CHS-828 (Synonyms: GMX1778)

Name: CHS-828
Brand: MedChemExpress
SKU: HY-10079
Rating: 4.5 (1 reviews)

Cat. No.: HY-10079 Purity: 99.74%: FAQs
Data Sheet SDS COA Handling Instructions

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CHS-828 (GMX1778) is a competitive inhibitor of nicotinamide phosphoribosyltransferase (NAMPT), with an IC₅₀ less than 25 nM. CHS-828 (GMX1778) exerts a cytotoxic effect by decreasing the cellular level of NAD⁺ and exhibits a potent anticancer activity.

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

CHS-828 Chemical Structure

CAS No. : 200484-11-3

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10 mM * 1 mL in DMSO ready for reconstitution	USD 66	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	USD 66	In-stock	Estimated Time of Arrival: December 31
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5 mg	USD 60	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 96	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 201	In-stock	Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

Other Forms of CHS-828:

CHS-828 (nicotinate) Get quote

1 Publications Citing Use of MCE CHS-828

•Clin Transl Sci. 2024 Sep;17(9):e70030. [Abstract]

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Biological Activity
Purity & Documentation
References
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Description

IC₅₀ & Target

IC50: < 25 nM (NAMPT)^[1].

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	IC₅₀	0.001 μM Compound: 7; GMX1778	Inhibition of NAMPT in human A2780 cells assessed as decrease in cell viability after 72 hrs by SRB assay Inhibition of NAMPT in human A2780 cells assessed as decrease in cell viability after 72 hrs by SRB assay	[PMID: 27541271]
A2780	IC₅₀	0.005 μM Compound: 2, GMX1778	Cytotoxicity against human A2780 cells after 72 hrs by SRB assay Cytotoxicity against human A2780 cells after 72 hrs by SRB assay	[PMID: 23617784]
A2780	IC₅₀	0.005 μM Compound: 1, GMX-1778, CHS828	Antiproliferative activity against human A2780 cells after 72 hrs by sulforhodamine B assay Antiproliferative activity against human A2780 cells after 72 hrs by sulforhodamine B assay	[PMID: 24405419]
A2780	IC₅₀	0.005 μM Compound: 1, GMX-1778	Antiproliferative activity against human A2780 cells assessed as growth inhibition after 72 hrs by SRB-based microplate reader analysis Antiproliferative activity against human A2780 cells assessed as growth inhibition after 72 hrs by SRB-based microplate reader analysis	[PMID: 23859118]
A2780	IC₅₀	0.56 nM Compound: 2, CHS828	Cytotoxicity against human A2780 cells assessed as growth inhibition after 72 hrs by WST-1 assay Cytotoxicity against human A2780 cells assessed as growth inhibition after 72 hrs by WST-1 assay	[PMID: 24164086]
DLD-1	IC₅₀	2315 nM Compound: CHS 828	Cytotoxicity against human DLD1 cells after 24 hrs by SRB assay Cytotoxicity against human DLD1 cells after 24 hrs by SRB assay	[PMID: 25147148]
DLD-1	IC₅₀	2315 nM Compound: CHS 828	Anticancer activity against human DLD-1 cells assessed as cell growth inhibition incubated for 24 hrs Anticancer activity against human DLD-1 cells assessed as cell growth inhibition incubated for 24 hrs	[PMID: 35694689]
HA22T cell line	IC₅₀	2067 nM Compound: CHS 828	Cytotoxicity against human HA22T cells after 24 hrs by SRB assay Cytotoxicity against human HA22T cells after 24 hrs by SRB assay	[PMID: 25147148]
HA22T cell line	IC₅₀	2067 nM Compound: CHS 828	Anticancer activity against human HA22T cells assessed as cell growth inhibition incubated for 24 hrs Anticancer activity against human HA22T cells assessed as cell growth inhibition incubated for 24 hrs	[PMID: 35694689]
HepG2	IC₅₀	1245 nM Compound: CHS 828	Cytotoxicity against human HepG2 cells after 24 hrs by SRB assay Cytotoxicity against human HepG2 cells after 24 hrs by SRB assay	[PMID: 25147148]
HepG2	IC₅₀	1245 nM Compound: CHS 828	Anticancer activity against human HepG2 cells assessed as cell growth inhibition incubated for 24 hrs Anticancer activity against human HepG2 cells assessed as cell growth inhibition incubated for 24 hrs	[PMID: 35694689]
HepG2	IC₅₀	18.3 nM Compound: 2, CHS828	Inhibition of NAMPT in human HepG2 cells using [14C]-nicotinamide/PRPP as substrate assessed as formation of [14C]-nicotinamide mononucleotide after 1 hr by liquid scintillation counting analysis Inhibition of NAMPT in human HepG2 cells using [14C]-nicotinamide/PRPP as substrate assessed as formation of [14C]-nicotinamide mononucleotide after 1 hr by liquid scintillation counting analysis	[PMID: 24164086]
HONE1 cell line	IC₅₀	15 nM Compound: CHS 828	Cytotoxicity against human HONE1 cells after 24 hrs by SRB assay Cytotoxicity against human HONE1 cells after 24 hrs by SRB assay	[PMID: 25147148]
HONE1 cell line	IC₅₀	15 nM Compound: CHS 828	Anticancer activity against human HONE1 cell line assessed as cell growth inhibition incubated for 24 hrs Anticancer activity against human HONE1 cell line assessed as cell growth inhibition incubated for 24 hrs	[PMID: 35694689]
MCF7	IC₅₀	1.6 nM Compound: 2, CHS828	Cytotoxicity against human MCF-7 cells assessed as growth inhibition after 72 hrs by WST-1 assay Cytotoxicity against human MCF-7 cells assessed as growth inhibition after 72 hrs by WST-1 assay	[PMID: 24164086]
MCF7	IC₅₀	18 nM Compound: CHS 828	Anticancer activity against human MCF7 cells assessed as cell growth inhibition incubated for 24 hrs Anticancer activity against human MCF7 cells assessed as cell growth inhibition incubated for 24 hrs	[PMID: 35694689]
NUGC	IC₅₀	25 nM Compound: CHS 828	Cytotoxicity against human NUGC cells after 24 hrs by SRB assay Cytotoxicity against human NUGC cells after 24 hrs by SRB assay	[PMID: 25147148]
NUGC	IC₅₀	25 nM Compound: CHS 828	Anticancer activity against human NUGC cells assessed as cell growth inhibition incubated for 24 hrs Anticancer activity against human NUGC cells assessed as cell growth inhibition incubated for 24 hrs	[PMID: 35694689]
PC-3	IC₅₀	4.4 nM Compound: 2; GMX1778	Antiproliferative activity against human PC3 cells assessed as reduction in cell viability incubated for 5 days by Cell-titer Glo reagent based assay Antiproliferative activity against human PC3 cells assessed as reduction in cell viability incubated for 5 days by Cell-titer Glo reagent based assay	[PMID: 28610984]

In Vitro

The phosphoribosyltransferase activity of recombinant NAMPT was sensitive to inhibition by CHS-828 (GMX1778) (IC50 < 25 nM) whereas the adenyltransferase activity of recombinant NMNAT1 was not. The Kd of recombinant NAMPT for GMX1778 labeled with a fluorescent tag (CHS-828 (GMX1778)-Alexa Fluor) was 120 nM. Overexpression of wild-type NAMPT was able to maintain a certain level of NAD+ under conditions of challenge with 3 nM GMX1778, but this effect was lost when cells were exposed to 300 nM CHS-828 (GMX1778)^[1]. CHS-828 (GMX1778) increases intracellular ROS in cancer cells by elevating the superoxide level while decreasing the intracellular NAD(+) level. Notably, CHS-828 (GMX1778) treatment does not induce ROS in normal cells. CHS-828 (GMX1778)-induced ROS can be diminished by adding nicotinic acid (NA) in a NA phosphoribosyltransferase 1 (NAPRT1)-dependent manner^[2].

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

In Vivo

A 4-h iv infusion of NA (120 mg/kg of body weight) did not adversely affect the antitumor activity of a 24-h iv infusion of CHS-828 (GMX1778) at a dose of 150 mg/kg or 650 mg/kg in the NAPRT1-deficient xenograft experiments. CHS-828 (GMX1778) at 650 mg/kg is above the maximum tolerated dose. The administration of NA as a 4-h iv infusion immediately following treatment with 750 mg/kg CHS-828 (GMX1778) reduced the mortality associated with toxic doses of GMX1777^[2].

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

Clinical Trial

Molecular Weight

371.86

Formula

C₁₉H₂₂ClN₅O

CAS No.

200484-11-3

Appearance

Solid

Color

White to off-white

SMILES

N#CN/C(NCCCCCCOC1=CC=C(C=C1)Cl)=N\C2=CC=NC=C2

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 : ≥ 39 mg/mL (104.88 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	2.6892 mL	13.4459 mL	26.8918 mL
5 mM	0.5378 mL	2.6892 mL	5.3784 mL
10 mM	0.2689 mL	1.3446 mL	2.6892 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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: ≥ 2.5 mg/mL (6.72 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)

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: 99.74%

Select Batch:

Data Sheet (271 KB) SDS (393 KB)

COA (244 KB) LCMS (272 KB)

Handling Instructions (2659 KB)

References

[1]. Watson M, et al. The small molecule GMX1778 is a potent inhibitor of NAD+ biosynthesis: strategy for enhanced therapy in nicotinic acid phosphoribosyltransferase 1-deficient tumors. Mol Cell Biol. 2009 Nov;29(21):5872-88. [Content Brief]

[2]. Cerna D, et al. Inhibition of nicotinamide phosphoribosyltransferase (NAMPT) activity by small molecule GMX1778 regulates reactive oxygen species (ROS)-mediated cytotoxicity in a p53- and nicotinic acid phosphoribosyltransferase1 (NAPRT1)-dependent manner. J Biol Chem. 2012 Jun 22;287(26):22408-17. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.6892 mL	13.4459 mL	26.8918 mL	67.2296 mL
	5 mM	0.5378 mL	2.6892 mL	5.3784 mL	13.4459 mL
	10 mM	0.2689 mL	1.3446 mL	2.6892 mL	6.7230 mL
	15 mM	0.1793 mL	0.8964 mL	1.7928 mL	4.4820 mL
	20 mM	0.1345 mL	0.6723 mL	1.3446 mL	3.3615 mL
	25 mM	0.1076 mL	0.5378 mL	1.0757 mL	2.6892 mL
	30 mM	0.0896 mL	0.4482 mL	0.8964 mL	2.2410 mL
	40 mM	0.0672 mL	0.3361 mL	0.6723 mL	1.6807 mL
	50 mM	0.0538 mL	0.2689 mL	0.5378 mL	1.3446 mL
	60 mM	0.0448 mL	0.2241 mL	0.4482 mL	1.1205 mL
	80 mM	0.0336 mL	0.1681 mL	0.3361 mL	0.8404 mL
	100 mM	0.0269 mL	0.1345 mL	0.2689 mL	0.6723 mL

CHS-828 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:

CHS-828200484-11-3GMX1778CHS828CHS 828GMX 1778GMX-1778NAMPTApoptosisNicotinamide phosphoribosyl transferasePBEFVisfatinpre-B cell-enhancing factorPre-B cell colony enhancing factorInhibitorinhibitorinhibit

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CHS-828 (Synonyms: GMX1778)

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CHS-828 Related Antibodies

1 Publications Citing Use of MCE CHS-828

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Complete Stock Solution Preparation Table

CHS-828 Related Classifications

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