1. Cell Cycle/DNA Damage
  2. Zinc Finger Protein
  3. iZMYND8-34

iZMYND8-34 is a ZMYND8 inhibitor with an IC50 of 0.66 μM. iZMYND8-34 inhibits the binding of H3K4me1–H3K14ac peptide to the ZMYND8 protein. iZMYND8-34 inhibits ZMYND8’s histone recognition. iZMYND8-34 blocks neuroendocrine prostate cancer development.

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

iZMYND8-34

iZMYND8-34 Chemical Structure

CAS No. : 1358901-59-3

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Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

  • References

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Description

iZMYND8-34 is a ZMYND8 inhibitor with an IC50 of 0.66 μM. iZMYND8-34 inhibits the binding of H3K4me1–H3K14ac peptide to the ZMYND8 protein. iZMYND8-34 inhibits ZMYND8’s histone recognition. iZMYND8-34 blocks neuroendocrine prostate cancer development[1].

In Vitro

iZMYND8-34 binds to recombinant ZMYND8-PBP with a dissociation constant (Kd) of 1.73 μM[1].
iZMYND8-34 exerts negligible effects on luminal C4-2 and 22Rv1 cells, but significantly inhibits the growth of NE1.3 cells, TKO and ST88 organoids[1].

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

In Vivo

iZMYND8-34 (10 mg/kg; i.p.; every 2 days; 6 weeks) potently inhibits NEPC development, extends survival, reduces tumor burden, and blocks metastasis in TKO mice with spontaneous NEPC[1].
iZMYND8-34 (10 mg/kg; i.p.; every 2 days; 4 weeks; in combination with Enzalutamide (HY-70002)) potently inhibits ADT-induced NEPC transdifferentiation in mice, reduces tumor growth, and extends survival in the LTL-331 PDX model[1].

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

Animal Model: C57BL/6 (male; 6-week-old; genetically engineered: ProbasinCre/+; Ptenflox/flox; Trp53flox/flox; Rb1flox/flox)[1]
Dosage: 10 mg/kg
Administration: i.p.; every 2 days; 6 weeks
Result: Significantly extended mouse survival (log-rank test, P < 0.0001).
Reduced end-stage tumor volume.
Shifted tumor histology from predominantly NEPC to adenocarcinoma or prostatic intraepithelial neoplasia.
Eliminated NEPC cell populations (CHGA+KRT8-AR- cells).
Reduced expression of NE markers (SYP, CHGA).
Restored AR expression.
Completely prevented metastatic spread to lymph nodes, lungs, and liver.
Animal Model: NSG (male; 6-week-old; castrated; subcutaneous implantation of LTL-331 PDX)[1]
Dosage: 10 mg/kg (in combination with enzalutamide)
Administration: i.p.; every 2 days; 4 weeks
Result: Significantly inhibited LTL-331 PDX tumor growth.
Extended mouse survival.
Reduced the percentage of CHGA+ NEPC cells.
Decreased Ki67+ proliferating cells compared to vehicle control.
Molecular Weight

449.42

Formula

C22H19N5O6

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=C2N(C)C(N(C3=CC=C(OCO4)C4=C3)C2=NC(C5=CC=CC(OCC)=C5O)=N1)=O)N

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 : 10 mg/mL (22.25 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 2.2251 mL 11.1255 mL 22.2509 mL
5 mM 0.4450 mL 2.2251 mL 4.4502 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.

  • Molarity Calculator

  • Dilution Calculator

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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: ≥ 1 mg/mL (2.23 mM); Clear solution

    This protocol yields a clear solution of ≥ 1 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 (10.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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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: 98.89%

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, 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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2251 mL 11.1255 mL 22.2509 mL 55.6273 mL
5 mM 0.4450 mL 2.2251 mL 4.4502 mL 11.1255 mL
10 mM 0.2225 mL 1.1125 mL 2.2251 mL 5.5627 mL
15 mM 0.1483 mL 0.7417 mL 1.4834 mL 3.7085 mL
20 mM 0.1113 mL 0.5563 mL 1.1125 mL 2.7814 mL
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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.

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Product Name:
iZMYND8-34
Cat. No.:
HY-403538
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