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  2. Epigenetics Apoptosis
  3. Histone Demethylase Apoptosis
  4. GSK-J4

GSK-J4 是一種有效的 H3K27me3/me2 去甲基化酶 JMJD3/KDM6B 和 UTX/KDM6A 雙抑制劑，IC50 分別為 8.6 μM 和 6.6 μM。GSK-J4 抑制 LPS 誘導(dǎo)的人原代巨噬細胞產(chǎn)生 TNF-α，IC50 值為 9 μM。GSK-J4 是 GSK-J1 的細胞通透性前體。GSK-J4 誘導(dǎo)內(nèi)質(zhì)網(wǎng)應(yīng)激相關(guān)的細胞凋亡 (apoptosis)。

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CAS No. : 1373423-53-0

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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥825
In-stock
5 mg ￥750
In-stock
10 mg ￥1195
In-stock
25 mg ￥2300
In-stock
50 mg ￥3600
In-stock
100 mg ￥4713
In-stock
200 mg 現(xiàn)貨 詢價
500 mg   詢價  
1 g   詢價  

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Customer Review

Other Forms of GSK-J4:

MCE 顧客使用本產(chǎn)品發(fā)表的 55 篇科研文獻

IHC
IF
WB
RT-PCR

    GSK-J4 purchased from MCE. Usage Cited in: Br J Pharmacol. 2023 Sep;180(17):2250-2265.  [Abstract]

    GSK-J4 (50 mg/kg, intraperitoneal injection for 10 days) significantly reduced total collagen deposition in the kidneys of mice with UUO compared with vehicle-treated UUO mice.

    GSK-J4 purchased from MCE. Usage Cited in: Br J Pharmacol. 2023 Sep;180(17):2250-2265.  [Abstract]

    Immunofluorescence staining revealed that GSK-J4 (50 mg/kg, intraperitoneal injection for 10 days) attenuated the upregulation of collagen I and fibronectin in the kidneys of UUO mice.

    GSK-J4 purchased from MCE. Usage Cited in: Br J Pharmacol. 2023 Sep;180(17):2250-2265.  [Abstract]

    Western blot analysis demonstrated that administration of GSK-J4 (50 mg/kg, intraperitoneal injection for 10 days) suppressed collagen I and fibronectin expression in obstructed kidneys.

    GSK-J4 purchased from MCE. Usage Cited in: Cancer Cell Int. 2020 Jun 3;20:209.  [Abstract]

    The mRNA expression level of PKC-α is detected using qRT-PCR. GAPDH is used as an internal control.

    GSK-J4 purchased from MCE. Usage Cited in: Cancer Cell Int. 2020 Jun 3;20:209.  [Abstract]

    After treatment with GSK-J4, the expression levels of PKC-α and p-Bcl2 in KG-1a cells are detected by Western blotting.

    GSK-J4 purchased from MCE. Usage Cited in: J Clin Invest. 2018 Jan 2;128(1):483-499.  [Abstract]

    Immunoblotting for H3K27me3 in cultured mouse podocytes treated with the Jmjd3 and UTX inhibitor GSK-J4 (5 μM for 48 hours) (n=3).

    查看 Histone Demethylase 亞型特異性產(chǎn)品:

    • 生物活性

    • 純度 & 產(chǎn)品資料

    • 參考文獻

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    生物活性

    GSK-J4 is a potent dual inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A with IC50s of 8.6 and 6.6 μM, respectively. GSK-J4 inhibits LPS-induced TNF-α production in human primary macrophages with an IC50 of 9 μM. GSK J4 is a cell permeable proagent of GSK-J1[1][2][3]. GSK-J4 induces endoplasmic reticulum stress-related apoptosis[4].

    IC50 & Target

    KDM6

     

    細胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    A549 IC50
    14.7 μM
    Compound: GSK-J4
    Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
    Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
    		[PMID: 37660833]
    HCT-116 IC50
    1.77 μM
    Compound: GSK-J4
    Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
    Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
    		[PMID: 37660833]
    HT-29 IC50
    14.93 μM
    Compound: GSK-J4
    Antiproliferative activity against human HT-29 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
    Antiproliferative activity against human HT-29 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
    		[PMID: 37660833]
    HeLa IC50
    21.65 μM
    Compound: GSK-J4
    Antiproliferative activity against human HeLa cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
    Antiproliferative activity against human HeLa cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
    		[PMID: 37660833]
    MCF7 IC50
    16.44 μM
    Compound: GSK-J4
    Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
    Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
    		[PMID: 37660833]
    Macrophage IC50
    9 μM
    Compound: Chemical probe: GSK-J4
    Antiinflammatory activity in human primary macrophages assessed as inhibition of LPS-induced TNFalpha production measured after 6 hrs by ELISA
    Antiinflammatory activity in human primary macrophages assessed as inhibition of LPS-induced TNFalpha production measured after 6 hrs by ELISA
    		[PMID: 22842901]
    Macrophage IC50
    9 μM
    Compound: GSK-J4
    Antiinflammatory activity against human primary macrophages assessed as inhibition of LPS-activated TNF-alpha production incubated for 6 hrs by ELISA
    Antiinflammatory activity against human primary macrophages assessed as inhibition of LPS-activated TNF-alpha production incubated for 6 hrs by ELISA
    		[PMID: 25279926]
    SW480 IC50
    1.08 μM
    Compound: GSK-J4
    Antiproliferative activity against human SW480 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
    Antiproliferative activity against human SW480 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
    		[PMID: 37660833]
    T47D IC50
    13.21 μM
    Compound: GSK-J4
    Antiproliferative activity against human T47D cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
    Antiproliferative activity against human T47D cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
    		[PMID: 37660833]
    U-937 IC50
    13.5 μM
    Compound: GSK-J4
    Antiproliferative activity against human U-937 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
    Antiproliferative activity against human U-937 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
    		[PMID: 37660833]
    體外研究
    (In Vitro)

    GSK-J4 has cellular activity in Flag-JMJD3-transfected HeLa cells, in which GSK-J4 prevents the JMJD3-induced loss of nuclear H3K27me3 immunostaining. Administration of GSK-J4 increases total nuclear H3K27me3 levels in untransfected cells. GSK-J4 significantly reduces the expression of 16 of 34 LPS-driven cytokines, including tumour-necrosis factor-α (TNF-α)[1].
    GSK-J4 (5 μM; 48 hours) causes a more than 3-fold increase in mouse podocyte H3K27me3 content. H3K27me3 levels in cultured podocytes, GSK-J4 reduces Jagged-1 mRNA and Jagged-1 protein levels. Correspondingly, when exposed podocytes to the inducer of dedifferentiation TGF-β1, pretreatment with GSK-J4 preventes both the increase in intracellular N1-ICD levels and the increase in α-SMA and the decrease in podocin mRNA levels[2].
    GSK-J4 (10, 25 nM) acts upon DCs promoting the differentiation of Treg cells, improving Treg stability and suppressive capacities, without affecting the differentiation of Th1 and Th17 cells[3].
    GSK-J4 inhibits JMJD3 expression that is induced by TGF-β1[4].
    GSK-J4 inhibits H3K4 demethylation at Xist, Nodal, and HoxC13 in female embryonic stem cells[5].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    體內(nèi)研究
    (In Vivo)

    GSK-J4 Hydrochloride (10 mg/kg; i.p.; thrice-weekly for 10 weeks) attenuates the development of kidney disease in diabetic mice[2].
    GSK-J4 (0.5 mg/kg, i.p.) significantly reduces the severity and delays the onset of the disease of the mouse model of experimental autoimmune encephalomyelitis[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Eight-week-old male db/m and db/db mice[2]
    Dosage: 10 mg/kg
    Administration: i.p.; thrice-weekly for 10 weeks
    Result: Attenuated the development of kidney disease in diabetic mice.
    分子量

    417.50

    Formula

    C24H27N5O2
    CAS 號