2. Apoptosis
  3. Bcl-2 Family Apoptosis
  4. CLZ-8

CLZ-8 (Compound 8) is an orally active Mcl-1-PUMA interface inhibitor, with a Ki 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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CLZ-8 Chemical Structure

CLZ-8 Chemical Structure

CAS No. : 678158-55-9

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 132 In-stock
Solution
10 mM * 1 mL in DMSO USD 132 In-stock
Solid
5 mg USD 120 In-stock
10 mg USD 200 In-stock
25 mg USD 400 In-stock
50 mg USD 640 In-stock
100 mg USD 1000 In-stock
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Based on 1 publication(s) in Google Scholar

CLZ-8 Related Antibodies

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Description

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

IC50 & Target[1]

Mcl-1

0.3 μM (Ki)

PUMA

 

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.

CLZ-8 Related Antibodies

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.
Molecular Weight

393.50

Formula

C22H23N3O2S
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

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

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5413 mL 12.7065 mL 25.4130 mL
5 mM 0.5083 mL 2.5413 mL 5.0826 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, 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

  • Dilution Calculator

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

Mass
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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C2

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Volume (final)

V2

In Vivo:

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

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

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.85%

COA (250 KB) LCMS (264 KB)

Handling Instructions (2659 KB)
References

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, 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 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:

CLZ-8678158-55-9CLZ8CLZ 8Bcl-2 FamilyApoptosisradioprotective abilityHUVECshuman umbilical vein endothelial cellsInhibitorinhibitorinhibit

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