Art. -Nr.: HY-101026

CCT251236

5 Cited Publications

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Based on 5 publication(s) in Google Scholar

CCT251236 is an orally available pirin ligand from a heat shock transcription factor 1 (hsf1) phenotypic screen with an IC₅₀ of 19 nM for inhibition of HSF1-mediated HSP72 induction.

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Reinheit: 99.04%
CAS. Nr.: 1693731-40-6
Formel: C₃₂H₃₂N₄O₅
Molecular Weight:552.62

Speicherung:

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

CCT251236 Chemical Structure

CAS. Nr.: 1693731-40-6

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Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (5)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

CCT251236 is an orally available pirin ligand from a heat shock transcription factor 1 (hsf1) phenotypic screen with an IC₅₀ of 19 nM for inhibition of HSF1-mediated HSP72 induction.

IC₅₀ & Target^[1]

HSP72

19 nM (IC₅₀, SK-OV-3 cells)

Alle HSP Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
SK-OV-3	GI₅₀	1.1 nM Compound: 26	Antiproliferative activity against human SKOV3 cells assessed as free compound concentration required for 50% growth inhibition after 96 hrs by CellTiter Blue assay Antiproliferative activity against human SKOV3 cells assessed as free compound concentration required for 50% growth inhibition after 96 hrs by CellTiter Blue assay	[PMID: 28004573]
SK-OV-3	GI₅₀	2.2 nM Compound: 26	Antiproliferative activity against human SKOV3 cells after 96 hrs by CellTiter Blue assay Antiproliferative activity against human SKOV3 cells after 96 hrs by CellTiter Blue assay	[PMID: 28004573]
SK-OV-3	GI₅₀	2.2 nM Compound: 1; CCT251236	Antiproliferative activity against human SK-OV-3 cells assessed as cell growth inhibition measured after 96 hrs by resazurin dye based celltiter-blue viability assay Antiproliferative activity against human SK-OV-3 cells assessed as cell growth inhibition measured after 96 hrs by resazurin dye based celltiter-blue viability assay	[PMID: 37017629]
WM 266-4	GI₅₀	12 nM Compound: 26	Antiproliferative activity against human WM266.4 cells after 96 hrs by CellTiter Blue assay Antiproliferative activity against human WM266.4 cells after 96 hrs by CellTiter Blue assay	[PMID: 28004573]

In Vitro

CCT251236 (0-100 nM; 24hours) displays a desired balance of in vitro properties, while maintaining excellent cellular activity with a pIC50=7.73 ± 0.07 (IC₅₀=19 nM) for inhibition of HSF1-mediated HSP72 induction. The free GI₅₀ is 1.1 nM in SK-OV-3 cells that calculated from the free fraction in the cell assay^[1].
CCT251236 (0-100 nM; 24 hours) blocks 17-AAG induced he HSF1-mediated heat-shock proteins, HSP72 and HSP27 expression as a concentration manner in SK-OV-3 cells^[1].
CCT251236 (0-100 nM; 24 hours), pre-treated with 250 nM 17-AAG for 6h, blocks the induction of HSPA1A mRNA by 17-AAG in a dosedependent manner^[1].

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

Western Blot Analysis^[1]

Cell Line:

SK-OV-3 cells
Concentration:

0 nM; 10 nM; 100 nM
Incubation Time:

24 hours
Result:

Inhibited HSP72 and HSP27 expression at the dose of 10 nM.

RT-PCR^[1]

Cell Line:

SK-OV-3 cells
Concentration:

0 nM; 10 nM; 100 nM and 1000 nM
Incubation Time:

24 hours
Result:

Decreased HSPA1A mRNA level.

In Vivo

CCT251236 (oral adminstation; 5 or 20 mg/kg) in nontumor bearing immunocompetent BALB/c mice exhibits free C_av^0-24h value of 2.0 nM and 1.2 nM, respectively^[2].
CCT251236 (oral adminstation; 20 mg/kg; 33 days) has a clear therapeutic efficacy in mice with a tumor growth inhibition (%TGI) of 70% based on final tumor volumes. After 33 days, the mean tumor weights decreases 64% when compares to control group. In addition, the compound’s basicity and high volume of distribution shows in tumor withtumor concentrations of CCT251236 as high as 940 nM^[2].

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

Animal Model:

Athymic mice with SK-OV-3 cells^[2]

Was efficacious in SK-OV-3 cell induced-tumor mice model.

Chemical Information

CAS. Nr. 1693731-40-6
Appearance Solid
Molecular Weight 552.62
Formel C₃₂H₃₂N₄O₅
Color White to off-white
SMILES

CC1=CC=C(NC(C2=CC(OCCO3)=C3C=C2)=O)C=C1NC(C4=CC(C=CC(OCCN5CCCC5)=N6)=C6C=C4)=O
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Publications (5)

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Journal Impact Factor

Nat Commun

Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]

2026 Feb 12;17(1):1214. PMID: 41680175
Proc Natl Acad Sci U S A

Local translation in nuclear condensate amyloid bodies. [Abstract]

2021 Feb 16;118(7):e2014457118. PMID: 33568529
Mol Med

Baicalin alleviates chronic obstructive pulmonary disease through regulation of HSP72-mediated JNK pathway. [Abstract]

2021 May 30;27(1):53. PMID: 34053448
Mol Oncol

Pirin: a potential novel therapeutic target for castration-resistant prostate cancer regulated by miR-455-5p. [Abstract]

2019 Feb;13(2):322-337. PMID: 30444038
Loyola University Chicago

2026.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (180.96 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

1.8096 mL

9.0478 mL

18.0956 mL

5 mM

0.3619 mL

1.8096 mL

3.6191 mL

10 mM

0.1810 mL

0.9048 mL

1.8096 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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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: ≥ 2.5 mg/mL (4.52 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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% Corn Oil

Solubility: 2.5 mg/mL (4.52 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL. 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 (25.0 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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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)

Verweise

[1]. Cheeseman MD, et al. Discovery of a Chemical Probe Bisamide (CCT251236): An OrallyBioavailable Efficacious Pirin Ligand from a Heat ShockTranscription Factor 1 (HSF1) Phenotypic Screen. J Med Chem. 2017 Jan 12;60(1):180-201. [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	1.8096 mL	9.0478 mL	18.0956 mL	45.2390 mL
	5 mM	0.3619 mL	1.8096 mL	3.6191 mL	9.0478 mL
	10 mM	0.1810 mL	0.9048 mL	1.8096 mL	4.5239 mL
	15 mM	0.1206 mL	0.6032 mL	1.2064 mL	3.0159 mL
	20 mM	0.0905 mL	0.4524 mL	0.9048 mL	2.2620 mL
	25 mM	0.0724 mL	0.3619 mL	0.7238 mL	1.8096 mL
	30 mM	0.0603 mL	0.3016 mL	0.6032 mL	1.5080 mL
	40 mM	0.0452 mL	0.2262 mL	0.4524 mL	1.1310 mL
	50 mM	0.0362 mL	0.1810 mL	0.3619 mL	0.9048 mL
	60 mM	0.0302 mL	0.1508 mL	0.3016 mL	0.7540 mL
	80 mM	0.0226 mL	0.1131 mL	0.2262 mL	0.5655 mL
	100 mM	0.0181 mL	0.0905 mL	0.1810 mL	0.4524 mL

Keywords

CCT251236

5 Cited Publications

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CCT251236

Cell Cycle/DNA Damage Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Cytoskeleton Compound Library

Orally Active Compound Library

Chemical Probe Library

Transcription Factor-Targeted Library

Heterocyclic Compound Library

Metabolic Enzyme Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) CCT251236

Alle HSP Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (5)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

CCT251236

Cell Cycle/DNA Damage Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Cytoskeleton Compound Library

Orally Active Compound Library

Chemical Probe Library

Transcription Factor-Targeted Library

Heterocyclic Compound Library

Metabolic Enzyme Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) CCT251236

Alle HSP Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (5)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

CCT251236 Related Classifications

HY-101026 Related Classifications