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

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.

For research use only. We do not sell to patients.

OTUB1/USP8-IN-1 Chemical Structure

OTUB1/USP8-IN-1 Chemical Structure

CAS No. : 2858800-98-1

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Based on 1 publication(s) in Google Scholar

OTUB1/USP8-IN-1 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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Description

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]
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].

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

OTUB1/USP8-IN-1 Related Antibodies

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.
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].

MedChemExpress (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
Molecular Weight

426.82

Formula

C22H16ClFN2O4
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=C2OC(C3=C(F)C=CC(O[C@H]4CN(C)CC4)=C3Cl)=N1)C5=C(C=CC=C5)C2=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (117.15 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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  • Dilution Calculator

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Purity & Documentation

Purity: 98.04%

COA (249 KB) HNMR (138 KB) RP-HPLC (139 KB) LCMS (107 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
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
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
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OTUB1/USP8-IN-1 Related Classifications

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:

OTUB1/USP8-IN-12858800-98-1DeubiquitinaseDUBsAntiproliferativeH1975EBC-1H1703H23A549antitumorInhibitorinhibitorinhibit

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