Art. -Nr.: HY-122627

CLZ-8

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CLZ-8 (Compound 8) is an orally active Mcl-1-PUMA interface inhibitor, with a K_i of 0.3 μM. CLZ-8 exhibits dual activity on reduce PUMA-dependent apoptosis while deactivating Mcl-1-mediated anti-apoptosis in cancer cells.

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Reinheit: 99.14%
CAS. Nr.: 678158-55-9
Formel: C₂₂H₂₃N₃O₂S
Molecular Weight:393.50

Speicherung:

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

CLZ-8 Chemical Structure

CAS. Nr.: 678158-55-9

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

Mcl-1

0.3 μM (Ki)

PUMA

Alle Bcl-2 Family Isoform-spezifische Produkte anzeigen :

In Vitro

CLZ-8 (Compound 8) (0-160 μM, 48 h) significantly inhibits PUMA-dependent apoptosis^[1].
CLZ-8 (0-1 μM, 2 h) significantly enhance the irradiated cell viability in a dose-dependent manner, provides significant protection for HUVECs, and inhibits overexpressed PUMA^[2].
CLZ-8 (0-1 μM, 24 h) attenuates the radiation-induced apoptosis^[2].
CLZ-8 (1 μM, 2 h) protects HUVECs from DNA breaks^[2].

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

Apoptosis Analysis^[1]^[2]

Cell Line:

DLD-1 cells or HUVEC cells
Concentration:

0-160 μM (DLD-1) or 0.01, 0.1 and 1 μM (HUVECs)
Incubation Time:

48 h (DLD-1) or 24 h (HUVECs)
Result:

Significantly inhibited PUMA-dependent apoptosis with an IC₅₀ of 38.93 ± 0.91 μM.
Attenuated the radiation-induced apoptosis.

Western Blot Analysis^[2]

Cell Line:

HUVEC cells
Concentration:

0.001, 0.01, 0.1 and 1 μM
Incubation Time:

2 h
Result:

Suppressed induction of PUMA after radiation, significantly decreased the level of p53.
Significantly decreased the level of MCL-1 and increased the level of Bcl-XL.

In Vivo

CLZ-8 (0-400 mg/kg; i.g.; once) shows powerful anti-radiation effects in mice^[2].

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

Animal Model:

6-8 week-old male BALB/c mice^[2]
Dosage:

100, 200 and 400 mg/kg
Administration:

Intragastric administration, once, 30 min prior to irradiation
Result:

Increased the survival rate of irradiated mice.

Chemical Information

CAS. Nr. 678158-55-9
Appearance Solid
Molecular Weight 393.50
Formel C₂₂H₂₃N₃O₂S
Color Light yellow to yellow
SMILES

O=C1N=C(N2CCN(CCO)CC2)S/C1=C\C3=CC=C(C4=CC=CC=C4)C=C3
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

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 50 mg/mL (127.06 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

2.5413 mL

12.7065 mL

25.4130 mL

5 mM

0.5083 mL

2.5413 mL

5.0826 mL

10 mM

0.2541 mL

1.2706 mL

2.5413 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 90% Corn Oil

Solubility: ≥ 0.83 mg/mL (2.11 mM); Clear solution

This protocol yields a clear solution of ≥ 0.83 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 (8.3 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 (275 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)

Verweise

[1]. Liu J, et al. Targeting the apoptotic Mcl-1-PUMA interface with a dual-acting compound. Oncotarget. 2017 Apr 20;8(33):54236-54242. [Content Brief]

[2]. Feng T, et al. CLZ-8, a potent small-molecular compound, protects radiation-induced damages both in vitro and in vivo. Environ Toxicol Pharmacol. 2018 Jul;61:44-51.

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	2.5413 mL	12.7065 mL	25.4130 mL	63.5324 mL
	5 mM	0.5083 mL	2.5413 mL	5.0826 mL	12.7065 mL
	10 mM	0.2541 mL	1.2706 mL	2.5413 mL	6.3532 mL
	15 mM	0.1694 mL	0.8471 mL	1.6942 mL	4.2355 mL
	20 mM	0.1271 mL	0.6353 mL	1.2706 mL	3.1766 mL
	25 mM	0.1017 mL	0.5083 mL	1.0165 mL	2.5413 mL
	30 mM	0.0847 mL	0.4235 mL	0.8471 mL	2.1177 mL
	40 mM	0.0635 mL	0.3177 mL	0.6353 mL	1.5883 mL
	50 mM	0.0508 mL	0.2541 mL	0.5083 mL	1.2706 mL
	60 mM	0.0424 mL	0.2118 mL	0.4235 mL	1.0589 mL
	80 mM	0.0318 mL	0.1588 mL	0.3177 mL	0.7942 mL
	100 mM	0.0254 mL	0.1271 mL	0.2541 mL	0.6353 mL

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CLZ-8

Apoptosis Compound Library

Anti-Cancer Compound Library

Covalent Screening Library

Orally Active Compound Library

Anti-Blood Cancer Compound Library

Mitochondria-Targeted Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Mitophagy Compound Library

Bioactive Compound Library Max

Covalent Screening Library Plus

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Alle Bcl-2 Family Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

CLZ-8

Apoptosis Compound Library

Anti-Cancer Compound Library

Covalent Screening Library

Orally Active Compound Library

Anti-Blood Cancer Compound Library

Mitochondria-Targeted Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Mitophagy Compound Library

Bioactive Compound Library Max

Covalent Screening Library Plus

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Alle Bcl-2 Family Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

CLZ-8 Related Classifications

HY-122627 Related Classifications