2. PROTAC Epigenetics Apoptosis
  3. PROTACs Histone Methyltransferase Apoptosis
  4. PROTAC EZH2 Degrader-9

PROTAC EZH2 Degrader-9 是一种通过泛素-蛋白酶体途径发挥作用的口服有效的 EZH2 PROTAC 降解剂。PROTAC EZH2 Degrader-9 能下调 PRC2 核心亚基并强效抑制 H3K27me3，不影响常见的 CRBN 新底物, 且对 GSPT1 和 IKZF1/3 具有选择性。PROTAC EZH2 Degrader-9 通过诱导细胞周期阻滞和细胞凋亡 (apoptosis) 对多种癌细胞系表现出强效的抗增殖活性。PROTAC EZH2 Degrader-9 能逆转 PRC2 介导的基因沉默，并抑制 EZH2 非催化靶基因的激活。PROTAC EZH2 Degrader-9 可用于白血病、淋巴瘤及非小细胞肺癌的研究。
(粉色: EZH2 配体 (HY-78694)；蓝色: Cereblon 配体 (HY-W087383)；黑色: 连接子)。

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PROTAC EZH2 Degrader-9

PROTAC EZH2 Degrader-9 Chemical Structure

CAS No. : 2978620-84-5

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PROTAC EZH2 Degrader-9 相关抗体

Top Publications Citing Use of Products

查看 PROTACs 亚型特异性产品:

查看所有亚型
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

查看 Histone Methyltransferase 亚型特异性产品:

查看所有亚型
EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC EZH2 Degrader-9 is orally active EZH2 PROTAC degrader degrading EZH2 via the ubiquitin-proteasome pathway. PROTAC EZH2 Degrader-9 downregulates PRC2 core subunits and potent inhibition of H3K27me3 without affecting common CRBN neosubstrates while it was selective over GSp'T1 and ikZF1/3. PROTAC EZH2 Degrader-9 exhibits potent antiproliferative activity against multiple cancer cell lines by inducing cell cycle and apoptosis. PROTAC EZH2 Degrader-9 reverses PRC2-mediated gene silencing and inhibiting EZH2 non-catalytic target gene activation. PROTAC EZH2 Degrader-9 can be used for leukemia, lymphoma, and non-small cell lung cancer research[1]. (Pink: EZH2 ligand (HY-78694); Blue: Cereblon ligand (HY-W087383); Black: linker).

IC50 & Target[1]

EZH2

 

体外研究
(In Vitro)

PROTAC EZH2 Degrader-9 (compound 5g) (0-10 μM, 0-48 小时) 在MV4–11细胞中诱导的EZH2降解依赖于泛素-蛋白酶体系统及其与 E3 连接酶 CRBN 的结合[1]。
PROTAC EZH2 Degrader-9 (72 小时) 对多种癌细胞具有抗增殖活性，包括 MV4–11 和 MOLM-13 (白血病)、SU-DHL-4 和 SU-DHL-6 (大 B 细胞淋巴瘤)、A549、NCI-H1299 和 NCI-H1703 (小细胞肺癌)，其 IC50 值分别为 2.22、2.60、6.35、9.23、19.26、4.41 和 6.35 μM；该活性与 EZH2 (皮尔逊相关系数 r = -0.860, p = 0.013) 和 CRBN (皮尔逊相关系数 r = -0.726, p = 0.049) 的表达水平呈显著负相关[1]。
PROTAC EZH2 Degrader-9 (10 μM, 24 小时) 通过降解 NCI-H1299、NCI-H1703、MOLM-13 和 A549 细胞中的 EZH2 及其他 PRC2 亚基，发挥抗增殖活性[1]。
PROTAC EZH2 Degrader-9 (10 μM, 72 小时) 诱导了 1,314 个差异表达基因，其中 657 个上调，下调 657 个；影响了包括 DNA 修复、有丝分裂细胞周期及其 G2/M 期转换在内的多个生物学过程；使差异表达基因富集于癌症相关通路，尤其是调控细胞周期的通路；并导致 G2/M 检查点通路呈负富集，凋亡通路呈正富集[1]。
PROTAC EZH2 Degrader-9 (0.12-10 μM, 24 和 72 小时) 导致 MV4-11 细胞周期阻滞于 G0/G1 期，阻止其进入 S 期和 G2/M 期，并剂量依赖性地诱导细胞凋亡[1]。
PROTAC EZH2 Degrader-9 (1-10 μM, 72 小时) 改变了 MV4-11 细胞中受 EZH2 催化和非催化活性调控的基因表达[1]。

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

PROTAC EZH2 Degrader-9 相关抗体:

Western Blot Analysis[1]

Cell Line: MV4–11 cells
Concentration: 0, 0.06, 0.13, 0.25, 0.5, 1.0, 3.0 and 10 μM
Incubation Time: 0, 0.5, 1, 2, 4, 8, 24, 48 h
Result: Decreased PRC2 levels with 10 μM at different durations.
Degraded EZH2, EED, SUZ12, and RbAp46 protein levels with 10 μM for 24 and 48 h.
Inhibited the expression of H3K27me3 at 10 μM 24 h, and achieved an almost complete elimination with 10 μM for 48 h.
Had a minimal impact on EZH2 at low concentrations of ≤ 0.25 μM h with different durations for 24 h.
Induced the degradation of all PRC2 core subunits (EZH2, EED, SUZ12, and RbAp46) at higher concentrations.
Observe no obvious changes in protein levels of GSPT1, IKZF1 or IKZF3 with different concentration for 24 h.
Exhibited no obvious effects on mRNA expression levels of EZH2, EED, SUZ12, and RbAp46 at either 3 or 10 μM.
Induced degradation of EZH2 can be reversed by MLN4924.

Western Blot Analysis[1]

Cell Line: NCI-H1299, NCI-H1703, MOLM-13, and A549 cells
Concentration: 10 μM
Incubation Time: 24 h
Result: Induced the degradation of EZH2 as well as PRC2 subunits SUZ12, EED, and RbAp46 in in NCI-H1299 and NCI-H1703 cells.
Weakly against EZH2 and decreased PRC2 subunits in MOLM-13 cells.
Had no obvious degradation effect on PRC2 subunits in A549 cells.

Cell Cycle Analysis[1]

Cell Line: MV4–11 cells
Concentration: 0.12, 0.37, 1.11, 3.33, 10 μM
Incubation Time: 24 h
Result: Demonstrated a significant dose-dependent rise in cell populations at the G0/G1 phase, increased to 63.20 %, 64.61 %, 66.12 %, 69.89 %, and 73.60 % at different concentration.

Real Time qPCR[1]

Cell Line: MV4-11 cells
Concentration: 1, 3 and 10 μM
Incubation Time: 72 h
Result: Up-regulated the mRNA expressions of PRC2- dependent genes, including ADRB2, CDKN2A, TXINP, and TNFRSF21 in a dose-dependent manner.
Downregulated the expression of several genes known as targets of EZH2 noncanonical functions, including ARL6IP, BRIC5, CENPK, CHEK1, TACC3, TRAP, CDC25A, and E2F1.
Not affected the expression of c-Myc.
药代动力学
(Parmacokinetics)
Species Dose Route Indicator value
Mice[1] 1 mg/kg i.v. Cmax 3536.71 μg/L
Mice[1] 10 mg/kg p.o. Cmax 989 μg/L
Mice[1] 1 mg/kg i.v. T1/2 2.32 h
Mice[1] 10 mg/kg p.o. T1/2 2.43 h
Mice[1] 1 mg/kg i.v. CL 0.13 L/h/kg
Mice[1] 10 mg/kg p.o. CL 1.50 L/h/kg
Mice[1] 1 mg/kg i.v. AUC0-t 7.56 mg·h/L
Mice[1] 10 mg/kg p.o. AUC0-t 6732.54 μg/L·h
Mice[1] 1 mg/kg i.v. Vz 0.44 L/kg
Mice[1] 10 mg/kg p.o. Vz 5.26 L/kg
Mice[1] 1 mg/kg i.v. MRT0-t 3.23 h
Mice[1] 10 mg/kg p.o. MRT0-t 4.91 h
Mice[1] 10 mg/kg p.o. F 8.91 %
分子量

882.06

Formula

C51H59N7O7
CAS 号
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.
纯度 & 产品资料
参考文献

PROTAC EZH2 Degrader-9 相关分类

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PROTAC EZH2 Degrader-92978620-84-5PROTACsHistone MethyltransferaseApoptosisEZH2PROTACubiquitin-proteasomeCRBNapoptosisleukemialymphomaand non-small cell lung cancerInhibitorinhibitorinhibit

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