货号:A135851
同义名:
Dual LCK/SRC inhibitor; KIN001-112
WH-4-023是一种选择性的 Lck/Src 激酶抑制剂,其IC50值分别为 2 nM 和 6 nM,抑制 p38α 和 KDR的效果稍弱。此外,它还可有效抑制SIK,IC50分别为10、22、60 nM。


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| 产品名称 | Fyn ↓ ↑ | Lck ↓ ↑ | Lyn ↓ ↑ | Src ↓ ↑ | Yes ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Saracatinib |
++
Fyn, IC50: 10 nM |
++++
LCK, IC50: <4 nM |
+++
Lyn, IC50: 5 nM |
++++
c-Src, IC50: 2.7 nM |
99%+ | ||||||||||||||
| SU6656 |
+
Fyn, IC50: 170 nM |
+
Lyn, IC50: 130 nM |
+
Src, IC50: 280 nM |
++
YES, IC50: 20 nM |
98% | ||||||||||||||
| PP1 |
+++
Fyn, IC50: 6 nM |
+++
LCK, IC50: 5 nM |
EGFR | 99%+ | |||||||||||||||
| PP2 |
+++
Fyn, IC50: 5 nM |
++++
LCK, IC50: 4 nM |
98% | ||||||||||||||||
| WH-4-023 |
++++
Lck, IC50: 2 nM |
+++
Src, IC50: 6 nM |
99%+ | ||||||||||||||||
| NVP-BHG 712 |
+
c-Src, IC50: 1.266 μM |
99%+ | |||||||||||||||||
| CCT196969 |
++
LCK, IC50: 0.02 μM |
+
Src, IC50: 0.03 μM |
98% | ||||||||||||||||
| MNS |
+
Src, IC50: 29.3 μM |
p97,Syk | 98% | ||||||||||||||||
| Tirbanibulin |
++
Src (HuH7), GI50: 13 nM Src (Hep 3B), GI50: 26 nM |
99%+ | |||||||||||||||||
| PP121 |
++
Src, IC50: 14 nM |
VEGFR,PDGFR | 99%+ | ||||||||||||||||
| Bosutinib |
++++
Src, IC50: 1.2 nM |
99% | |||||||||||||||||
| Dasatinib monohydrate |
++++
Src, IC50: 0.8 nM |
98% | |||||||||||||||||
| Quercetin | ✔ | PKC,Sirtuin | 95% | ||||||||||||||||
| Dasatinib |
++++
Src, IC50: 0.8 nM |
98% | |||||||||||||||||
| Repotrectinib |
+++
Src, IC50: 5.3 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。 | |||||||||||||||||||
| 靶点 |
|
| 描述 | WH-4-023 demonstrates comparable potency enhancement on Lck to that of 2-substituted variants[1]. |
| 体外研究 | WH-4-023 demonstrates comparable potency enhancement on Lck to that of 2-substituted variants[1]. |
| Concentration | Treated Time | Description | References | |
| Human cardiac fibroblasts | 5, 10, 20 µM | 72 hours | WH-4-023 significantly reduced the expression of procollagen I, F-actin, and αSMA in a TGFβ signaling context. | Proc Natl Acad Sci U S A. 2024 Jan 30;121(5):e2303513121. |
| Porcine embryonic stem cells | 0.3 µM | The addition of WH-4-023 significantly enhanced the self-renewal capacity and single-cell clonal efficiency of porcine embryonic stem cells, upregulating proliferation-related genes and downregulating EMT-related genes. | Stem Cell Res Ther. 2024 Aug 7;15(1):245. |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
1.76mL 0.35mL 0.18mL |
8.79mL 1.76mL 0.88mL |
17.58mL 3.52mL 1.76mL |
|
| CAS号 | 837422-57-8 |
| 分子式 | C32H36N6O4 |
| 分子量 | 568.67 |
| SMILES Code | O=C(OC1=C(C)C=CC=C1C)N(C2=CC=C(OC)C=C2OC)C3=NC(NC4=CC=C(N5CCN(C)CC5)C=C4)=NC=C3 |
| MDL No. | MFCD28138072 |
| 别名 | Dual LCK/SRC inhibitor; KIN001-112; KIN112 |
| 运输 | 蓝冰 |
| InChI Key | NBTNHSGBRGTFJS-UHFFFAOYSA-N |
| Pubchem ID | 11844351 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C |
| 溶解方案 |
DMSO: 25 mg/mL(43.96 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 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
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