Cat. No.: HY-100012

CBR-5884

21 Cited Publications

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Based on 21 publication(s) in Google Scholar

CBR-5884 is an active, selective inhibitor of phosphoglycerate dehydrogenase (PHGDH) with an IC₅₀ of 33 μM. CBR-5884 inhibits de novo serine synthesis in cancer cells and is selectively toxic to cancer cell lines with high serine biosynthetic activity. CBR-5884 selectively inhibits the proliferation of melanoma and breast cancer lines that have a high propensity for serine synthesis.

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Pureté: 98.73%
CAS No.: 681159-27-3
Formule: C₁₄H₁₂N₂O₄S₂
Masse moléculaire:336.39

Stockage:

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

CBR-5884 Chemical Structure

CAS No.: 681159-27-3

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (21)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

PHGDH, serine synthesis^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
MCF-10A	IC₅₀	57.2 μM Compound: 6; CBR-5884	Antiproliferative activity against human MCF-10A cells assessed as reduction in cell viability measured for 72 hrs by CCK-8 assay Antiproliferative activity against human MCF-10A cells assessed as reduction in cell viability measured for 72 hrs by CCK-8 assay	[PMID: 36594670]
MDA-MB-468	IC₅₀	20.9 μM Compound: 6; CBR-5884	Antiproliferative activity against human MDA-MB-468 cells expressing PHGDH assessed as reduction in cell viability measured for 72 hrs by CCK-8 assay Antiproliferative activity against human MDA-MB-468 cells expressing PHGDH assessed as reduction in cell viability measured for 72 hrs by CCK-8 assay	[PMID: 36594670]

In Vitro

CBR-5884 (15 or 30 μM; 3-5 days) selectively inhibits the proliferation of melanoma and breast cancer lines that have a high propensity for serine synthesis.

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

Cell Proliferation Assay^[1]

Cell Line:

Breast and melanoma cell lines
Concentration:

15 or 30 μM
Incubation Time:

3-5 days
Result:

Inhibited the proliferation of melanoma and breast cancer lines.

Chemical Information

CAS No. 681159-27-3
Appearance Solid
Masse moléculaire 336.39
Formule C₁₄H₁₂N₂O₄S₂
Color Light yellow to yellow
SMILES

O=C(C1=C(C)C(SC#N)=C(NC(C2=CC=CO2)=O)S1)OCC
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

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

Publications (21)

All RT-PCRWBCell Proliferation/Viability Assay

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Journal Impact Factor

Cell Metab

Serine metabolism antagonizes antiviral innate immunity by preventing ATP6V0d2-mediated YAP lysosomal degradation. [Abstract]

2021 May 4;33(5):971-987.e6. PMID: 33798471

CBR-5884 purchased from MedChemExpress. Usage Cited in: Cell Metab. 2021 May 4;33(5):971-987.e6. [Abstract]

WT PMs were pretreated with the PHGDH inhibitor CBR-5884 (15 μM or 30 μM) for 12 h and then infected with VSV for western blot detection of p-IRF3(S396), IRF3, p-TBK1(S172), and TBK1.
Immunity

Multiomics analyses reveal a critical role of selenium in controlling T cell differentiation in Crohn's disease. [Abstract]

2021 Aug 10;54(8):1728-1744.e7. PMID: 34343498
Cell Mol Immunol

Serine metabolism orchestrates macrophage polarization by regulating the IGF1-p38 axis. [Abstract]

2022 Nov;19(11):1263-1278. PMID: 36180780

CBR-5884 purchased from MedChemExpress. Usage Cited in: Cell Mol Immunol. 2022 Nov;19(11):1263-1278. [Abstract]

PHGDH inhibits M(IFN-γ) but promotes M(IL-4) polarization through its enzymatic activity. Wild-type bone marrow-derived macrophages (BMDMs) were pretreated with the PHGDH inhibitor CBR-5884 (15 μM) for 12 h and were then stimulated with IFN-γ (100 ng/ml) for 12 h followed by qRT-PCR analysis of M1.

CBR-5884 purchased from MedChemExpress. Usage Cited in: Cell Mol Immunol. 2022 Nov;19(11):1263-1278. [Abstract]

PHGDH inhibits M(IFN-γ) but promotes M(IL-4) polarization through its enzymatic activity. Wild-type bone marrow-derived macrophages (BMDMs) were pretreated with the PHGDH inhibitor CBR-5884 (15 μM) for 12 h and were then stimulated with IFN-γ (100 ng/ml) for 12 h followed by western blot analysis of M1.
Autophagy

Porcine reproductive and respiratory syndrome virus hijacks the non-canonical enzymatic function of PHGDH to arrest autophagic flux for viral replication. [Abstract]

2026 Jun 16:1-20. PMID: 42260976
Nat Commun

Mitochondria preserve an autarkic one-carbon cycle to confer growth-independent cancer cell migration and metastasis. [Abstract]

2022 May 16;13(1):2699. PMID: 35577770
Nat Commun

Identification of metabolic vulnerabilities of receptor tyrosine kinases-driven cancer. [Abstract]

2019 Jun 20;10(1):2701. PMID: 31221965

CBR-5884 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2019 Jun 20;10(1):2701. [Abstract]

Sensitivity to PHGDH inhibition. Cell viability was measured using CCK-8 assay after treatment with CBR5884 (20 µM) for 72 h. Data were means of triplicates; error bars represented SD.
Mol Cell

One-Carbon Metabolism Supports S-Adenosylmethionine and Histone Methylation to Drive Inflammatory Macrophages. [Abstract]

2019 Sep 19;75(6):1147-1160.e5. PMID: 31420217
J Clin Invest

Parkin ubiquitinates phosphoglycerate dehydrogenase to suppress serine synthesis and tumor progression. [Abstract]

2020 Jun 1;130(6):3253-3269. PMID: 32478681
Cell Rep Med

Targeting the noncanonical function of metabolic enzyme PHGDH in driving PD-L1 expression and cancer immune evasion. [Abstract]

2026 Mar 26:102704. PMID: 41905348
Sci Adv

Extracellular serine empowers epidermal proliferation and psoriasis-like symptoms. [Abstract]

2022 Dec 16;8(50):eabm7902. PMID: 36525488
Cell Rep

Macrophage-specific PHGDH protects against MAFLD by suppressing TAK1. [Abstract]

2025 Mar 16;44(3):115426. PMID: 40096087

CBR-5884 purchased from MedChemExpress. Usage Cited in: Cell Rep. 2025 Mar 16;44(3):115426. [Abstract]

CBR-5884 (15 μM; 6 h) increases PA-induced TAK1 activation and proinflammatory cytokine expression.
Sci Signal

Themis is indispensable for IL-2 and IL-15 signaling in T cells. [Abstract]

2022 Feb 15;15(721):eabi9983. PMID: 35167340
Int Immunopharmacol

Artesunate attenuates serum amyloid A-induced M1 macrophage differentiation through the promotion of PHGDH. [Abstract]

2024 Jan 25:127:111462. PMID: 38159553
Front Cell Dev Biol

Serine Metabolism Regulates YAP Activity Through USP7 in Colon Cancer. [Abstract]

2021 May 12:9:639111. PMID: 34055773
Discov Oncol

Preclinical efficacy of CBR-5884 against epithelial ovarian cancer cells by targeting the serine synthesis pathway. [Abstract]

2024 May 11;15(1):154. PMID: 38733440
Technol Cancer Res Treat

Multi-omics Analysis of the Role of PHGDH in Colon Cancer. [Abstract]

2023 Jan-Dec:22:15330338221145994. PMID: 36707056
Onco Targets Ther

Inhibition of Serine Metabolism Promotes Resistance to Cisplatin in Gastric Cancer. [Abstract]

2020 May 29;13:4833-4842. PMID: 32581546
bioRxiv

2025 July 02.
bioRxiv

2023 Aug 22.
Research Square Preprint

2023 Mar 29.
Oxid Med Cell Longev

PHGDH Inhibitor CBR-5884 Inhibits Epithelial Ovarian Cancer Progression via ROS/Wnt/ β-Catenin Pathway and Plays a Synergistic Role with PARP Inhibitor Olaparib. [Abstract]

2022 Sep 5:2022:9029544. PMID: 36105480

Solvant et solubilité

In Vitro:

DMSO : 50 mg/mL (148.64 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

2.9727 mL

14.8637 mL

29.7274 mL

5 mM

0.5945 mL

2.9727 mL

5.9455 mL

10 mM

0.2973 mL

1.4864 mL

2.9727 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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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: ≥ 2.08 mg/mL (6.18 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

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: 15% Cremophor EL 85% Saline

Solubility: 7 mg/mL (20.81 mM); Suspended solution; Need ultrasonic

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (276 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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)
Instruction de manipulation (2659 KB)

Références

[1]. Edouard Mullarky et al. Identification of a small molecule inhibitor of 3-phosphoglycerate dehydrogenase to target serine biosynthesis in cancers Proc Natl Acad Sci U S A, 2016 Feb 16, 113(7):1778-83. [Content Brief]

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	2.9727 mL	14.8637 mL	29.7274 mL	74.3185 mL
	5 mM	0.5945 mL	2.9727 mL	5.9455 mL	14.8637 mL
	10 mM	0.2973 mL	1.4864 mL	2.9727 mL	7.4318 mL
	15 mM	0.1982 mL	0.9909 mL	1.9818 mL	4.9546 mL
	20 mM	0.1486 mL	0.7432 mL	1.4864 mL	3.7159 mL
	25 mM	0.1189 mL	0.5945 mL	1.1891 mL	2.9727 mL
	30 mM	0.0991 mL	0.4955 mL	0.9909 mL	2.4773 mL
	40 mM	0.0743 mL	0.3716 mL	0.7432 mL	1.8580 mL
	50 mM	0.0595 mL	0.2973 mL	0.5945 mL	1.4864 mL
	60 mM	0.0495 mL	0.2477 mL	0.4955 mL	1.2386 mL
	80 mM	0.0372 mL	0.1858 mL	0.3716 mL	0.9290 mL
	100 mM	0.0297 mL	0.1486 mL	0.2973 mL	0.7432 mL

Keywords

CBR-5884

21 Cited Publications

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CBR-5884

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Anti-Breast Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Targeted Diversity Library

Heterocyclic Compound Library

Metabolic Enzyme Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) CBR-5884

Activité biologique

Chemical Information

Publications (21)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

CBR-5884

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Anti-Breast Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Targeted Diversity Library

Heterocyclic Compound Library

Metabolic Enzyme Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) CBR-5884

Activité biologique

Chemical Information

Publications (21)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

CBR-5884 Related Classifications

HY-100012 Related Classifications