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My CartCAS：837422-57-8
Storage：Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：White to off-white Solid
Qty：
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| CAS | 837422-57-8 |
| Name | WH-4-023 |
| Molecular Formula | C32H36N6O4 |
| Molecular Weight | 568.67 |
| Solubility | Soluble in DMSO |
| Purity | ≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD28138072 |
| SMILES | 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 |
| Target Point | LCK;Src |
| Passage | Protein Tyrosine Kinase/RTK |
| Background | WH-4-023 is a potent and selective Lck/Src inhibitor. |
| Biological Activity | WH-4-023 是一种有效的选择性的 Lck/Src 抑制剂，IC50 分别为 2 nM/6 nM，对p38α 和 KDR作用效果稍弱。[1] |
| In Vitro | WH-4-023对p38 和 KDR显示出低活性。[1] |
| Cell Experiment | 该测定的目的是测试T细胞受体(TCR; CD3)和CD28信号传导途径抑制剂在人T细胞中的效力。从人外周血淋巴细胞(hPBL)中纯化T细胞，并在用96孔组织培养板(1×105T细胞/孔)中的抗CD3和抗CD28抗体的组合刺激之前用或不用化合物预孵育。)。将细胞在37℃，5％CO 2中培养约20小时，然后通过细胞因子ELISA定量上清液中分泌的IL-2。然后将保留在孔中的细胞用3H-胸苷脉冲过夜以评估T细胞增殖反应。将细胞收获到玻璃纤维滤器上，并通过液体闪烁计数器分析3H-胸苷掺入DNA中。出于比较目的，佛波醇肉豆蔻酸(PMA)和钙离子载体组合使用以诱导纯化的T细胞分泌IL-2。如上文针对抗CD3和-CD28抗体所述，测试潜在的抑制剂化合物对该反应的抑制。人体全血抗CD3/CD28诱导的IL-2分泌测定以与上述类似的方式进行，使用来自在刺激前在组织培养基中稀释50％的正常志愿者的全血[1]。 |
| Kinase Experiment | Lck HTRF激酶测定涉及在存在或不存在抑制剂化合物的情况下生物素化的胃泌素底物肽的ATP依赖性磷酸化。胃泌素的最终浓度为1.2μM。 ATP的最终浓度为0.5μM(Km app = 0.6±0.1μM)，并且Lck的最终浓度(GST-激酶结构域融合(AA 225-509))为250pM。缓冲条件如下：50mM HEPES pH = 7.5，50mM NaCl，20mM MgCl 2，5mM MnCl 2，2mM DTT，0.05％BSA。淬灭测定并用160μL检测试剂终止。检测试剂如下：由50mM Tris，pH = 7.5，100mM NaCl，3mM EDTA，0.05％BSA，0.1％Tween20制成的缓冲液。在阅读之前，链霉抗生物素蛋白别藻蓝蛋白(SA-APC)以0.0004mg/mL的测定中的最终浓度加入，以及最终浓度为0.025nM的欧洲化的抗磷酸酪氨酸Ab(Eu-抗-PY)。在Discovery荧光板读数器中读取测定板，激发波长为320nm，发射波长为615和655nm [1]。 |
| Data Literature Source | [1]. Martin MW，et al. Novel 2-aminopyrimidine carbamates as potent and orally active inhibitors of Lck: synthesis，SAR，and in vivo antiinflammatory activity. J Med Chem. 2006 Aug 10;49(16):4981-91 |
| Unit | Bottle |
| Specification | 5mg 10mg 20mg |
WH-4-023 是一种有效的选择性的 Lck/Src 抑制剂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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