Cat. No.: HY-151563

OTUB1/USP8-IN-1

3 Cited Publications

고객리뷰

Based on 3 publication(s) in Google Scholar

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.

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

Purity: 98.31%
CAS No.: 2858800-98-1
화학식: C₂₂H₁₆ClFN₂O₄
분자량:426.82

보관:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

OTUB1/USP8-IN-1 Chemical Structure

CAS No.: 2858800-98-1

사이즈

가격

재고

수량

Amount: USD 0.00

* 장바구니에 담기 전 물품의 수량을 선택해 주십시오.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (3)
용액&용해도
- In Vitro
순도&문서
References
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

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]

All Deubiquitinase Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	1004 nM Compound: 61	Antiproliferative activity against human A549 cells harboring KRAS mutant incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells harboring KRAS mutant incubated for 72 hrs by MTT assay	[PMID: 36221183]
EBC-1	IC₅₀	172 nM Compound: 61	Antiproliferative activity against human EBC-1 cells harboring wild type KRAS incubated for 72 hrs by MTT assay Antiproliferative activity against human EBC-1 cells harboring wild type KRAS incubated for 72 hrs by MTT assay	[PMID: 36221183]
NCI-H1703	IC₅₀	145 nM Compound: 61	Antiproliferative activity against human NCI-H1703 cells harboring wild type KRAS incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H1703 cells harboring wild type KRAS incubated for 72 hrs by MTT assay	[PMID: 36221183]
NCI-H1975	IC₅₀	118 nM Compound: 61	Antiproliferative activity against human NCI-H1975 cells harboring wild type KRAS incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells harboring wild type KRAS incubated for 72 hrs by MTT assay	[PMID: 36221183]
NCI-H23	IC₅₀	431 nM Compound: 61	Antiproliferative activity against human NCI-H23 cells harboring KRAS mutant incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H23 cells harboring KRAS mutant incubated for 72 hrs by MTT assay	[PMID: 36221183]

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.

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)

T_1/2 (h) 0.83 1.75

T_max (h) 0.33

C_max (μg/L) 4274

AUC (μg·h/L) 1345 3747

CL (L/h/kg) 44

Vdss (L/kg) 0.77

Chemical Information

CAS No. 2858800-98-1
Appearance Solid
분자량 426.82
화학식 C₂₂H₁₆ClFN₂O₄
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
선적

Room temperature in continental US; may vary elsewhere.

보관

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (3)

All

Sort by:

Journal Impact Factor

J Med Chem

Discovery of New OTUB1 Covalent Ligands via Structure-Activity Relationship Studies for Targeted Protein Stabilization. [Abstract]

2026 May 14;69(9):10263-10277. PMID: 42083385
Biochem Pharmacol

OTUB1 enhances fatty acid oxidation in APAP-induced liver injury by mediating ACSL5 deubiquitination. [Abstract]

2025 Jul:237:116957. PMID: 40280245
Sci Rep

4-Octyl itaconate alleviates sepsis-induced liver injury by regulating ferroptosis via the OTUB1/TRAF3 axis. [Abstract]

2026 Feb 10;16(1):8201. PMID: 41667684

용액&용해도

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)

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

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.3429 mL

11.7145 mL

23.4291 mL

5 mM

0.4686 mL

2.3429 mL

4.6858 mL

10 mM

0.2343 mL

1.1715 mL

2.3429 mL

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.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

몰농도 계산기

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Tan L, et, al. Discovery of Potent OTUB1/USP8 Dual Inhibitors Targeting Proteostasis in Non-Small-Cell Lung Cancer. J Med Chem. 2022 Oct 11. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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
H₂O / DMSO	1 mM	2.3429 mL	11.7145 mL	23.4291 mL	58.5727 mL
H₂O / DMSO	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

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Keywords

OTUB1/USP8-IN-1

3 Cited Publications

100 mg 견적 받기

Subscribe to the

MedChemExpress

Newsletter

상품명:
Cat. No.:
수량:
MCE Japan Authorized Agent:

상품명:
CAS No.:
Species:
Purity:
수량:

OTUB1/USP8-IN-1

Bioactive Compound Library Max

Bioactive Compound Library

Cell Cycle/DNA Damage Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Ubiquitination Compound Library

Orally Active Compound Library

Anti-Lung Cancer Compound Library

Metabolic Enzyme Compound Library

Protease Inhibitor Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) OTUB1/USP8-IN-1

All Deubiquitinase Isoforms

Biological Activity

Chemical Information

Publications (3)

용액&용해도

순도&문서

References

Help & FAQs

Complete Stock Solution Preparation Table

Administration	i.v. (1 mg/kg)	p.o. (10 mg/kg)
T_1/2 (h)	0.83	1.75
T_max (h)		0.33
C_max (μg/L)		4274
AUC (μg·h/L)	1345	3747
CL (L/h/kg)	44
Vdss (L/kg)	0.77

OTUB1/USP8-IN-1

Bioactive Compound Library Max

Bioactive Compound Library

Cell Cycle/DNA Damage Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Ubiquitination Compound Library

Orally Active Compound Library

Anti-Lung Cancer Compound Library

Metabolic Enzyme Compound Library

Protease Inhibitor Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) OTUB1/USP8-IN-1

All Deubiquitinase Isoforms

Biological Activity

Chemical Information

Publications (3)

용액&용해도

순도&문서

References

Help & FAQs

Complete Stock Solution Preparation Table

OTUB1/USP8-IN-1 Related Classifications

HY-151563 Related Classifications