연구용

Monastrol Kinesin 억제제

Name: Monastrol
Brand: Selleck Chemicals
SKU: S8439
Rating: 5 (19 reviews)

제품 번호S8439

Monastrol((±)-Monastrol)은 IC50이 14μM인 세포 투과성 저분자 kinesin-5(KIF11) 억제제로, 반방추체 분리 유지에 필수적입니다.

Monastrol Kinesin 억제제 Chemical Structure

화학 구조

분자량: 292.35

바로가기

품질 관리

배치: 순도: 99.86%

99.86

관련 타겟	Akt Wnt/beta-catenin PKC HSP ROCK Microtubule Associated Integrin Bcr-Abl Actin FAK
기타 Kinesin 억제제	GSK923295 Ispinesib (SB-715992) SB743921 HCl ARQ 621 K 858 BTB-1 VLS-1488(KIF18A-IN-6 ) H-Cys(Trt)-OH Filanesib hydrochloride GW406108X

세포 배양, 처리 및 작업 농도

세포주	분석 유형	농도	배양 시간	활성 설명	PMID
HeLa	Function assay		12 hrs	Inhibition of Eg5 ATPase activity expressed in HeLa cells after 12 hrs, IC50=6.1μM	17587586
HCT116	Cell cycle assay			Effect on cell cycle progression in human HCT116 cells assessed as mitotic arrest measured by doubling DNA content by fluorescence microscopy, EC50=1.2μM	18793847
HCT116	Cell cycle assay			Effect on cell cycle progression in human HCT116 cells assessed as increase in phospho-histone H3 by fluorescence microscopy, EC50=1.5μM	18793847
KBV1/KB3-1	Function assay			Drug resistant ratio of EC50 for human KBV1 cells overexpressing MDR1 to EC50 for KB3-1 cells, EC50=0.0012μM	20597485
HCT116	Antiproliferative assay		72 hrs	Antiproliferative activity against human HCT116 cells after 72 hrs by Alamar blue assay, EC50=24.155μM	20597485
hTERT-HME1	Antiproliferative assay		72 hrs	Antiproliferative activity against human hTERT-HME1 cells after 72 hrs by Alamar blue assay, EC50=45.082μM	20597485
KBV1	Antiproliferative assay		72 hrs	Antiproliferative activity against human KBV1 cells overexpressing MDR1 after 72 hrs by Alamar blue assay in presence of zosuquidar, EC50=45.394μM	20597485
HL-60(TB)	Growth inhibition assay			Growth inhibition of human HL-60(TB) cells, GI50=25.1μM	21855351
M14	Growth inhibition assay			Growth inhibition of human M14 cells, GI50=25.1μM	21855351
CCRF-CEM	Growth inhibition assay			Growth inhibition of human CCRF-CEM cells, GI50=31.6μM	21855351
K562	Growth inhibition assay			Growth inhibition of human K562 cells, GI50=31.6μM	21855351
MOLT4	Growth inhibition assay			Growth inhibition of human MOLT4 cells, GI50=31.6μM	21855351
SR	Growth inhibition assay			Growth inhibition of human SR cells, GI50=31.6μM	21855351
NCI-H522	Growth inhibition assay			Growth inhibition of human NCI-H522 cells, GI50=31.6μM	21855351
COLO205	Growth inhibition assay			Growth inhibition of human COLO205 cells, GI50=31.6μM	21855351
HCT116	Growth inhibition assay			Growth inhibition of human HCT116 cells, GI50=31.6μM	21855351
KM12	Growth inhibition assay			Growth inhibition of human KM12 cells, GI50=31.6μM	21855351
SF295	Growth inhibition assay			Growth inhibition of human SF295 cells, GI50=31.6μM	21855351
U251	Growth inhibition assay			Growth inhibition of human U251 cells, GI50=31.6μM	21855351
SK-MEL-2	Growth inhibition assay			Growth inhibition of human SK-MEL-2 cells, GI50=31.6μM	21855351
RPMI8266	Growth inhibition assay			Growth inhibition of human RPMI8266 cells, GI50=31.6μM	21855351
NCI-H322M	Growth inhibition assay			Growth inhibition of human NCI-H322M cells, GI50=39.8μM	21855351
HCC2998	Growth inhibition assay			Growth inhibition of human HCC2998 cells, GI50=39.8μM	21855351
HCT15	Growth inhibition assay			Growth inhibition of human HCT15 cells, GI50=39.8μM	21855351
SW620	Growth inhibition assay			Growth inhibition of human SW620 cells, GI50=39.8μM	21855351
SNB75	Growth inhibition assay			Growth inhibition of human SNB75 cells, GI50=39.8μM	21855351
SK-MEL-5	Growth inhibition assay			Growth inhibition of human SK-MEL-5 cells, GI50=39.8μM	21855351
UACC62	Growth inhibition assay			Growth inhibition of human UACC62 cells, GI50=39.8μM	21855351
SN12C	Growth inhibition assay			Growth inhibition of human SN12C cells, GI50=39.8μM	21855351
HL-60(TB)	Growth inhibition assay		24 hrs	Growth inhibition of human HL-60(TB) cells incubated for 24 hrs by MTT assay, IC50=0.147μM	28667871
MOLT4	Growth inhibition assay		24 hrs	Growth inhibition of human MOLT4 cells incubated for 24 hrs by MTT assay, IC50=0.215μM	28667871
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells	29435139
DAOY	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	29435139
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
NB-EBc1	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	29435139
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
BT-12	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	29435139
OHS-50	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells	29435139
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells	29435139
U-2 OS	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells	29435139
McCoy	Cytotoxicity assay		72 hrs	Cytotoxicity against mouse McCoy cells assessed as decrease in cell viability after 72 hrs by MTT assay, IC50=26.8μM	29908443
MM1S	Antiproliferative assay		72 hrs	Antiproliferative activity against human MM1S cells incubated for 72 hrs by MTT assay, IC50=8.7μM	ChEMBL
HCT116	Antiproliferative assay		72 hrs	Antiproliferative activity against human HCT116 cells incubated for 72 hrs by MTT assay, IC50=9μM	ChEMBL
C6	Antiproliferative assay	100 uM	24 hrs	Antiproliferative activity against rat C6 cells assessed as reduction in cell viability at 100 uM after 24 hrs by MTS assay relative to control	ChEMBL
C6	Cell cycle assay	100 uM	24 hrs	Cell cycle arrest in rat C6 cells assessed as accumulation at G2/M phase at 100 uM after 24 hrs by propidium iodide staining based flow cytometry	ChEMBL
U138MG	Apoptosis assay	200 uM	48 hrs	Induction of apoptosis in human U138MG cells at 200 uM after 48 hrs by Annexin V/propidium iodide staining based flow cytometry	ChEMBL
U138MG	Necrosis assay	200 uM	48 hrs	Induction of necrosis in human U138MG cells at 200 uM after 48 hrs by Annexin V/propidium iodide staining based flow cytometry	ChEMBL
C6	Apoptosis assay	100 uM	48 hrs	Induction of apoptosis in rat C6 cells at 100 uM after 48 hrs by Annexin V/propidium iodide staining based flow cytometry	ChEMBL
U138MG	Function assay	200 uM	24 hrs	Inhibition of EG5 in human U138MG cells assessed as monopolar spindle formation at 200 uM after 24 hrs by Hoechst staining based immunofluorescence microscopic method	ChEMBL
C6	Function assay	100 uM	24 hrs	Inhibition of EG5 in rat C6 cells assessed as monopolar spindle formation at 100 uM after 24 hrs by Hoechst staining based immunofluorescence microscopic method	ChEMBL
C6	Antiproliferative assay	5 to 50 uM	48 hrs	Antiproliferative activity against rat C6 cells at 5 to 50 uM after 48 hrs by Neubauer chamber method	ChEMBL
MCF7	Antiproliferative assay	25 uM	48 hrs	Antiproliferative activity against human MCF7 cells at 25 uM after 48 hrs by sulforhodamine B assay	ChEMBL
NCI/ADR-RES	Antiproliferative assay	25 uM	48 hrs	Antiproliferative activity against human NCI/ADR-RES cells at 25 uM after 48 hrs by sulforhodamine B assay	ChEMBL
786-0	Antiproliferative assay	25 uM	48 hrs	Antiproliferative activity against human 786-0 cells at 25 uM after 48 hrs by sulforhodamine B assay	ChEMBL
HT-29	Antiproliferative assay	25 uM	48 hrs	Antiproliferative activity against human HT-29 cells at 25 uM after 48 hrs by sulforhodamine B assay	ChEMBL
UACC62	Antiproliferative assay	25 uM	48 hrs	Antiproliferative activity against human UACC62 cells at 25 uM after 48 hrs by sulforhodamine B assay	ChEMBL
PC3	Antiproliferative assay	25 uM	48 hrs	Antiproliferative activity against human PC3 cells at 25 uM after 48 hrs by sulforhodamine B assay	ChEMBL
OVCAR3	Antiproliferative assay	25 uM	48 hrs	Antiproliferative activity against human OVCAR3 cells at 25 uM after 48 hrs by sulforhodamine B assay	ChEMBL
클릭하여 더 많은 세포주 실험 데이터 보기

화학 정보, 보관 및 안정성

분자량	292.35	화학식	C₁₄H₁₆N₂O₃S	보관 (수령일로부터)	3 years -20°C(in the dark) powder
CAS 번호	329689-23-8	SDF 다운로드		원액 보관	1년-80°C용매에 보관 1개월-20°C용매에 보관
동의어	(±)-Monastrol			Smiles	CCOC(=O)C1=C(NC(=S)NC1C2=CC(=CC=C2)O)C

용해도

In vitro
배치:

DMSO : 58 mg/mL (198.39 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 58 mg/mL

Water : Insoluble

DMSO : 69 mg/mL (236.01 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 15 mg/mL

Water : Insoluble

몰농도 계산기

질량	농도	부피	분자량
=	×	×

희석 계산기 분자량 계산기

In vivo 배치:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Selleck 연구소에서 검증되었습니다. 이 제형에 대한 조정이 필요한 경우 맞춤 테스트를 위해 당사 영업팀에 문의하십시오.	2.900mg/ml (9.92mM)
	5% DMSO 1 95% Corn oil Selleck 연구소에서 검증되었습니다. 이 제형에 대한 조정이 필요한 경우 맞춤 테스트를 위해 당사 영업팀에 문의하십시오.	0.710mg/ml (2.43mM)
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

생체 내 제형 계산기 (투명한 용액)

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

투여량: mg/kg 동물 평균 체중: g 동물당 투여량:μL 동물 수:

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

Targets/IC₅₀/Ki	KIF11(Eg5) (Cell-based assay) 14 μM
시험관 내(In vitro)	Monastrol은 세포 주기의 S 및 G2 단계 진행이나 중심체 복제를 억제하지 않습니다. 이 화합물로 인한 유사분열 정지 또한 빠르게 가역적입니다. 또한 Xenopus 난자 추출물에서 양극성 방추 형성도 억제합니다. 이 화학물질은 유사분열 세포를 단성 방추로 정지시키며, 이는 염색체 고리로 둘러싸인 방사형 미세소관 배열로 구성되며, 간기 세포의 미세소관이나 시험관 내 미세소관 중합에는 영향을 미치지 않습니다. 배양된 교감신경 뉴런을 이 화합물에 몇 시간 동안 노출시키면 축삭의 수와 성장 속도가 모두 증가합니다. 추가 시간이 지나면 축삭의 전체 길이는 대조군과 구별할 수 없습니다. 감각 뉴런은 축삭 성장 속도의 유사한 단기 증가를 보입니다. 그러나 장기간 노출되면 축삭이 짧아지는데, 이는 감각 뉴런이 약물의 독성 효과에 더 민감할 수 있음을 시사합니다. 그럼에도 불구하고, 배양물의 전반적인 건강은 일반적으로 항암 치료에 사용되는 약물인 탁솔로 처리된 배양물보다 훨씬 더 견고합니다. HeLa 세포에서 이 화합물은 방추체 검문점을 활성화하여 유사분열 정지 및 세포자멸사를 유발합니다.
참조	[1] https://pubmed.ncbi.nlm.nih.gov/10973989/ [2] https://pubmed.ncbi.nlm.nih.gov/14983520/ [3] https://pubmed.ncbi.nlm.nih.gov/17041103/ [4] https://pubmed.ncbi.nlm.nih.gov/10542155/

적용 분야

방법	바이오마커	이미지	PMID
Growth inhibition assay	Cell viability		26035434
Western blot	Cyclin B / Survivin		26035434

기술 지원

취급 설명서

Tel: +1-832-582-8158 Ext:3

다른 문의사항이 있으시면 메시지를 남겨주세요.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):