1. Epigenetics
  2. Histone Methyltransferase
  3. PFI-2

PFI-2  (Synonyms: (R)-PFI-2)

目录号: HY-18627 纯度: 99.68%
COA 产品使用指南 技术支持

PFI-2 ((R)-PFI-2) 是一种化学探针,是一种强效的选择性 SETD7 抑制剂。(R)-PFI-2 具有高度抑制活性,其 IC50 值为2.0 nM,(S)-PFI-2 的抑制活性 IC50 值为 1.0 μM。PFI-2 hydrochloride 可用于研究慢性肾脏疾病和肾纤维化发展过程中的炎症反应。

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PFI-2

PFI-2 Chemical Structure

CAS No. : 1627676-59-8

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10 mg ¥1600
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25 mg ¥2886
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50 mg ¥4185
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Customer Review

Other Forms of PFI-2:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PFI-2 ((R)-PFI-2 hydrochloride) hydrochloride, a chemical probe, is a potent and selective SET domain containing lysine methyltransferase 7 (SETD7) inhibitor. (R)-PFI-2 shows high inhibiting activity with IC50 value of 2.0 nM and (S)-PFI-2 shows inhibiting activity with IC50 value of 1.0 μM. PFI-2 hydrochloride can be used for the research of chronic kidney disease and inflammation response in the development of renal fibrosis[1][2].

IC50 & Target

SETD7/KMT7

 

体外研究
(In Vitro)

(R)-PFI-2 shows high inhibiting activity with IC50 value of 2.0 nM and (S)-PFI-2 shows inhibiting activity with IC50 value of 1.0 μM[1].

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

体内研究
(In Vivo)

PFI-2 (i.p., 200 μM, twice a week) attenuates the progression of renal fibrosis and preserves renal function in FA nephropathy[2].
PFI-2 (i.p., 200 μM, twice a week) reduced ECM accumulation and fibroblasts activation after FA injury[2].
PFI-2 (i.p., 200 μM, twice a week) impeded Th2 cytokine signaling activation and M2 macrophage polarization[2].
PFI-2 (i.p., 200 μM, twice a week) suppressed M2 macrophages-myofibroblasts transition and myeloid myofibroblasts accumulation in the FA-treated kidneys[2].
PFI-2 (i.p., 200 μM, twice a week) attenuated macrophages M2 polarization and M2 macrophages-to-myofibroblasts transition in obstructed kidneys[2].
PFI-2 (i.p., 200 μM, twice a week) suppressed myeloid myofibroblast accumulation and renal fibrosis after UUO injury[2].
PFI-2 (i.p., 200 μM, twice a week) reduced the infiltration of inflammatory cells, the production of inflammatory molecules, and NF-κB activation in FA nephropathy.

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

Animal Model: Male C57BL/6 mice (8-10 week old, 20-25 g)[2]
Dosage: 200 μM (PFI-2 is diluted in 100 μL 0.1% (v/v) DMSO to a concentration of 200 μM/100 μL)
Administration: intraperitoneal injection, twice a week
Result: Presented less bone marrow-derived myofibroblasts, fewer CD206+/α-smooth muscle actin + cells and developed less renal fibrosis (P<0.01).
Reduced the infiltration of inflammatory cells and decreased the production of pro-inflammatory cytokines and chemokines in the kidneys after folic acid treatment (P<0.01).
Suppressed the accumulation of NF-κB p65+ cells in folic acid nephropathy (P<0.01).
分子量

499.52

Formula

C23H25F4N3O3S

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
细胞实验: 

DMSO 中的溶解度 : ≥ 100 mg/mL (200.19 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0019 mL 10.0096 mL 20.0192 mL
5 mM 0.4004 mL 2.0019 mL 4.0038 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0019 mL 10.0096 mL 20.0192 mL 50.0480 mL
5 mM 0.4004 mL 2.0019 mL 4.0038 mL 10.0096 mL
10 mM 0.2002 mL 1.0010 mL 2.0019 mL 5.0048 mL
15 mM 0.1335 mL 0.6673 mL 1.3346 mL 3.3365 mL
20 mM 0.1001 mL 0.5005 mL 1.0010 mL 2.5024 mL
25 mM 0.0801 mL 0.4004 mL 0.8008 mL 2.0019 mL
30 mM 0.0667 mL 0.3337 mL 0.6673 mL 1.6683 mL
40 mM 0.0500 mL 0.2502 mL 0.5005 mL 1.2512 mL
50 mM 0.0400 mL 0.2002 mL 0.4004 mL 1.0010 mL
60 mM 0.0334 mL 0.1668 mL 0.3337 mL 0.8341 mL
80 mM 0.0250 mL 0.1251 mL 0.2502 mL 0.6256 mL
100 mM 0.0200 mL 0.1001 mL 0.2002 mL 0.5005 mL
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.

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PFI-2
目录号:
HY-18627
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