cells, and potentiats the cytotoxicity of CB-1348, FaraA, and 2-CdA. It kills myeloma cells from relapsed patients at doses that does not kill PBMCs. Caspase 3, 7, 8, and 9 are induced by this compound treatment, as well as PARP cleavage. It is found to induce apoptosis in the colon cancer cell lines RKO. This chemical potentiates apoptosis, suppresses osteoclastogenesis, and inhibits invasion through modulation of nuclear factor-kappaB activation pathway. It may act as a potent anti-inflammatory agent with multipotential activities due to an inhibitory effect on the PI3K/Akt pathway.

생체 내(In vivo)

Honokiol is highly effective against SVR angiosarcoma in nude mice. This compound inhibits the growth of RKO cells in murine xenografts. It prevents the growth of MDA-MD-231 breast cancer cells in murine xenografts.

참조
  • [4] https://pubmed.ncbi.nlm.nih.gov/15259066/
  • [5] https://pubmed.ncbi.nlm.nih.gov/16966432/
  • [6] https://pubmed.ncbi.nlm.nih.gov/18158873/
  • [7] https://pubmed.ncbi.nlm.nih.gov/17487375/
  • [8] https://pubmed.ncbi.nlm.nih.gov/15922325/

적용 분야 (Applications)

방법 바이오마커 이미지 PMID
Western blot p-EGFR / p-AKT / p-STAT3 / p-ERK / p-GSK3α/β / Bax / p-pRb / p-BAD / IκBα / CDK2 / CDK4 / Cyclin D1 p-Lyn / Lyn / p-PI3K
S2310-WB1
27458163
Immunofluorescence Vimentin / Occludin IκBα / NF-κB p65
S2310-IF1
24508063