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产品名称 | BET ↓ ↑ | bromodomain ↓ ↑ | BRPF ↓ ↑ | CBP/beta-catenin ↓ ↑ | p300/CBP ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
MS436 |
++
BRD4 (2), Ki: 0.34 μM BRD4 (1), Ki: <0.085 μM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
CPI-203 |
+++
BRD4, IC50: 37 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
GSK1324726A |
+++
BRD2, IC50: 31 nM BRD4, IC50: 22 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
PFI-1 |
++
BRD2, IC50: 98 nM BRD4, IC50: 0.22 μM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Apabetalone |
+
BD2, IC50: 0.51 μM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
(+)-JQ1 |
+++
BRD4 (1), IC50: 77 nM BRD4 (2), IC50: 33 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
I-BET151 |
+
BRD3, IC50: 0.25 μM BRD4, IC50: 0.5 μM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Molibresib |
+++
BET proteins, IC50: 35 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
I-BRD9 |
+++
BRD9, pIC50: 7.3 BRD4, pIC50: 5.3 |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
BI-7273 |
++++
BRD7, IC50: 117 nM BRD9, IC50: 19 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Pelabresib |
+++
BRD4-BD1, IC50: 39 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
ARV-825 |
+++
BRD4 BD2, Kd: 28 nM BRD4 BD1, Kd: 90 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Birabresib | {[allProObj[0].p_purity_real_show]} | ||||||||||||||||||
BI 2536 |
+++
BRD4, Kd: 37 nM |
c-Myc | {[allProObj[0].p_purity_real_show]} | ||||||||||||||||
Bromosporine |
++
BRD2, IC50: 0.29 μM BRD9, IC50: 0.122 μM |
++++
CECR2, IC50: 17 nM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||||
XMD8-92 |
++
BRD4 (1), Kd: 170 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Mivebresib | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
BI-9564 |
++++
BRD9, Kd: 5.9 nM BRD7, Kd: 73 nM |
++
CECR2, Kd: 77 nM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||||
AZD5153 6-Hydroxy-2-naphthoic acid |
++++
FL-BRD4, IC50: 5 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
PLX51107 |
++++
BRD4 BD2, Kd: 1.7 nM BRD3 BD1, Kd: 2.1 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
FL-411 |
+
BRD4(1), IC50: 0.43 μM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
ABBV-744 | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
dBET6 |
++++
BRD4, IC50: 14 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
dBET1 |
++++
BRD4, IC50: 20 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
MZ1 |
++++
Brd3(BD2), Kd: 13 nM Brd2(BD2), Kd: 62 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
dBET57 |
+
BRD4BD1, DC50: 500 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
SF2523 |
+
BRD4, IC50: 241 nM |
DNA-PK | {[allProObj[0].p_purity_real_show]} | ||||||||||||||||
INCB054329 |
++++
BRD3-BD1, IC50: 9 nM BRD4-BD1, IC50: 119 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
INCB-057643 | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
(E/Z)-ZL0420 |
+++
BRD4 BD1, IC50: 27 nM BRD4 BD2, IC50: 32 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
BMS-986158 | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
BRD4 Inhibitor-10 |
++++
BRD4-BD2, IC50: 41 nM BRD4-BD1, IC50: 5 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
A1874 | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Y06036 |
++
BRD4 (1), Kd: 82 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Alobresib | ✔ | NF-κB | {[allProObj[0].p_purity_real_show]} | ||||||||||||||||
ODM-207 | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
GSK778 |
+++
BRD2-BD1, IC50: 75nM BRD4-BD1, IC50: 143 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
SRX3207 |
+
BRD41, IC50: 3070 nM BRD42, IC50: 3070 nM |
Syk | {[allProObj[0].p_purity_real_show]} | ||||||||||||||||
GSK046 |
+++
BRD4BD2, IC50: 214 nM BRD3BD2, IC50: 98 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
GSK620 | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Thalidomide-NH-C4-NH-Boc | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Trotabresib | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
NHWD-870 | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
CFT8634 |
++++
BRD9, DC50: 3 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
GSK2801 |
++
BAZ2B, Kd: 136 nM BAZ2A, Kd: 257 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
KG-501 | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
UNC 669 |
+
L3MBTL3, IC50: 35 μM L3MBTL4, IC50: 6 μM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
PFI-3 |
+++
SMARCA2A, Kd: 72 nM SMARCA4, Kd: 55 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
UNC1215 |
+++
L3MBTL3- D274A, IC50: 3.5 μM L3MBTL3, IC50: 120 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
EED226 |
++
PRC2, Kd: 114 nM EED, Kd: 82 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
BRD9539 | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
UNC926 |
+
L3MBTL1, Kd: 3.9 μM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
666-15 |
++
CREB, IC50: 81 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
UNC6852 |
+
EED, IC50: 247 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
BAZ1A-IN-1 |
+
BAZ1A, Kd: 0.52 μM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
PFI-4 |
++
BRPF2, IC50: 7.9 μM BRPF1, IC50: 80 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
OF-1 |
++
BRPF2, Kd: 500 nM BRPF1B, Kd: 100 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
GSK-5959 |
++
BRPF3, pIC50: 7.1 BRPF2, pIC50: 5.2 |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
GSK6853 |
++++
BRPF1, pIC50: 8.1 |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
NI-42 |
++++
BRPF1, IC50: 48 nM BRPF3, IC50: 260 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
E-7386 |
+++
CBP/beta-catenin, IC50: 0.0484 μM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
I-CBP112 |
++
p300, Kd: 167 nM CBP, Kd: 151 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Histone Acetyltransferase Inhibitor II |
+
p300, IC50: 5 μM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
C646 |
+
p300/CBP, Ki: 400 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Anacardic Acid |
+
p300/CBP, IC50: 8.5 μM PCAF, IC50: 5 μM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
SGC-CBP30 |
++++
EP300, IC50: 38 nM CREBBP, IC50: 21 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Nordihydroguaiaretic acid | ✔ | HER2,IGF-1R | {[allProObj[0].p_purity_real_show]} | ||||||||||||||||
Curcumin |
+
p300, IC50: ~25 μM |
Nrf2,Ferroptosis,NF-κB | {[allProObj[0].p_purity_real_show]} | ||||||||||||||||
PF-CBP1 HCl |
++
p300/CBP, IC50: 363nM CREBBP, IC50: 125nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
CPI-637 |
+++
EP300, IC50: 0.051 μM CBP, IC50: 0.03 μM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Foscenvivint | ✔ | β-catenin | {[allProObj[0].p_purity_real_show]} | ||||||||||||||||
A-485 |
++
p300 HAT, IC50: 0.06 μM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
GNE-781 |
+
BRD4(1), IC50: 5100 nM |
++++
CBP, IC50: 0.94 nM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||||
NEO2734 |
+++
BET, IC50: <30 nM |
+++
p300/CBP, IC50: <30 nM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||||
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。 |
描述 | MS402 is a BD1-selective BET BrD inhibitor with Kis of 77 nM, 718 nM, 110 nM, 200 nM, 83 nM, and 240 nM for BRD4(BD1), BRD4(BD2), BRD3(BD1), BRD3(BD2), BRD2(BD1), BRD2(BD2), and BRD2(BD2), respectively. MS402 prevents Th17 cell differentiation and ameliorates colitis in mice[1]. |
Animal study | Reconstruction of Rag1-/- mice with naïve CD4+CD45RBhi cells isolated from spleens and lymph nodes of C57BL/6 mice started to decrease body weights after 4 weeks. The weight loss with MS402 (10 mg/kg; intraperitoneal injections twice a week for 3 weeks) showed a much less decrease in body weight[1] . |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.70mL 0.54mL 0.27mL |
13.48mL 2.70mL 1.35mL |
26.97mL 5.39mL 2.70mL |
CAS号 | 1672684-68-2 |
分子式 | C20H19ClN2O3 |
分子量 | 370.829 |
别名 | |
运输 | 蓝冰 |
存储条件 |
粉末 Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 105 mg/mL(283.15 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |