1. Cell Cycle/DNA Damage
  2. Deubiquitinase
  3. OTUB1/USP8-IN-1

OTUB1/USP8-IN-1 是一种有效的双重 OTUB1/USP8 抑制剂,抑制 OTUB1USP8IC50 值分别为 0.17 和 0.28 nM。OTUB1/USP8-IN-1 可用于癌症的研究。

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OTUB1/USP8-IN-1 Chemical Structure

OTUB1/USP8-IN-1 Chemical Structure

CAS No. : 2858800-98-1

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5 mg ¥3000
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10 mg ¥4800
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Customer Review

Other Forms of OTUB1/USP8-IN-1:

查看 Deubiquitinase 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

OTUB1/USP8-IN-1 is a potent dual OTUB1/USP8 inhibitor with IC50 values of 0.17 and 0.28 nM for OTUB1 and USP8, respectively. OTUB1/USP8-IN-1 can be used in research of cancer[1].

IC50 & Target

IC50: 0.17 nM (OTUB1) and 0.28 nM (USP8)[1]

体外研究
(In Vitro)

OTUB1/USP8-IN-1 (compound 61; 10 nM-10 μM; 72 h) has antiproliferative effects in KRAS-WT (H1975, EBC-1, H1703) and KRAS-mutated (H23, A549) NSCLC cell lines[1].
OTUB1/USP8-IN-1 (500 nM; 24 h) decreases in protein levels of both UBE2N and EGFR in H1975 cells[1].

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

Cell Viability Assay[1]

Cell Line: KRAS-WT (H1975, EBC-1, H1703) and KRAS-mutated (H23, A549) NSCLC cell lines
Concentration: 10 nM-10 μM
Incubation Time: 72 hours
Result: Inhibited cell proliferative with IC50 values of 118, 145, 172, 431, and 1004 nM for H1975, H1703, EBC-1, H23, and A549 cells, respectively.

Western Blot Analysis[1]

Cell Line: H1975 cells
Concentration: 500 nM
Incubation Time: 24 hours
Result: Decreased the levels of both UBE2N and EGFR in a dose-dependent manner.
体内研究
(In Vivo)

OTUB1/USP8-IN-1 (compound 61; 10 nM-10 μM; 72 h) decreases the tumor burden in the H1975 xenograft mouse model[1].

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

Animal Model: Female BALB/c nude mice with H1975 xenografts (5 weeks of age)[1]
Dosage: 5 mg/kg
Administration: Intraperitoneal injection; QD and BID, for 2 weeks
Result: Reduced total tumor weight and average tumor volume in an over twofold with BID dosing.
Animal Model: Female BALB/c nude mice with H1975 xenograft (5 weeks of age)[1]
Dosage: 1 and 10 mg/kg
Administration: Intravenous injection (1 mg/kg) and oral administration (10 mg/kg)
Result: 1.19
Administration i.v. (1 mg/kg) p.o. (10 mg/kg)
T1/2 (h) 0.83 1.75
Tmax (h) 0.33
Cmax (μg/L) 4274
AUC (μg·h/L) 1345 3747
CL (L/h/kg) 44
Vdss (L/kg) 0.77
分子量

426.82

Formula

C22H16ClFN2O4

CAS 号
性状

固体

颜色

Light yellow to yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 50 mg/mL (117.15 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

H2O 中的溶解度 : 4.07 mg/mL (9.54 mM; ultrasonic and warming and adjust pH to 3 with 1 M HCL and heat to 60°C)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.3429 mL 11.7145 mL 23.4291 mL
5 mM 0.4686 mL 2.3429 mL 4.6858 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。-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。

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

  • 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

纯度: 98.05%

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。-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
H2O / DMSO 1 mM 2.3429 mL 11.7145 mL 23.4291 mL 58.5727 mL
5 mM 0.4686 mL 2.3429 mL 4.6858 mL 11.7145 mL
DMSO 10 mM 0.2343 mL 1.1715 mL 2.3429 mL 5.8573 mL
15 mM 0.1562 mL 0.7810 mL 1.5619 mL 3.9048 mL
20 mM 0.1171 mL 0.5857 mL 1.1715 mL 2.9286 mL
25 mM 0.0937 mL 0.4686 mL 0.9372 mL 2.3429 mL
30 mM 0.0781 mL 0.3905 mL 0.7810 mL 1.9524 mL
40 mM 0.0586 mL 0.2929 mL 0.5857 mL 1.4643 mL
50 mM 0.0469 mL 0.2343 mL 0.4686 mL 1.1715 mL
60 mM 0.0390 mL 0.1952 mL 0.3905 mL 0.9762 mL
80 mM 0.0293 mL 0.1464 mL 0.2929 mL 0.7322 mL
100 mM 0.0234 mL 0.1171 mL 0.2343 mL 0.5857 mL

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

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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产品名称:
OTUB1/USP8-IN-1
目录号:
HY-151563
需求量: