2. PROTAC Epigenetics Apoptosis
  3. PROTACs Histone Methyltransferase Apoptosis
  4. C199

C199 是一种靶向 PRMT4 的 PROTAC 降解剂 (DC50 = 106 nM)。C199对 PRMT4 相对于其他蛋白质精氨酸甲基转移酶表现出高选择性。C199 表现出强大的细胞降解能力。C199 诱导骨髓瘤细胞系凋亡 (Apoptosis)。C199 通过 VHL-蛋白酶体途径高效清除 PRMT4 蛋白。C199 具有相对较长的半衰期，并显示出强大的抗多发性骨髓瘤 (MM) 活性 (Pink: Target protein ligand (HY-111109); Blue: E3 ligase ligand (HY-112078), E3 ligase ligand + linker (HY-174474); black: Linker)。

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C199 Chemical Structure

C199 Chemical Structure

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C199 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

C199 is a PROTAC degrader targeting PRMT4 (DC50 = 106 nM). C199 shows high selectivity for PRMT4 over other protein arginile methyltransferases. C199 exhibits strong cell degradation ability. C199 induces apoptosis in MM cell lines. C199 efficiently clears PRMT4 protein via the VHL-proteasome pathway. C199 has a relatively long half-life and shows strong anti-multiple myeloma (MM) tumor activity (Pink: Target protein ligand (HY-111109); Blue: E3 ligase ligand (HY-112078), E3 ligase ligand + linker (HY-174474); black: Linker)[1].

IC50 & Target

VHL

 

PRMT4

 

体外研究
(In Vitro)

C199 (Compound C199) (0.001-1 μM, 12 天) 有效抑制骨髓瘤细胞增殖[1]。

C199 (0.007-0.5 μM, 6 天) 在 NCI-H929 细胞中诱导剂量依赖性细胞凋亡[1]。

C199 (0.01-0.5 μM, 12-72 h) 在 NCI-H929 细胞中高效、选择性降解 PRMT4 蛋白[1]。

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

C199 相关抗体:

Apoptosis Analysis[1]

Cell Line: NCI-H929 cells
Concentration: 0.007 μM, 0.031 μM, 0.062 μM, 0.125 μM, 0.5 μM
Incubation Time: 6 days
Result: Apoptosis rates prominently reached 81.9% at 0.5 μM.

Western Blot Analysis[1]

Cell Line: NCI-H929 cells
Concentration: 0.01 μM, 0.03 μM, 0.06 μM, 0.1 μM, 0.12 μM, 0.25 μM, 0.5 μM
Incubation Time: 12 h, 24 h, 48 h, 72 h
Result: Reached a degradation efficiency of 92 % when the compound concentration was 0.5 μM.
Still maintained a high degradation efficiency of 56 % when the concentration dropped to 0.1 μM.
Had a DC50 of 0.106 μM, caused a significant decrease in PRMT4 level by about half after 24 hours, and reached a Dmax of 93.1 % after 72 hours.
Degraded PRMT4 via a VHL- and proteasome-dependent instead of lysosomal pathway.
Inhibited PABP1 methylation by 97 %, while EZM2302 only inhibited 37 %. Was about three times more efficient than EZM2302 in inhibiting BAF155 methylation.
Affected only the expression of PRMT4 and had no effect on other homologous proteins.
Effectively modulated asymmetric dimethylation of PRMT4 substrates through targeted degradation of the methyltransferase.

Cell Proliferation Assay[1]

Cell Line: NCI-H929 cells, RPMI-8226 cells
Concentration: 0.001 μM, 0.01 μM. 0.1 μM, 1 μM
Incubation Time: 12 days
Result: Outperformed the inhibitor EZM2302 significantly (GI50: 0.089 μM for NCI-H929 cells, 0.145 μM for RPMI-8226 cells).
体内研究
(In Vivo)

C199 (Compound C199) (40-80 mg/kg, i.p, 每日 2 次连续 20 天) 抑制BALB/c裸鼠体内多发性骨髓瘤异种移植物的生长，并下调 PRMT4 的表达，且无明显的器官毒性[1]。

C199 (100-1000 mg/kg, i.p, 每日 1 次连续 14 天) 高剂量下在 CD1 小鼠中安全性良好，治疗窗宽，安全性优异[1]。

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

Animal Model: NCI-H929 xenograft model established in female BALB/c nude mice (6-8 weeks, 18-22 g)[1]
Dosage: 40 mg/kg, 80 mg/kg
Administration: Intraperitoneal injection (i.p.), twice daily for 20 days
Result: Inhibited tumor growth (TGI = 78 %).
Significantly reduced tumor PRMT4 protein.
Left the heart, liver, spleen and kidneys morphologically normal.
Animal Model: Famale and male CD1 nude mice[1]
Dosage: 100 mg/kg, 500 mg/kg, 1000 mg/kg
Administration: Intraperitoneal injection (i.p.), once daily for 14 days
Result: Left body weight and organ indexes normal, and caused no death or organ damage at 1000 mg/kg.
分子量

1236.05

Formula

C67H95ClN10O8S
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

C199 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • 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:

C199C 199C-199PROTACsHistone MethyltransferaseApoptosisNCI-H929 cellsRPMI-8226 cellsPRMT4BALB/c miceCD1 miceMultiple MyelomadegradationInhibitorinhibitorinhibit

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产品名称：
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目录号：
HY-174445
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