Syk-IN-6 是脂质与 SH2 结构域相互作用的抑制剂，控制含有 SH2 结构域的激酶的细胞活性。Syk-IN-6 能够阻断Syk激酶活性，与造血恶性肿瘤相关，包括急性髓系白血病(AML)
| 生物活性 | Syk-IN-6 is an inhibitor of the lipid-SH2 domaininteraction, control the cellular activity of kinases containing SH2 domain. Syk-IN-6 blocksSykkinase activity, which associated hematopoietic malignancies, including acute myeloid leukemia (AML)[1]. |
| IC50& Target[1] | |
体外研究
(In Vitro) | Syk-IN-6 (WC36) specifically and potently suppresses oncogenic activities of Syk in AML cell lines and patient-derived AML cells[1].
Syk-IN-6 (5 μM; 16 h) inhibits FcγRI-specific antibody (IgG2)-stimulated phosphorylation of Syk, STAT3/STAT5 and ERK1/2 in naive MV4-11 cells rather not entospletinib-resistant/Syk-deficient MV4-11 cells[1].
Syk-IN-6 (0.01 μM-100 μM; 16 h) inhibits the proliferation of MV4-11 cells, HL-60 and patient-derived AML cells by SykcSH2 dose-dependently[1].
Western Blot Analysis[1] | Cell Line: | Raji B cell, HL-60 cell, naive and entospletinib-resistant MV4-11 cells | | Concentration: | 5 μM, 10 μM | | Incubation Time: | 16 hours | | Result: | Suppressed the phosphorylation and activation of Syk, ERK1/2 and STAT3/5 in entospletinib-resistant MV4-11 cells.
Was potent against phosphorylation of ERK1/2 and STAT3 in HL-60 cells.
Inhibited phosphorylation of Syk, ERK1/2 and STAT3/5 in AML cells from four patients refractory or relapsed following standard AML therapies. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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