表观遗传阅读框 | Epigenetic Reader Domain

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Epigenetic Reader Domain 亚型比较

全部(466) Inhibitor(35)

货号			产品名	纯度
A1147976	现货	促	(+)-JQ1 PA (+)-JQ1 PA is a warhead ligand with an alkinyl group for conjugation reactions of PROTAC targeting on BET.	98%
A1483444	现货	促	XX-650-23 XX-650-23是一种有效的CREB抑制剂，通过破坏CBP-CREB的相互作用来抑制CREB功能，适用于AML的研究。	98%
A1921215	现货	促	WDR5-0102 WDR5-0102是一种靶向 WDR5-MLL1 相互作用的抑制剂，具有选择性抑制 MLL1 HMT 活性，K_d 值为 4 μM，而不会影响 H3K4 甲基转移酶 SETD7 及其他 HMTs（如 G9a、EHMT1 等）的活性。	99%+
A530203	现货	促	GSK8573 GSK8573是 GSK2801 的无活性对照化合物。GSK8573 对 BRD9 具有结合活性 (Kd = 1.04 μM)，但对 BAZ2A/B 和其他溴结构域家族无活性，适用于作为结构相关的阴性对照化合物，用于生物实验的对照研究。	97%
A1177069	现货	促	BRM/BRG1 ATP Inhibitor-1 BRM/BRG1 ATP Inhibitor-1是一种口服有效的变构抑制剂，靶向 Brahma 同系物 (BRM)/SMARCA2 和 BRG1/SMARCA4 的 ATP 酶活性。该化合物在癌症研究中展示出显著的抗癌潜力。	97%
A2305170	现货	促	Bleximenib oxalate Bleximenib (Menin-MLL inhibitor 24) oxalate 是一种 Menin-mixed-lineage leukemia 1 (menin-MLL) 抑制剂，可用于癌症研究。	98%
A761249	现货	促	MI-2-2 MI-2-2是一种高效的 menin-MLL 蛋白相互作用抑制剂，具有低纳摩尔亲和力 (Kd=22 nM)，能够特异性破坏 menin 和 MLL 之间的相互作用。在 MLL 白血病细胞中具有显著的抗增殖作用，常用于白血病及相关基因表达调控的研究。	95%
A1218626	现货	促	BET bromodomain inhibitor 3 BET bromodomain inhibitor 3是一种 BET 溴结构域抑制剂，Ki 值大于 40 µM，主要用于避孕、癌症和心血管疾病的研究。	99%+
A1365245	现货	促	BRD7-IN-1 BRD7-IN-1 是 BI7273 (BRD7/9 抑制剂) 的一种改良衍生物，通过与 VHL 配体连接形成 PROTAC VZ185。VZ185 对 BRD7 和 BRD9 的 DC50 值分别为 4.5 nM 和 1.8 nM。	99%+
A1177083	现货	促	MS402 MS402 is a domain-selective inhibitor of BRD4-BD1 with Ki value of 77nM, over BRD4-BD2.	99%+
A365466	现货	促	UNC1079 UNC1079 is the piperidine analog of UNC1021, as a structurally similar but significantly less potent inhibitor for use as a negative control in cellular studies.	98%+
A449341	现货	促	dTRIM24 dTRIM24 是一种强效且选择性的 PROTAC，靶向 TRIM24，而 TRIM24 被认为是许多癌症中的依赖因子，dTRIM24 将 TRIM24 配体 IACS-9571 与 VHL 配体结合。	98%
A1365567	现货	促	Revumenib Revumenib (SNDX-5613) 是一种有效且特异的 Menin-MLL 抑制剂，结合 Ki 为 0.149 nM。在细胞实验中，Revumenib 以 IC50 为 10-20 nM 抑制 Menin-MLL。Revumenib 可用于 MLL 基因重排的急性白血病研究，包括急性淋巴细胞白血病 (ALL) 和急性髓细胞白血病 (AML)。	99%+
A104099	现货	促	Bromosporine Bromosporine inhibits various bromodomains including BRD2, BRD4, BRD9 and CECR2 with IC50s of 0.41 μM, 0.29 μM, 0.122 μM and 0.017 μM respectively.	99%+
A118771	现货	促	(R)-(-)-JQ1 Enantiomer (R)-(-)-JQ1 enantiomer, the stereoisomer(+)-JQ1, showed no significant interaction with any bromodomain. (+)-JQ1 is an inhibitor for the BET which targets the BET bromodomain. The (R)-(-)-JQ1 enantiomer stereoisomer has no appreciable affinity to BET bromodomains, whereas S-enantiomer pure (+)-JQ1 binds to BRD4 bromodomains 1 and 2 with Kd values of ~ 50 and 90 nM, respectively.	99%+
A114568	现货	促	GSK126 GSK126 is a potent, highly selective EZH2 methyltransferase inhibitor with IC50 of 9.9 nM, > 1000-fold selective for EZH2 over 20 other human methyltransferases.	99%+
A728121	现货	促	MG 149 MG149 is a potent histone acetyltransferase inhibitor with IC50 of 74 μM and 47 μM for Tip60 and MOF,respectively.	99%+
A961925	现货	促	NVS-CECR2-1 NVS-CECR2-1 is a potent and selective CECR2 (cat eye syndrome chromosome region, candidate 2) inhibitor with IC50 of 47 nM.	98%
A806747	现货	促	CeMMEC1 CeMMEC1 is an N-methylisoquinolinone that inhibits the second bromodomain of TAF1 with Kd of 1.8 µM and IC50 of 0.9 µM.	98%
A1147982	现货	促	A1874 A1874 is a nutlin-based PROTAC targeting on BRD4, consist of a BRD4-ligand JQ1 linked to a MDM2 E3 ligase ligand RG7388.	99%+

产品名	BET ↓ ↑	bromodomain ↓ ↑	BRPF ↓ ↑	CBP/beta-catenin ↓ ↑	p300/CBP ↓ ↑	其他靶点	纯度
MS436	++ BRD4 (1), Ki: <0.085 μM BRD4 (2), Ki: 0.34 μM						99%+
CPI-203	+++ BRD4, IC50: 37 nM						99+%
GSK1324726A	+++ BRD2, IC50: 31 nM BRD4, IC50: 22 nM						99%+
PFI-1	++ BRD2, IC50: 98 nM BRD4, IC50: 0.22 μM						98%
Apabetalone	+ BD2, IC50: 0.51 μM						99%
(+)-JQ1	+++ BRD4 (2), IC50: 33 nM BRD4 (1), IC50: 77 nM						98%
I-BET151	+ BRD3, IC50: 0.25 μM BRD4, IC50: 0.5 μM						98%
Molibresib	+++ BET proteins, IC50: 35 nM						99%+
I-BRD9	+++ BRD9, pIC50: 7.3 BRD4, pIC50: 5.3						99%+
BI-7273	++++ BRD7, IC50: 117 nM BRD9, IC50: 19 nM						99+%
Pelabresib	+++ BRD4-BD1, IC50: 39 nM						98%
ARV-825	+++ BRD4 BD1, Kd: 90 nM BRD4 BD2, Kd: 28 nM						99%+
Birabresib							99%+
BI 2536	+++ BRD4, Kd: 37 nM					c-Myc	99%+
Bromosporine	++ BRD2, IC50: 0.29 μM BRD9, IC50: 0.122 μM	++++ CECR2, IC50: 17 nM					99%+
XMD8-92	++ BRD4 (1), Kd: 170 nM						99%+
Mivebresib	✔						99%+
BI-9564	++++ BRD7, Kd: 73 nM BRD9, Kd: 5.9 nM	++ CECR2, Kd: 77 nM					98%
AZD5153 6-Hydroxy-2-naphthoic acid	++++ FL-BRD4, IC50: 5 nM						99%+
PLX51107	++++ BRD3 BD1, Kd: 2.1 nM BRD4 BD2, Kd: 1.7 nM						99%+
FL-411	+ BRD4(1), IC50: 0.43 μM						99%+
ABBV-744	✔						99%+
dBET6	++++ BRD4, IC50: 14 nM						99%+
dBET1	++++ BRD4, IC50: 20 nM						99%+
MZ1	++++ Brd2(BD2), Kd: 62 nM Brd3(BD2), Kd: 13 nM						99%+
dBET57	+ BRD4_BD1, DC50: 500 nM						99%+
SF2523	+ BRD4, IC50: 241 nM					DNA-PK	99%+
INCB054329	++++ BRD4-BD1, IC50: 119 nM BRD3-BD1, IC50: 9 nM						99%
INCB-057643	✔						99%+
(E/Z)-ZL0420	+++ BRD4 BD2, IC50: 32 nM BRD4 BD1, IC50: 27 nM						99%+
BMS-986158	✔						99%+
BRD4 Inhibitor-10	++++ BRD4-BD2, IC50: 41 nM BRD4-BD1, IC50: 5 nM						97%
A1874	✔						99%+
Y06036	++ BRD4 (1), Kd: 82 nM						99%+
Alobresib	✔					NF-κB	98%
ODM-207	✔						99%
GSK778	+++ BRD2-BD1, IC50: 75nM BRD4-BD1, IC50: 143 nM						97%
SRX3207	+ BRD41, IC50: 3070 nM BRD42, IC50: 3070 nM					Syk	98%
GSK046	+++ BRD4_BD2, IC50: 214 nM BRD3_BD2, IC50: 98 nM						98%
GSK620	✔						97%
Thalidomide-NH-C4-NH-Boc	✔						98%
Trotabresib	✔						99%
NHWD-870	✔						98%
CFT8634	++++ BRD9, DC50: 3 nM						98%
GSK2801		++ BAZ2A, Kd: 257 nM BAZ2B, Kd: 136 nM					99%+
KG-501		✔					99%+
UNC 669		+ L3MBTL3, IC50: 35 μM L3MBTL4, IC50: 6 μM					98%
PFI-3		+++ SMARCA4, Kd: 55 nM SMARCA2A, Kd: 72 nM					99%+
UNC1215		+++ L3MBTL3- D274A, IC50: 3.5 μM L3MBTL3, IC50: 120 nM					99%+
EED226		++ PRC2, Kd: 114 nM EED, Kd: 82 nM					99%+
BRD9539		✔					98%
UNC926		+ L3MBTL1, Kd: 3.9 μM					99%
666-15		++ CREB, IC50: 81 nM					99%+
UNC6852		+ EED, IC50: 247 nM					98%
BAZ1A-IN-1		+ BAZ1A, Kd: 0.52 μM					99%+
PFI-4			++ BRPF2, IC50: 7.9 μM BRPF1, IC50: 80 nM				99%+
OF-1			++ BRPF1B, Kd: 100 nM BRPF2, Kd: 500 nM				99%+
GSK-5959			++ BRPF3, pIC50: 7.1 BRPF2, pIC50: 5.2				99%
GSK6853			++++ BRPF1, pIC50: 8.1				99%+
NI-42			++++ BRPF3, IC50: 260 nM BRPF1, IC50: 48 nM				99%+
E-7386				+++ CBP/beta-catenin, IC50: 0.0484 μM			97%
I-CBP112					++ p300, Kd: 167 nM CBP, Kd: 151 nM		98+%
Histone Acetyltransferase Inhibitor II					+ p300, IC50: 5 μM		98%
C646					+ p300/CBP, Ki: 400 nM		99%+
Anacardic Acid					+ PCAF, IC50: 5 μM p300/CBP, IC50: 8.5 μM		99%+
SGC-CBP30					++++ EP300, IC50: 38 nM CREBBP, IC50: 21 nM		99%+
Nordihydroguaiaretic acid					✔	IGF-1R,HER2	99%+
Curcumin					+ p300, IC50: ~25 μM	Nrf2,NF-κB,Ferroptosis	98%
PF-CBP1 HCl					++ CREBBP, IC50: 125nM p300/CBP, IC50: 363nM		97%
CPI-637					+++ EP300, IC50: 0.051 μM CBP, IC50: 0.03 μM		99%+
Foscenvivint					✔	β-catenin	99%+
A-485					++ p300 HAT, IC50: 0.06 μM		99%+
GNE-781	+ BRD4(1), IC50: 5100 nM				++++ CBP, IC50: 0.94 nM		98%
NEO2734	+++ BET, IC50: <30 nM				+++ p300/CBP, IC50: <30 nM		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

表观遗传阅读框 / Epigenetic Reader Domain

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