Home Autophagy Autophagy inhibitor HCQ (Hydroxychloroquine) Sulfate

연구용

HCQ (Hydroxychloroquine) Sulfate Autophagy inhibitor

제품 번호: S4430

Hydroxychloroquine (HCQ) Sulfate is an antimalarial agent used for the treatment of systemic lupus erythematosus, rheumatoid arthritis and other autoimmune, inflammatory and dermatologic conditions. Also acts as an inhibitor of autophagy and toll-like receptor (TLR) 7/9.
HCQ (Hydroxychloroquine) Sulfate Autophagy inhibitor Chemical Structure

화학 구조

분자량: 433.95

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품질 관리 (Quality Control)

배치: 순도: 99.86%
99.86

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

세포주 분석 유형 농도 배양 시간 제형 활성 설명 PMID
Function assay HEK-Blue cells Antagonist activity at human TLR9 expressed in HEK-Blue cells assessed as reduction in CpGB-induced NF-kappaB levels after 24 hrs by spectrophotometric analysis, IC50 = 0.11 μM. 30292896
Antiviral assay Vero E6 cells 48 h IC50 for antiviral activity against SARS-CoV-2 in the Vero E6 cell line at 48 h by immunofluorescence-based assay (detecting the viral NP protein in the nucleus of the Vero E6 cells)., IC50 = 0.67608 μM. 32353859
Function assay HEK-Blue cells Antagonist activity at human TLR7 expressed in HEK-Blue cells assessed as reduction in CL264-induced NF-kappaB levels after 24 hrs by spectrophotometric analysis, IC50 = 0.8 μM. 30292896
Function assay HEK293 cells hERG binding assays: Displacement of [3H]-Dofetilide (5 nM final) from hERG membranes obtained from HEK293 cells, Ki = 2.51189 μM. 32353859
Antiviral assay Vero E6 cells IC90 for antiviral activity against SARS-CoV-2 in the Vero E6 cell line by measuring infectious viral titer of supernatent from compound-treated Vero E6 cells by Median Tissue Culture Infectious Dose (TCID)50 by the method of Reed and Muench, IC90 = 5.78 μM. 32353859
Antiproliferative assay BxPC3 cells 72 hrs Antiproliferative activity against human BxPC3 cells after 72 hrs by SRB method, IC50 = 33 μM. 25699157
qHTS assay A673 cells qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
qHTS assay BT-37 cells qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
qHTS assay SK-N-MC cells qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
qHTS assay NB-EBc1 cells qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
qHTS assay LAN-5 cells qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
Antiproliferative assay A549 cells 25 ug/ml 20 hrs Antiproliferative activity in human A549 cells at 25 ug/ml up to 20 hrs by xCELLigence RTCA SP based cellular impedance analysis 28570977
Antiproliferative assay A549 cells 25 ug/ml 60 hrs Antiproliferative activity in human A549 cells at 25 ug/ml after 60 hrs by xCELLigence RTCA SP based cellular impedance analysis 28570977
Autophagy assay NCI-H3122 cells 25 to 50 uM 6 hrs Inhibition of autophagy in human NCI-H3122 cells assessed as increase in punctate LC3 expression at 25 to 50 uM after 6 hrs by fluorescence microscopic analysis 25699157
Apoptosis assay H460 cells 25 to 75 uM 24 hrs Induction of apoptosis in human H460 cells at 25 to 75 uM after 24 hrs by annexin-V staining-based flow cytometry 25699157
Autophagy assay H460 cells 24 hrs Inhibition of autophagy in human H460 cells assessed as increase in LC3-2 level at IC50 after 24 hrs by immunoblot analysis 25699157
Antiviral assay Vero E6 cells 2 days Antiviral efficacy against SARS-CoV-2 (strain BavPat1) in Vero E6 cells assessed by inhibition of viral RNA replication measured by RT-PCR after 2 days, EC50 = 4.17 μM. ChEMBL
Antiviral assay Vero E6 cells 3 days IC50 determination at MOI 0.004 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in SARS-CoV-2 infected Vero E6 cells, IC50 = 9.21 μM. ChEMBL
Antiviral assay Vero E6 cells 3 days IC50 determination at MOI 0.01 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in SARS-CoV-2 infected Vero E6 cells, IC50 = 11.17 μM. ChEMBL
Antiviral assay Vero E6 cells 2 days Antiviral efficacy against SARS-CoV-2 (strain BavPat1) in Vero E6 cells assessed by inhibition of viral RNA replication measured by RT-PCR after 2 days, EC90 = 25.49 μM. ChEMBL
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화학 정보, 보관 및 안정성 (Chemical Information, Storage & Stability)

분자량 433.95 화학식

C18H28ClN3O5S

 보관 (수령일로부터)
CAS 번호 747-36-4 SDF 다운로드 원액 보관

동의어 NSC 4375 Smiles CCN(CCCC(C)NC1=C2C=CC(=CC2=NC=C1)Cl)CCO.OS(=O)(=O)O

용해도 (Solubility)

In vitro
배치:

Water : 87 mg/mL

DMSO : Insoluble
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

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
TLR9
Autophagy
시험관 내(In vitro)

Hydroxychloroquine Sulfate is a potent inhibitor of autophagy. It prevents lysosomal acidification, thereby interfering with a key step in the autophagic process.HCQ treatment inhibits RCC (renal cell cancer) cell growth, promotes apoptosis, inhibits mitochondrial oxygen consumption, and increases rates of glycolysis.
키나아제 분석
In vitro kinase assays
with purified proteins, recombinant S6 protein and recombinant active P70S6K are incubated in 1x kinase buffer with various amount of HCQ or RAD001 in the presence (25 μM) or absence of ATP for 30 minutes at 30°C. Total and phosphorylated S6 at ser235/236 and ser240/244 are detected by western analysis using phosphospecific antibodies. Note that recombinant GST-tagged S6 (53 kd) is distinguished from endogenous S6 (32 kd) on the western blot.
생체 내(In vivo)

The treatment of Hydroxychloroquine Sulfate reduces the infarct size in an in vivo rat model of I/R injury and the cardioprotective effect of Hydroxychloroquine is ERK1/2 dependent.

In addition, Hydroxychloroquine Sulfate shows an early vascular protective effect. HCQ seems to prevent the occurrence of endothelial dysfunction(ED) in treated animals.
참조
  • [4] http://acrabstracts.org/abstract/effects-of-in-vivo-treatment-with-hydroxychloroquine-on-endothelial-function-in-a-murine-model-of-systemic-lupus-erythematosus/
  • [5] https://pubmed.ncbi.nlm.nih.gov/24342772/

적용 분야 (Applications)

방법 바이오마커 이미지 PMID
Western blot NOX2 / β-actin p-NF-κB / β-actin NLRP3 / β-actin p62 / LC3-I / LC3-II / GAPDH
S4430-WB-1
32260307
IHC HE staining of spleen tissue
S4430-IHC-2
29456648
Immunofluorescence ZO-1
S4430-IF-1
32260307

임상시험 정보 (Clinical Trial Information)

(데이터 출처 https://clinicaltrials.gov, 업데이트 날짜 2024-05-22)

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NCT05733897 Recruiting
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NCT05237843 Unknown status
Recurrent Pregnancy Loss
Ain Shams University
 March 1 2022 Phase 1