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NHWD-870

货号:A1549806

NHWD-870 is a potent and selective BET inhibitor that targets the bromodomains of BRD2/3/4 with IC50 values of 2.7nM, as well as BRDT.

NHWD-870 化学结构 CAS号:2115742-03-3
NHWD-870 化学结构
CAS号:2115742-03-3
NHWD-870 3D分子结构
CAS号:2115742-03-3
NHWD-870 化学结构 CAS号:2115742-03-3
NHWD-870 3D分子结构 CAS号:2115742-03-3
规格 价格 库存 数量
50μL*10mM(DMSO) ¥379 咨询
100μL*10mM(DMSO) ¥639 咨询
250μL*10mM(DMSO) ¥1269 咨询
500μL*10mM(DMSO) ¥2079 咨询
10mM*1mL(DMSO) ¥3104 咨询
1mg ¥945 咨询
5mg ¥2583 咨询
10mg ¥4391 咨询
25mg ¥9134 咨询
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NHWD-870 纯度/质量文件 产品仅供科研

货号:A1549806 标准纯度:
批次查询: 批次纯度:

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产品名称 HIV Protease HIV-1 caspid 其他靶点 纯度
Dextran sulfate sodium, mw 40,000 M.W 40000
Vicriviroc maleate 95%
Rosamultin 97%
Darunavir 98%
Lopinavir ++++

HIV protease, Ki: 1.3 pM

99+%
Chloroquine Autophagy 95%
Amprenavir +

HIV protease, IC50: 14.6 ng/mL

PXR 99%+
NBD-556 99%+
Nelfinavir Mesylate +++

HIV protease, Ki: 2 nM

99%+
Atazanavir Sulfate 98%
Limonin 98%
Saquinavir ++

HIV proteinase, IC50: 2.7 nM

98%
Ritonavir 98%
Azvudine 98%
Lenacapavir ++++

HIV-1 capsid, EC50: 0.1 nM

97%
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。
产品名称 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

98+%
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 (1), IC50: 77 nM

BRD4 (2), IC50: 33 nM

98%
I-BET151 +

BRD4, IC50: 0.5 μM

BRD3, IC50: 0.25 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

97%
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 ++++

BRD9, Kd: 5.9 nM

BRD7, Kd: 73 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 ++++

Brd3(BD2), Kd: 13 nM

Brd2(BD2), Kd: 62 nM

99%+
dBET57 +

BRD4BD1, DC50: 500 nM

99%+
SF2523 +

BRD4, IC50: 241 nM

DNA-PK 99%+
INCB054329 ++++

BRD3-BD1, IC50: 9 nM

BRD4-BD1, IC50: 119 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 95%
ODM-207 98%
GSK778 +++

BRD4-BD1, IC50: 143 nM

BRD2-BD1, IC50: 75nM

97%
SRX3207 +

BRD42, IC50: 3070 nM

BRD41, IC50: 3070 nM

Syk 98%
GSK046 +++

BRD3BD2, IC50: 98 nM

BRD4BD2, IC50: 214 nM

98%
GSK620 97%
Thalidomide-NH-C4-NH-Boc 98%
Trotabresib 99%
NHWD-870 98%
CFT8634 ++++

BRD9, DC50: 3 nM

99%
GSK2801 ++

BAZ2A, Kd: 257 nM

BAZ2B, Kd: 136 nM

99%+
KG-501 99%+
UNC 669 +

L3MBTL4, IC50: 6 μM

L3MBTL3, IC50: 35 μM

99%
PFI-3 +++

SMARCA2A, Kd: 72 nM

SMARCA4, Kd: 55 nM

99%+
UNC1215 +++

L3MBTL3, IC50: 120 nM

L3MBTL3- D274A, IC50: 3.5 μM

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

99%
I-CBP112 ++

CBP, Kd: 151 nM

p300, Kd: 167 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 HER2,IGF-1R 99%+
Curcumin +

p300, IC50: ~25 μM

Ferroptosis,NF-κB,Nrf2 98%
PF-CBP1 HCl ++

p300/CBP, IC50: 363nM

CREBBP, IC50: 125nM

97%
CPI-637 +++

CBP, IC50: 0.03 μM

EP300, IC50: 0.051 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

99%
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。

NHWD-870 生物活性

靶点
  • BET

描述 NHWD-870 is a potent and selective BET inhibitor that targets the bromodomains of BRD2/3/4 with IC50 values of 2.7nM, as well as BRDT. It has multiple anti-tumor effects, including the inhibition of tumor cell proliferation, c-MYC expression, and BRD4 phosphorylation, as well as the induction of apoptosis. It also blocks the proliferation of tumor associated macrophages (TAMs) by suppressing the expression and secretion of CSF1 from tumor cells. The inhibition of CSF1 is mediated by the downregulation of BRD4 and its target HIF1α. NHWD-870 shows potent activity against A375 cells with an IC50 value of 2.46nM. It also exhibits oral bioavailability and strong anti-tumor efficacy in mouse models bearing various tumor types, such as NCI-H526, A2780, A375, B16F10, and TMD-8 cells, at doses of 0.75-3 mg/kg[1].

NHWD-870 参考文献

[1]Yin M, Guo Y, Hu R, Cai WL, Li Y, Pei S, Sun H, Peng C, Li J, Ye R, Yang Q, Wang N, Tao Y, Chen X, Yan Q. Potent BRD4 inhibitor suppresses cancer cell-macrophage interaction. Nat Commun. 2020 Apr 14;11(1):1833. doi: 10.1038/s41467-020-15290-0. PMID: 32286255; PMCID: PMC7156724.

NHWD-870 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.03mL

0.41mL

0.20mL

10.17mL

2.03mL

1.02mL

20.34mL

4.07mL

2.03mL

NHWD-870 技术信息

CAS号2115742-03-3
分子式C29H29N7O
分子量 491.587
别名
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry,Room Temperature

溶解方案

DMSO: 60 mg/mL(122.05 mM),配合低频超声,并水浴加热至45℃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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案一
方案二
动物实验配方
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