SJ1008030

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SJ1008030

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

SJ1008030 (compound 8) 是一种JAK2 PROTAC选择性地降解JAK2。SJ1008030 对 MHH–CALL-4 细胞系的EC₅₀值为 5.4 nM，IC₅₀值为 32.09 nM。SJ1008030 可用于白血病的研究。

生物活性

SJ1008030 (compound 8) is aJAK2PROTACwhich selectively degradesJAK2. SJ1008030 inhibits MHH–CALL-4 cells with anEC₅₀of 5.4 nM and anIC₅₀of 32.09 nM. SJ1008030 can be used for the research of leukemia^[1].

IC₅₀& Target

IC50: 32.09 nM (MHH-CALL-4), 33.41 nM (MHH-CALL4-GSPT1-WT), 33.55 nM (MHH-CALL-4-GSPT1-G575N)^[1]

体外研究
(In Vitro)

SJ1008030 (compound 8) (0-3 μM; 72 h) shows activity in CRLF2r cell lines^[1].
SJ1008030 (compound 8) (0-4.3 μM; 72 h) shows cytotoxicity to MHH–CALL-4 cells^[1].
SJ1008030 (compound 8) (0-10000 nM; 24 h) inhibits the JAK-STAT signaling pathway in xenograft SJBALL021415 bone marrow cells^[1].

Cell Cytotoxicity Assay^[1]

Cell Line:	The CRLF2r cell lines MHH–CALL-4, KOPN49, MHH–CALL-2, KOP N75, NALM-6 and 697
Concentration:	0-3 μM
Incubation Time:	72 hours
Result:	Showed best activity in MHH–CALL-4 cells with an EC₅₀value of 5.4 nM.

Western Blot Analysis^[1]

Cell Line:	MHH–CALL-4 cells
Concentration:	1 nM, 10 nM, 100 nM, 1 μM and 4.3 μM
Incubation Time:	72 hours
Result:	Significantly degradated JAK2 in MHH–CALL-4 cells dose-dependently while showed weakly effect to JAK1, JAK3 and GSPT1.

Western Blot Analysis^[1]

Cell Line:	Xenograft SJBALL021415 bone marrow cells
Concentration:	1, 10, 100, 1000 and 1000 nM
Incubation Time:	24 hours
Result:	Near-completely degradated JAK2 in a dose-dependent way while showed no effect on GSPT1.

分子量

873.94

Formula

C₄₂H₄₃N₁₃O₇S

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.