Cat. No.: HY-78695

JQ-1 carboxylic acid

9 Cited Publications

Customer Review

Based on 9 publication(s) in Google Scholar

JQ-1 carboxylic acid, a (+)-JQ-1 (HY-13030) derivative, is a potent BET bromodomain inhibitor. JQ-1 carboxylic acid can be used to synthesize PROTAC, which can target the degradation of BRD4.

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

Purity: 99.69%
CAS No.: 202592-23-2
Formula: C₁₉H₁₇ClN₄O₂S
Molecular Weight:400.88

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

JQ-1 carboxylic acid Chemical Structure

CAS No.: 202592-23-2

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Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (9)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

JQ-1 carboxylic acid, a (+)-JQ-1 (HY-13030) derivative, is a potent BET bromodomain inhibitor. JQ-1 carboxylic acid can be used to synthesize PROTAC, which can target the degradation of BRD4.

IC₅₀ & Target^[1]

BET

BRD4

DCAF1

BRD2

BRD3

BRD4BD1

KLHDC2

GSPT1

All Epigenetic Reader Domain Isoforms :

All Ligands for E3 Ligase Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	EC₅₀	>50 μM Compound: JQ1-CO2H	Cytotoxicity against human HEK293 cells assessed as inhibition of cell viability incubated for 30 mins by cell titer-glo assay Cytotoxicity against human HEK293 cells assessed as inhibition of cell viability incubated for 30 mins by cell titer-glo assay	[PMID: 35859867]
HEK293	IC₅₀	>50 μM Compound: JQ1-CO2H	Cytotoxicity against human HEK293 cells assessed as inhibition of cell viability incubated for 30 mins in presence of CRBN-tracer by nanoBRET assay Cytotoxicity against human HEK293 cells assessed as inhibition of cell viability incubated for 30 mins in presence of CRBN-tracer by nanoBRET assay	[PMID: 35859867]
HEK293	IC₅₀	>50 μM Compound: JQ1-CO2H	Cytotoxicity against permeabilized HEK293 cells assessed as inhibition of cell viability incubated for 30 mins in presence of CRBN-tracer by nanoBRET assay Cytotoxicity against permeabilized HEK293 cells assessed as inhibition of cell viability incubated for 30 mins in presence of CRBN-tracer by nanoBRET assay	[PMID: 35859867]

In Vitro

JQ-1 carboxylic acid downregulates PD-L1 expression on the surface of B16F10 cells^[1].

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

Chemical Information

CAS No. 202592-23-2
Appearance Solid
Molecular Weight 400.88
Formula C₁₉H₁₇ClN₄O₂S
Color Off-white to yellow
SMILES

ClC1=CC=C(C(C2=C(N3C4=NN=C3C)SC(C)=C2C)=N[C@H]4CC(O)=O)C=C1
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (9)

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Journal Impact Factor

Int J Oral Sci

Stabilization of EREG via STT3B-mediated N-glycosylation is critical for PDL1 upregulation and immune evasion in head and neck squamous cell carcinoma. [Abstract]

2024 Jul 1;16(1):47. PMID: 38945975

JQ-1 carboxylic acid purchased from MedChemExpress. Usage Cited in: Int J Oral Sci. 2024 Jul 1;16(1):47. [Abstract]

CAL27 and HN13 cells were pretreated with JQ-1 carboxylic acid (JQ-1) for 1 h followed by stimulation with epiregulin for 24 h. The levels of PDL1 and c-Myc were examined by Western blot analysis.

JQ-1 carboxylic acid purchased from MedChemExpress. Usage Cited in: Int J Oral Sci. 2024 Jul 1;16(1):47. [Abstract]

CAL27 and HN4 cells were pretreated with JQ-1 carboxylic acid (JQ-1) for 1 h followed by stimulation with epiregulin for 24 h. The levels of PDL1 and c-Myc were examined by Western blot analysis.

JQ-1 carboxylic acid purchased from MedChemExpress. Usage Cited in: Int J Oral Sci. 2024 Jul 1;16(1):47. [Abstract]

HN30 cells were treated with JQ-1 carboxylic acid (JQ-1) for 24 h, and the levels of PDL1 and c-Myc were examined by Western blot analysis
J Am Chem Soc

Targeted Protein O-GlcNAcylation Using Bifunctional Small Molecules. [Abstract]

2024 Apr 10;146(14):9779-9789. PMID: 38561350
Nucleic Acids Res

A histidine cluster determines YY1-compartmentalized coactivators and chromatin elements in phase-separated enhancer clusters. [Abstract]

2022 May 20;50(9):4917-4937. PMID: 35390165
Cell Rep Med

A triple-action PROTAC for wild-type p53 cancer therapy. [Abstract]

2025 Dec 16;6(12):102467. PMID: 41308642
Cell Death Dis

Brd4 inhibition ameliorates Pyocyanin-mediated macrophage dysfunction via transcriptional repression of reactive oxygen and nitrogen free radical pathways. [Abstract]

2020 Jun 15;11(6):459. PMID: 32541671
Biochem Pharmacol

BRD2 promotes inflammation and lipid accumulation through the NF-κB pathway in alcoholic liver injury. [Abstract]

2025 Oct 19;243(Pt 1):117442. PMID: 41120012
Biochem Pharmacol

BRD4 promotes hepatic stellate cells activation and hepatic fibrosis via mediating P300/H3K27ac/PLK1 axis. [Abstract]

2023 Apr:210:115497. PMID: 36907496

JQ-1 carboxylic acid purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2023 Apr:210:115497. [Abstract]

The LX2 cells were pretreated with gradient concentrations (μM) of JQ-1 carboxylic acid (JQ1; 0-100 μM) and DMSO (0.1%) for 2 h and then stimulated with TGFβ for 24 h, and the mRNA levels of αSMA and COLI were detected.

JQ-1 carboxylic acid purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2023 Apr:210:115497. [Abstract]

Fibrosis-related protein expressions after treatment with JQ-1 carboxylic acid (JQ1; 1 μM) in LX2 cells.

JQ-1 carboxylic acid purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2023 Apr:210:115497. [Abstract]

The mRNA and protein expressions of PLK1 with JQ-1 carboxylic acid (JQ1; 1 μM) treatment as detected by qRT-PCR and western blot in TGFβ-activated LX2 cells.
Biochem Biophys Res Commun

Topical application of phenformin ameliorates the psoriasis-like inflammatory response via the inhibition of c-Myc expression in keratinocytes. [Abstract]

2024 Dec 3:736:150503. PMID: 39121669
Patent

US20240261416A1.

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (249.45 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

2.4945 mL

12.4726 mL

24.9451 mL

5 mM

0.4989 mL

2.4945 mL

4.9890 mL

10 mM

0.2495 mL

1.2473 mL

2.4945 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (5.19 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.08 mg/mL (5.19 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (5.19 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 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]. Huang Y, et, al. Design, Synthesis, and Evaluation of Trivalent PROTACs Having a Functionalization Site with Controlled Orientation. Bioconjug Chem. 2022 Jan 19;33(1):142-151. [Content Brief]

[2]. Chen W, et, al. Dual drugs decorated bacteria irradiate deep hypoxic tumor and arouse strong immune responses. Biomaterials. 2022 Jul;286:121582. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.4945 mL	12.4726 mL	24.9451 mL	62.3628 mL
	5 mM	0.4989 mL	2.4945 mL	4.9890 mL	12.4726 mL
	10 mM	0.2495 mL	1.2473 mL	2.4945 mL	6.2363 mL
	15 mM	0.1663 mL	0.8315 mL	1.6630 mL	4.1575 mL
	20 mM	0.1247 mL	0.6236 mL	1.2473 mL	3.1181 mL
	25 mM	0.0998 mL	0.4989 mL	0.9978 mL	2.4945 mL
	30 mM	0.0832 mL	0.4158 mL	0.8315 mL	2.0788 mL
	40 mM	0.0624 mL	0.3118 mL	0.6236 mL	1.5591 mL
	50 mM	0.0499 mL	0.2495 mL	0.4989 mL	1.2473 mL
	60 mM	0.0416 mL	0.2079 mL	0.4158 mL	1.0394 mL
	80 mM	0.0312 mL	0.1559 mL	0.3118 mL	0.7795 mL
	100 mM	0.0249 mL	0.1247 mL	0.2495 mL	0.6236 mL

Keywords

JQ-1 carboxylic acid

9 Cited Publications

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JQ-1 carboxylic acid

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Publications Citing Use of MedChemExpress (MCE) JQ-1 carboxylic acid

All Epigenetic Reader Domain Isoforms

All Ligands for E3 Ligase Isoforms

Biological Activity

Chemical Information

Publications (9)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

JQ-1 carboxylic acid Related Classifications

HY-78695 Related Classifications