OTUB1/USP8-IN-1

Name: OTUB1/USP8-IN-1
Brand: MedChemExpress
SKU: HY-151563
Rating: 4.5 (1 reviews)

Cat. No.: HY-151563 Purity: 98.31%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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

CAS No. : 2858800-98-1

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 330	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 330	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 300	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 480	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 950	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1450	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 2250	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of OTUB1/USP8-IN-1:

OTUB1/USP8-IN-1 TFA Get quote

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USP1 USP2 USP7 USP8 USP30 UCHL1

Biological Activity
Purity & Documentation
References
Customer Review

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]

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

Molecular Weight

426.82

Formula

C₂₂H₁₆ClFN₂O₄

CAS No.

2858800-98-1

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)

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)

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
10 mM	0.2343 mL	1.1715 mL	2.3429 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.

* 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 98.31%

Select Batch:

Data Sheet (277 KB) SDS (251 KB)

COA (249 KB) HNMR (136 KB) RP-HPLC (169 KB) LCMS (234 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]

Complete Stock Solution Preparation Table

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.

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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OTUB1/USP8-IN-1

Customer Review

Other Forms of OTUB1/USP8-IN-1:

OTUB1/USP8-IN-1 Related Antibodies

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Deubiquitinase Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

OTUB1/USP8-IN-1 Related Antibodies

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Dilution Calculator

Complete Stock Solution Preparation Table

OTUB1/USP8-IN-1 Related Classifications

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