Home Metabolism HSP inhibitor Novobiocin Sodium (Cathomycin, Albamycin)

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Novobiocin Sodium (Cathomycin, Albamycin) Hsp90 C-terminal Inhibitor

제품 번호: S2492

Novobiocin Sodium (NSC 2382, Albamycin, Cathomycin) is an aminocoumarin antibiotic that targets bacterial DNA gyrase (TopoIV), used to treat susceptible gram positive bacteria.
Novobiocin Sodium (Cathomycin, Albamycin) HSP inhibitor Chemical Structure

화학 구조

분자량: 634.61

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품질 관리 (Quality Control)

배치: 순도: 99.91%
99.91

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

세포주 분석 유형 농도 배양 시간 제형 활성 설명 PMID
MCF7-MX Function assay TP_TRANSPORTER: inhibition of mitoxantrone efflux in BCRP-expressing MCF7-MX cells, IC50=25μM 16460798
MELN Function assay 200 uM 18 hrs Inhibition of estradiol-induced ER-mediated transcription in MELN cells by measuring luciferase activity at 200 uM after 18 hrs 17979263
SH-SY5Y Neuroprotection assay Neuroprotection against beta-amyloid peptide 1-42-induced toxicity in human SH-SY5Y cells assessed as lactate dehydrogenase release, EC50=0.04839μM 19138859
SH-SY5Y Neuroprotection assay 10 nM Neuroprotection against beta-amyloid peptide 1-42-induced toxicity in retinoic acid-differentiated human SH-SY5Y cells assessed as lactate dehydrogenase release at 10 nM 19138859
SH-SY5Y Neuroprotection assay Neuroprotection against beta-amyloid peptide 1-42-induced toxicity in retinoic acid-differentiated human SH-SY5Y cells assessed as lactate dehydrogenase release 19138859
LNCaP-LN3 Antiproliferative assay Antiproliferative activity against human LNCaP-LN3 cells, IC50=1.05μM 21129982
yeast PP30 Function assay 100 uM 3 hrs Inhibition of human HSP90alpha expressed in yeast PP30 cells co-expressing HSF-lacZ reporter assessed as inhibition of heat stress-induced response at 100 uM after 3 hrs 21129982
Sf9 Function assay Inhibition of Escherichia coli His6-tagged ParC/ParE expressed in baculovirus-infected Sf9 cells by gel electrophoresis, IC50=0.21μM 21235241
SKBR3 Function assay 1000 uM 18 hrs Inhibition of HSP90 in human SKBR3 cells assessed as aggregation of intracellular HER2 at 1000 uM after 18 hrs by DAPI staining-based immunofluorescence microscopic analysis 23859777
BL21 (DE3) pLysS Function assay 100 mins Inhibition of 6-His-tagged Mycobacterium smegmatis GyrB expressed in Escherichia coli BL21 (DE3) pLysS cells incubated for 100 mins in presence of ATP by malachite green dye based ATP assay, IC50=0.18μM 25129171
BL21 (DE3) pLysS Function assay 100 mins Inhibition of Mycobacterium smegmatis GyrB ATPase activity expressed in Escherichia coli BL21 (DE3) pLysS cells after 100 mins by inorganic phosphate release detection based malachite green reagent assay, IC50=0.18μM 25801151
BL21 (DE3) pLysS Function assay 100 mins Inhibition of Mycobacterium smegmatis DNA gyrase B expressed in Escherichia coli BL21 (DE3) pLysS cells assessed as reduction in ATPase activity incubated for 100 mins by inorganic phosphate detection assay, IC50=0.18μM 26318054
BL21 (DE3) pLysS Function assay 120 mins Inhibition of Mycobacterium smegmatis 155 6His-tagged DNA gyrase B catalytic domain ATPase activity expressed in Escherichia coli BL21 (DE3) pLysS cells assessed as inorganic phosphate release after 120 mins in presence of ATP by malachite green dye based, IC50=0.046μM 27371925
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화학 정보, 보관 및 안정성 (Chemical Information, Storage & Stability)

분자량 634.61 화학식

C31H35N2O11.Na

 보관 (수령일로부터)
CAS 번호 1476-53-5 SDF 다운로드 원액 보관

동의어 Albamycin,Cathomycin,NSC 2382 Smiles CC1=C(C=CC2=C1OC(=O)C(=C2O)NC(=O)C3=CC(=C(C=C3)[O-])CC=C(C)C)OC4C(C(C(C(O4)(C)C)OC)OC(=O)N)O.[Na+]

용해도 (Solubility)

In vitro
배치:

DMSO : 100 mg/mL (157.57 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : 100 mg/mL

Ethanol : 100 mg/mL

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
Topoisomerase II
Topoisomerase IV
시험관 내(In vitro)

Novobiocin also interacts with Hsp90, altering the affinity of the chaperone for geldanamycin and radicicol and causing in vitro and in vivo depletion of key regulatory Hsp90-dependent kinases including v-Src, Raf-1, and p185(ErbB2). Novobiocin interferes with association of the co-chaperones Hsc70 and p23 with Hsp90.

Novobiocin specifically inhibits the maturation of the heme-regulated eIF2alpha kinase (HRI) in a concentration-dependent manner. Novobiocin induces the dissociation of Hsp90 and Cdc37 from immature HRI, while the Hsp90 cochaperones p23, FKBP52, and protein phosphatase 5 remained associated with immature HRI.

Novobiocin causes morphological and biochemical changes which lead to induction of cell death exhibiting characteristic features of metazoan apoptosis.

Novobiocin, a HSP90 inhibitor, could decrease the expression of SMYD3 and dose dependently inhibit the proliferation and migration of MDA-MB-231 human breast cancer cells. Novobiocin can inhibit the migration of breast cancer cells and such event may involve the downregulation of SMYD3.

Novobiocin, an aminocoumarin antibiotic, interferes with heat shock protein 90 and hypoxia inducible factor dependent gene expression and thus compromises cell survival. Novobiocin (500 礛) results in a significant increase of [Ca(2+)]i, decrease of forward scatter, increase of annexin-V-binding and enhances ceramide formation. Novobiocin stimulates eryptosis, an effect at least in part due to entry of extracellular Ca(2+) and formation of ceramide.

생체 내(In vivo)

Novobiocin sodium shows anti-infection activity in mice infected with amoxicillin-resistant Streptococcus pneumoniae.
참조
  • [4] https://pubmed.ncbi.nlm.nih.gov/20039369/
  • [5] https://pubmed.ncbi.nlm.nih.gov/24643001/
  • [6] https://pubmed.ncbi.nlm.nih.gov/20303716/