质量水平
检测方案
≥98% (HPLC)
形式
powder
颜色
white to beige
溶解性
DMSO: 20 mg/mL, clear
储存温度
−20°C
SMILES字符串
CN1CCN(C2=CC=C(NC3=NC=CC(N(C4=CC=C(OC)C=C4OC)C(OC5=C(C)C=CC=C5C)=O)=N3)C=C2)CC1
InChI
1S/C32H36N6O4/c1-22-7-6-8-23(2)30(22)42-32(39)38(27-14-13-26(40-4)21-28(27)41-5)29-15-16-33-31(35-29)34-24-9-11-25(12-10-24)37-19-17-36(3)18-20-37/h6-16,21H,17-20H2,1-5H3,(H,33,34,35)
InChI key
NBTNHSGBRGTFJS-UHFFFAOYSA-N
生化/生理作用
WH-4-023 (KIN112) is a potent and selective inihbitor of the tyrosine kinases Lck and Src with IC50 values of 2 nM for Lck and 6 nM for Src. WH-4-023 is a somewhat less potent inhibitor of salt-inducible kinases (SIKs) with IC50 values of 10, 22 and 60 nM for SIK 1, 2 and 3 respectively. WH-4-023 was found to support self-renewal of naive human embryonic stem cells, in particular in combination with PD 0325901 (PZ0162), CHIR99021 (SML1046), and SB-590885 (SML0501).
WH-4-023 belongs to the Src kinase family. It stimulates apoptosis in GC-resistant T-acute lymphoblastic leukemia (T-ALL) cells.
其他说明
WH-4-023 has been expertly reviewed and recommended by the Chemical Probes Portal. For more information, please visit the WH-4-023 probe summary on the Chemical Probes Portal website.
警示用语：
Danger
危险声明
危险分类
Acute Tox. 3 Oral
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
Glucocorticoid resistance is reverted by LCK inhibition in pediatric T-cell acute lymphoblastic leukemia
Serafin, et al.
Blood, blood-b2017 (2017)
Glucocorticoid resistance is reverted by LCK inhibition in pediatric T-cell acute lymphoblastic leukemia
Serafin, et al.
Blood, blood-b2017 (2017)
Targeting loss of the Hippo signaling pathway in NF2-deficient papillary kidney cancers
Sourbier, et al.
Oncotarget, 9(12), 10723-10723 (2018)
Cheong-Yong Yun et al.
Theranostics, 9(3), 646-660 (2019-02-28)
Rationale: SOX10 (SRY-related HMG-box 10) and MITF-M (microphthalmia-associated transcription factor M) restrict the expression of melanogenic genes, such as TYR (tyrosinase), in melanocytes. DACE (diacetylcaffeic acid cyclohexyl ester) inhibits melanin production in α-MSH (α-melanocyte stimulating hormone)-activated B16-F0 melanoma cells. In
商品
Naive pluripotent stem cells cultured in vitro using specialized media and inhibitors mimic "ground-state" cells from blastocysts.
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