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DZ2002 is an orally active, reversible and low-cytotoxic type III SAHH inhibitor (Ki=17.9 nM), with good immunosuppressive activity. DZ2002 prevents the development of experimental dermal fibrosis by reversing the profibrotic phenotype of various cell types. DZ2002 can be used in studies of autoimmune diseases such as lupus syndrome and systemic sclerosis.

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DZ2002 Chemical Structure

DZ2002 Chemical Structure

CAS No. : 33231-14-0

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 374 In-stock
Solution
10 mM * 1 mL in DMSO USD 374 In-stock
Solid
5 mg USD 340 In-stock
10 mg USD 500 In-stock
50 mg USD 1150 In-stock
100 mg USD 1550 In-stock
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500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

DZ2002 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE DZ2002

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

DZ2002 is an orally active, reversible and low-cytotoxic type III SAHH inhibitor (Ki=17.9 nM), with good immunosuppressive activity. DZ2002 prevents the development of experimental dermal fibrosis by reversing the profibrotic phenotype of various cell types. DZ2002 can be used in studies of autoimmune diseases such as lupus syndrome and systemic sclerosis[1][2].

In Vitro

DZ2002 (0.1, 1, 10 µM; 96 h) inhibits the mixed lymphocyte reaction (MLR) response[1].
DZ2002 (0.1, 1, 10 µM; 24 h) inhibits IL-12 and TNF-α production from both mouse peritoneal exudate cells and humanTHP-1 Cells[1].
DZ2002 (0.1, 1, 10 µM; 64 h) inhibits expression of B7 (CD80/CD86) on differentiated THP-1 cells[1].

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

DZ2002 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: BALB/c and C57BL/6 splenocytes (Mitomycin C-pretreated; mixed lymphocyte)
Concentration: 0.1, 1, 10 µM
Incubation Time: 96 h
Result: Suppressed the MLR by 24.5, 42.3, and 46.0% at dosages of 0.1, 1, and 10 µM, respectively.

Cell Viability Assay[1]

Cell Line: TG-stimulated mouse peritoneal macrophages and human THP-1 cells
Concentration: 0.1, 1, 10 µM
Incubation Time: 24 h
Result: Significantly blocked IL-12 p40 production from ~1800 pg/mL in untreated cells to ~850 pg/ml at 10 µM, and drastically reduced the active p70 form from ~1200 pg/mL in untreated cells to ~50 pg/mL.
Reduced TNF-α level by 45%.

Cell Viability Assay[1]

Cell Line: THP-1 cells
Concentration: 0.1, 1, 10 µM
Incubation Time: 64 h
Result: Dramatically down-regulated CD80 and, in particular, CD86 expression in a dose-dependent manner.
In Vivo

DZ2002 (2, 10, 50 mg/kg; i.p.; twice) blocks the DNFB-induced DTH response. (DNFB-induced DTH is a Th1 cell-mediated immune response, in which IL-12 is highly expressed and macrophages have been shown to play an important role)[1].
DZ2002 (0.08, 2 mg/kg; i.p.; single daily for 7 days) significantly suppresses a delayed-type hypersensitivity reaction as well as antibody secretion[1].
DZ2002 (50, 100 mg/kg; p.o.; single daily for 4 weeks) exerts a potent anti-fibrotic effect on dermal fibrosis by reducing the production of collagen, facilitating its degradation and regulating expression of various soluble factors in SSc mice model[2].

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

Animal Model: Male and female BALB/c and C57BL/6 mice (6 to 8-week-old; DNFB-induced ear swelling model)[1].
Dosage: 2, 10, 50 mg/kg
Administration: Intraperitoneal injection; twice (1 h before and 24 h after challenge)
Result: Suppressed ear swelling by 19.1, 28.7, and 33.1%, respectively and in a dose-dependent manner.
Animal Model: Male and female BALB/c and C57BL/6 mice (6 to 8-week-old; DNFB-induced ear swelling model)[1].
Dosage: 0.08, 2 mg/kg
Administration: Intraperitoneal injection; single daily for 7 days.
Result: Inhibited hemolysis by 24.5 and 18.4% at doses of 0.08 and 2 mg/kg, respectively, thus decreasing anti-SRBC antibody production in vivo.
Animal Model: Wild-type C57BL/6 mice (8 to 12-week-old; BLM-induced mice model of SSc)[2].
Dosage: 50, 100 mg/kg
Administration: Oral gavage; single daily for 4 weeks.
Result: Significantly decreased skin thickness and dermal thickness in BLM-induced mice.
Significantly reduced collagen accumulation and α-SMA expression in the dermis of mice and suppressed the mRNA expression of vascular endothelial growth factor (VEGF) in mice skin tissue.
Notably reduced collagen content and mRNA expression of the Col1a1 and Col1a2 while promoting that of the matrix metalloproteinase-13 (MMP-13) in the lesional skin of BLM-induced mice.
Molecular Weight

251.24

Formula

C10H13N5O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OC(C(OC)=O)CCN1C(N=CN=C2N)=C2N=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
Solvent & Solubility
In Vitro: 

DMSO : ≥ 61 mg/mL (242.80 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.9803 mL 19.9013 mL 39.8026 mL
5 mM 0.7961 mL 3.9803 mL 7.9605 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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Concentration
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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)

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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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (9.95 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
  • Protocol 2

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

    Solubility: ≥ 2.5 mg/mL (9.95 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 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 (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

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
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 3.9803 mL 19.9013 mL 39.8026 mL 99.5064 mL
5 mM 0.7961 mL 3.9803 mL 7.9605 mL 19.9013 mL
10 mM 0.3980 mL 1.9901 mL 3.9803 mL 9.9506 mL
15 mM 0.2654 mL 1.3268 mL 2.6535 mL 6.6338 mL
20 mM 0.1990 mL 0.9951 mL 1.9901 mL 4.9753 mL
25 mM 0.1592 mL 0.7961 mL 1.5921 mL 3.9803 mL
30 mM 0.1327 mL 0.6634 mL 1.3268 mL 3.3169 mL
40 mM 0.0995 mL 0.4975 mL 0.9951 mL 2.4877 mL
50 mM 0.0796 mL 0.3980 mL 0.7961 mL 1.9901 mL
60 mM 0.0663 mL 0.3317 mL 0.6634 mL 1.6584 mL
80 mM 0.0498 mL 0.2488 mL 0.4975 mL 1.2438 mL
100 mM 0.0398 mL 0.1990 mL 0.3980 mL 0.9951 mL
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DZ2002 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:

DZ200233231-14-0DZ 2002DZ-2002OtherssplenocytesimmunosuppressionTHP-1macrophageslupus syndromesystemic sclerosisInhibitorinhibitorinhibit

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