연구용

I-BET151 (GSK1210151A) BET 억제제

Name: I-BET151 (GSK1210151A)
Brand: Selleck Chemicals
SKU: S2780
Rating: 5 (61 reviews)

제품 번호S2780

I-BET151 (GSK1210151A)은 무세포 분석에서 BRD2, BRD3 및 BRD4를 각각 0.5 μM, 0.25 μM, 0.79 μM의 IC50 값으로 표적하는 새로운 선택적 BET 억제제입니다.

I-BET151 (GSK1210151A) BET 억제제 Chemical Structure

화학 구조

분자량: 415.44

바로가기

품질 관리

배치: 순도: 99.99%

99.99

관련 타겟	HDAC JAK Histone Methyltransferase PKC PARP HIF PRMT EZH2 AMPK Histone Acetyltransferase
기타 BET 억제제	Pelabresib (CPI-0610) ZEN-3694 (BET-IN-19) Molibresib (I-BET-762) Mivebresib (ABBV-075) INCB054329 Birabresib (OTX015) Apabetalone (RVX-208) AZD5153 6-hydroxy-2-naphthoic acid CPI-203 I-BRD9

세포 배양, 처리 및 작업 농도

세포주	분석 유형	농도	배양 시간	제형	활성 설명	PMID
MV4;11	cytotoxicity assay	~100 μM		DMSO	IC50=26 nM	21964340
RS4;11	cytotoxicity assay	~100 μM		DMSO	IC50=192 nM	21964340
MOLM13	cytotoxicity assay	~100 μM		DMSO	IC50=120 nM	21964340
NOMO1	cytotoxicity assay	~100 μM		DMSO	IC50=15 nM	21964340
HEL	cytotoxicity assay	~100 μM		DMSO	IC50=1 μM	21964340
K562	cytotoxicity assay	~100 μM		DMSO	IC50>100 μM	21964340
MEG01	cytotoxicity assay	~100 μM		DMSO	IC50=25 μM	21964340
HL60	cytotoxicity assay	~100 μM		DMSO	IC50=890 nM	21964340
MV4;11	Apoptosis assay	~100 μM		DMSO	induces apoptosis	21964340
MOLM13	Apoptosis assay	~100 μM		DMSO	induces apoptosis	21964340
MV4;11	Function assay			DMSO	decreases the recruitment of BRD3/4 and impaired recruitment of CDK9 and PAF1 to the transcriptional start site	21964340
PBMC	Function assay			DMSO	inhibits IL-6 with pIC50 of 6.7	22437115
A2	Function assay	~10 μM		DMSO	reactivates latent HIV-1	23255218
A72	Function assay	~10 μM		DMSO	reactivates latent HIV-1	23255218
BC1	Growth inhibitory assay	~1 μM		DMSO	IC50=220 nM	23792448
BC3	Growth inhibitory assay	~1 μM		DMSO	IC50=460 nM	23792448
BCBL1	Growth inhibitory assay	~1 μM		DMSO	IC50=330 nM	23792448
BJAB	Growth inhibitory assay	~1 μM		DMSO	IC50=970 nM	23792448
Namalwa	Growth inhibitory assay	~1 μM		DMSO	IC50=970 nM	23792448
Jurkat	Growth inhibitory assay	~1 μM		DMSO	IC50=1220 nM	23792448
MM1S	Growth inhibitory assay	~1 μM		DMSO	IC50=760 nM	23792448
U266	Growth inhibitory assay	~1 μM		DMSO	IC50=950 nM	23792448
UM-PEL-1	Growth inhibitory assay	~1 μM		DMSO	IC50=210 nM	23792448
UM-PEL-3	Growth inhibitory assay	~1 μM		DMSO	IC50=180 nM	23792448
BC1	Function assay	500 nM		DMSO	induces cell-cycle arrest	23792448
BC3	Function assay	500 nM		DMSO	induces cell-cycle arrest	23792448
BC1	Function assay	800 nM		DMSO	reduces c-Myc protein levels	23792448
BC3	Function assay	800 nM		DMSO	reduces c-Myc protein levels	23792448
H929	Function assay	~1 μM		DMSO	induces cell cycle arrest	24335499
KMS12PE	Function assay	~1 μM		DMSO	induces cell cycle arrest	24335499
KMS12BM	Function assay	~1 μM		DMSO	induces cell cycle arrest	24335499
KMS18	Function assay	~1 μM		DMSO	induces cell cycle arrest	24335499
KMS11	Function assay	~1 μM		DMSO	induces cell cycle arrest	24335499
RPMI8226	Function assay	~1 μM		DMSO	induces cell cycle arrest	24335499
H929	Apoptosis assay	~1 μM		DMSO	induces cell apoptosis	24335499
KMS12PE	Apoptosis assay	~1 μM		DMSO	induces cell apoptosis	24335499
KMS12BM	Apoptosis assay	~1 μM		DMSO	induces cell apoptosis	24335499
KMS18	Apoptosis assay	~1 μM		DMSO	induces cell apoptosis	24335499
KMS11	Apoptosis assay	~1 μM		DMSO	induces cell apoptosis	24335499
RPMI8226	Apoptosis assay	~1 μM		DMSO	induces cell apoptosis	24335499
U87MG	Function assay	~10 μM		DMSO	reduces U87MG cellular ATP with IC50 of 1.05 μM	24496381
A172	Function assay	~10 μM		DMSO	reduces cellular ATP with IC50 of 1.28 μM	24496381
SW1783	Function assay	~10 μM		DMSO	reduces cellular ATP with IC50 of 2.68 μM	24496381
U87MG	Function assay	~10 μM		DMSO	increases proportion of cells in the G1/S transition	24496381
RAW267.4	Function assay	1 μM		DMSO	reduces IL-6 production induced by LPS	24859008
RAW267.4	Function assay	1 μM		DMSO	reduces the association between BRD4 and acetylated p65	24859008
Me007	Growth inhibitory assay	~100 μM		DMSO	inhibits the growth	24906137
SK-Mel-28	Growth inhibitory assay	~100 μM		DMSO	inhibits the growth	24906137
Mel-RMU	Growth inhibitory assay	~100 μM		DMSO	inhibits the growth	24906137
Mel-JD	Growth inhibitory assay	~100 μM		DMSO	inhibits the growth	24906137
Mel-RM	Growth inhibitory assay	~100 μM		DMSO	inhibits the growth	24906137
Me007	Apoptosis assay	~100 μM		DMSO	induces apoptosis	24906137
SK-Mel-28	Apoptosis assay	~100 μM		DMSO	induces apoptosis	24906137
Mel-RMU	Apoptosis assay	~100 μM		DMSO	induces apoptosis	24906137
Mel-JD	Apoptosis assay	~100 μM		DMSO	induces apoptosis	24906137
Mel-RM	Apoptosis assay	~100 μM		DMSO	induces apoptosis	24906137
Me007	Function assay	10 μM		DMSO	induces cell cycle arrest by upregulation of p21	24906137
SK-Mel-28	Function assay	10 μM		DMSO	induces cell cycle arrest by upregulation of p21	24906137
Mel-RMU	Function assay	10 μM		DMSO	induces cell cycle arrest by upregulation of p21	24906137
Mel-JD	Function assay	10 μM		DMSO	induces cell cycle arrest by upregulation of p21	24906137
Mel-RM	Function assay	10 μM		DMSO	induces cell cycle arrest by upregulation of p21	24906137
Me007	Function assay	10 μM		DMSO	upregulates proapoptotic and cell cycle arrest genes	24906137
SK-Mel-28	Function assay	10 μM		DMSO	upregulates proapoptotic and cell cycle arrest genes	24906137
Mel-RMU	Function assay	10 μM		DMSO	upregulates proapoptotic and cell cycle arrest genes	24906137
Mel-JD	Function assay	10 μM		DMSO	upregulates proapoptotic and cell cycle arrest genes	24906137
Mel-RM	Function assay	10 μM		DMSO	upregulates proapoptotic and cell cycle arrest genes	24906137
HepG2	Function assay		18 hrs		Upregulation of ApoA1 expression in human HepG2 cells assessed as concentration required to increase 70% of luciferase activity after 18 hrs by luciferase reporter gene assay, EC170 = 0.09 μM.	22386529
Raji	Function assay		4 hrs		Inhibition of BRD4 in human Raji cells assessed as reduction of MYC expression after 4 hrs, IC50 = 0.13 μM.	24900758
MV4-11	Growth inhibition assay		72 hrs		Growth inhibition of human MV4-11 cells after 72 hrs by SRB assay, IC50 = 0.119 μM.	25559428
MM1S	Growth inhibition assay		72 hrs		Growth inhibition of human MM1S cells after 72 hrs by SRB assay, IC50 = 0.299 μM.	25559428
HT-29	Growth inhibition assay		72 hrs		Growth inhibition of human HT-29 cells after 72 hrs by SRB assay, IC50 = 0.945 μM.	25559428
Rosetta2 DE3	Function assay		30 mins		Displacement of FAM-labeled ZBA248 from BRD4 BD1 (44 to 168 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells after 30 mins by fluorescence polarization assay, IC50 = 0.0317 μM.	26080064
MV4-11	Cytotoxicity assay		4 days		Cytotoxicity against human MV4-11 cells harboring MLL1 fusion gene assessed as growth inhibition after 4 days by CellTiter-Glo luminescent assay, IC50 = 0.162 μM.	26080064
Rosetta2 DE3	Function assay		30 mins		Displacement of FAM-labeled ZBA248 from BRD4 BD2 (333 to 460 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells after 30 mins by fluorescence polarization assay, IC50 = 0.226 μM.	26080064
MOLM13	Cytotoxicity assay		4 days		Cytotoxicity against human MOLM13 cells harboring MLL1 fusion gene assessed as growth inhibition after 4 days by CellTiter-Glo luminescent assay, IC50 = 0.228 μM.	26080064
Rosetta2 DE3	Function assay		30 mins		Inhibition of FAM-labeled ZBA248 binding to recombinant human N-terminal His6-tagged BRD4 bromodomain 1 (44 to 168 residues) expressed in Rosetta2 DE3 cells after 30 mins by Flourescence polarization assay, IC50 = 0.0317 μM.	28463487
MV4-11	Growth inhibition assay		4 days		Growth inhibition of human MV4-11 cells after 4 days by WST-8 assay, IC50 = 0.162 μM.	28463487
Rosetta2 DE3	Function assay		30 mins		Inhibition of FAM-labeled ZBA248 binding to recombinant human N-terminal His6-tagged BRD4 bromodomain 2 (333 to 460 residues) expressed in Rosetta2 DE3 cells after 30 mins by Flourescence polarization assay, IC50 = 0.226 μM.	28463487
MOLM13	Growth inhibition assay		4 days		Growth inhibition of human MOLM13 cells after 4 days by WST-8 assay, IC50 = 0.228 μM.	28463487
Rosetta2 DE3	Function assay				Binding affinity to biotinylated BRD3 BD1 (24 to 144 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells by bio-layer interferometry method, Kd = 0.0298 μM.	26080064
Rosetta2 DE3	Function assay				Binding affinity to biotinylated BRD3 BD2 (306 to 417 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells by bio-layer interferometry method, Kd = 0.0405 μM.	26080064
Rosetta2 DE3	Function assay				Binding affinity to biotinylated BRD4 BD1 (44 to 168 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells by bio-layer interferometry method, Kd = 0.0528 μM.	26080064
Rosetta2 DE3	Function assay				Binding affinity to biotinylated BRD2 BD1 (72 to 205 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells by bio-layer interferometry method, Kd = 0.0548 μM.	26080064
Rosetta2 DE3	Function assay				Binding affinity to biotinylated BRD2 BD2 (349 to 460 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells by bio-layer interferometry method, Kd = 0.0703 μM.	26080064
Rosetta2 DE3	Function assay				Binding affinity to biotinylated BRD4 BD2 (333 to 460 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells by bio-layer interferometry method, Kd = 0.215 μM.	26080064
Rosetta2 DE3	Function assay				Binding affinity to biotinylated CREBBP (1043 to 1159 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells by bio-layer interferometry method, Kd = 3.084 μM.	26080064
Rosetta2 DE3	Function assay		30 mins		Displacement of FAM-labeled ZBA248 from BRD3 BD1 (24 to 144 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells after 30 mins by fluorescence polarization assay, Ki = 0.0072 μM.	26080064
Rosetta2 DE3	Function assay		30 mins		Displacement of FAM-labeled ZBA248 from BRD4 BD1 (44 to 168 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells after 30 mins by fluorescence polarization assay, Ki = 0.009 μM.	26080064
Rosetta2 DE3	Function assay		30 mins		Displacement of FAM-labeled ZBA248 from BRD2 BD1 (72 to 205 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells after 30 mins by fluorescence polarization assay, Ki = 0.009 μM.	26080064
Rosetta2 DE3	Function assay		30 mins		Displacement of FAM-labeled ZBA248 from BRD3 BD2 (306 to 417 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells after 30 mins by fluorescence polarization assay, Ki = 0.0223 μM.	26080064
Rosetta2 DE3	Function assay		30 mins		Displacement of FAM-labeled ZBA248 from BRD2 BD2 (349 to 460 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells after 30 mins by fluorescence polarization assay, Ki = 0.0496 μM.	26080064
Rosetta2 DE3	Function assay		30 mins		Displacement of FAM-labeled ZBA248 from BRD4 BD2 (333 to 460 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells after 30 mins by fluorescence polarization assay, Ki = 0.0748 μM.	26080064
Rosetta2 DE3	Function assay		30 mins		Inhibition of FAM-labeled ZBA248 binding to recombinant human N-terminal His6-tagged BRD4 bromodomain 1 (44 to 168 residues) expressed in Rosetta2 DE3 cells after 30 mins by Flourescence polarization assay, Ki = 0.009 μM.	28463487
Rosetta2 DE3	Function assay		30 mins		Inhibition of FAM-labeled ZBA248 binding to recombinant human N-terminal His6-tagged BRD4 bromodomain 2 (333 to 460 residues) expressed in Rosetta2 DE3 cells after 30 mins by Flourescence polarization assay, Ki = 0.0748 μM.	28463487
THP1	Antiinflammatory assay				Antiinflammatory activity in human THP1 cells	22386529
HT-29	Function assay	0.3125 uM to 5 uM	24 hrs		Inhibition of BRD4 in human HT-29 cells assessed as reduction in c-Myc protein expression at 0.3125 uM to 5 uM uM after 24 hrs by Western blotting method	25559428
MV4-11	Function assay				Inhibition of BRD4 in human MV4-11 cells assessed as downregulation of BCL2 RNA expression by RNA-seq analysis	29259751
MV4-11	Function assay				Inhibition of BRD4 in human MV4-11 cells assessed as downregulation of cMYC RNA expression by RNA-seq analysis	29259751
U-2 OS	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells	29435139
A673	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
DAOY	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	29435139
BT-37	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	29435139
RD	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
SK-N-SH	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH 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
MG 63 (6-TG R)	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	29435139
NB1643	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 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
fibroblast cells	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells	29435139
Rh41	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	29435139
Rh30	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 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
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
Rh18	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells	29435139
클릭하여 더 많은 세포주 실험 데이터 보기

화학 정보, 보관 및 안정성

분자량	415.44	화학식	C₂₃H₂₁N₅O₃	보관 (수령일로부터)	3년-20°C분말
CAS 번호	1300031-49-5	SDF 다운로드		원액 보관	1년-80°C용매에 보관 1개월-20°C용매에 보관
동의어	N/A			Smiles	CC1=C(C(=NO1)C)C2=C(C=C3C(=C2)N=CC4=C3N(C(=O)N4)C(C)C5=CC=CC=N5)OC

용해도

In vitro
배치:

DMSO : 83 mg/mL (199.78 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 83 mg/mL

Water : Insoluble

DMSO : 83 mg/mL (199.78 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 27 mg/mL

Water : Insoluble

Ethanol : 44 mg/mL

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

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.
Clear solution	5%DMSO 1 Corn oil Selleck 연구소에서 검증되었습니다. 이 제형에 대한 조정이 필요한 경우 맞춤 테스트를 위해 당사 영업팀에 문의하십시오.	4.500mg/ml (10.83mM)	Taking the 1 mL working solution as an example, add 50 μL of 90 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
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

특징	Optimized to retain excellent BET target potency and selectivity while enhancing the in vivo pharmacokinetics and terminal half-life to enable prolonged in vivo studies.
Targets/IC₅₀/Ki	BRD3 (Cell-free assay) 0.25 μM BRD2 (Cell-free assay) 0.5 μM BRD4 (Cell-free assay) 0.79 μM
시험관 내(In vitro)	I-BET151 (GSK1210151A)은 COX-2, P450, Aurora B, GSK3β, PI3K-γ, GPCR, 이온 채널 및 수송체와 같은 광범위한 다양한 단백질 유형에 대해 강력한 선택성을 나타냅니다. I-BET762 (GSK525762A)와 유사하게, BRD2, BRD3 및 BRD4에 대해 0.02-0.1 μM의 K_D를 갖는 강력한 결합 친화도를 나타내며, 사람 말초 혈액 단핵 세포 (PBMC) 및 전혈 (WB)은 물론 쥐 WB에서 지질다당류 자극 IL-6 사이토카인 생성을 각각 0.16 μM, 1.26 μM 및 1.26 μM의 IC50으로 유의하게 억제합니다. 이 화합물 (0.5 또는 5 μM)은 BET (BRD2, BRD3, BRD4 및 BRD9)의 결합을 억제하지만 HL60 핵 추출물에서 23개의 다른 브로모도메인 단백질이 아세틸화된 히스톤 펩타이드에 결합하는 것을 억제하지 않습니다. MV4;11, RS4;11, MOLM13 및 NOMO1 세포와 같은 다양한 MLL 융합을 포함하는 세포주에 대해 15-192 nM의 IC50으로 강력한 효능을 가집니다. 일관되게, MLL 융합 유도 백혈병 (MOLM13)의 콜로니 형성 능력을 완전히 제거하지만 티로신 키나제 활성화 유도 백혈병 (K562)은 제거하지 않습니다. I-BET151은 또한 MLL-ENL 또는 MLL-AF9으로 형질전환된 1차 마우스 전구체를 사용하는 액체 배양 및 클론형성 분석 모두에서 강력한 효능을 나타냅니다. 이 화합물로 처리하면 다른 MLL 융합 (MLL-AF9 및 MLL-AF4를 각각 포함하는 MOLM13 및 MV4;11)에 의해 유도되는 MLL 융합 세포주에서 현저한 G0/G1 정지 및 세포자멸사를 유의하게 유도하지만 K562 세포에서는 그렇지 않습니다. 이는 BRD3/4, PAFc 및 SEC 구성 요소의 전사 시작 부위 (TSS)로의 모집을 차단하여 BCL2, C-MYC 및 CDK6의 전사를 억제하기 때문일 가능성이 높습니다.
키나아제 분석	형광 이방성 (FP) 리간드 변위 분석
키나아제 분석	모든 구성 요소는 50mM HEPES pH 7.4, 150mM NaCl, 0.5mM CHAPS 조성의 버퍼에 용해되며, 최종 농도는 BRD 2/3/4 75nM, 형광 리간드 5nM입니다. 이 반응 혼합물 10 μL를 마이크로 멀티드롭을 사용하여 Greiner 384웰 블랙 저용량 마이크로타이터 플레이트에 있는 다양한 농도의 I-BET151 (GSK1210151A) 또는 DMSO 용매 (최종 1%)를 포함하는 웰에 추가하고, 실온에서 60분 동안 어두운 곳에서 평형화시킵니다. 형광 이방성은 Envision (lex = 485 nm, lEM = 530 nm; Dichroic = 505 nM)에서 판독됩니다.
생체 내(In vivo)	I-BET151 (GSK1210151A)은 30 mg/kg/일로 투여했을 때 마우스에서 murine MLL-AF9 및 human MLL-AF4 백혈병의 종양 성장을 유의하게 억제하고 현저한 생존 이점을 제공합니다.
참조	[1] https://pubmed.ncbi.nlm.nih.gov/21964340/

적용 분야

방법	바이오마커	이미지	PMID
Western blot	α-SMA / Fibronectin / Collagen-1 FoxM1 / AURKB / Survivin / cyclin B / PLK1 HP1α / HP1β / HP1γ		27732564

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):