Art. -Nr.: HY-112066

SHIN1

(Synonyms: RZ-2994)

23 Cited Publications

Kundenbewertung

Based on 23 publication(s) in Google Scholar

SHIN1 (RZ-2994) is a human serine hydroxymethyltransferse 1 and 2 (SHMT1/2) inhibitor with IC₅₀s of 5 and 13 nM, respectively, in an in vitro assay.

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Reinheit: 98.63%
CAS. Nr.: 2146095-85-2
Formel: C₂₄H₂₄N₄O₂
Molecular Weight:400.47

Speicherung:

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

SHIN1 Chemical Structure

CAS. Nr.: 2146095-85-2

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Publications (23)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

SHIN1 (RZ-2994) is a human serine hydroxymethyltransferse 1 and 2 (SHMT1/2) inhibitor with IC₅₀s of 5 and 13 nM, respectively, in an in vitro assay.

IC₅₀ & Target

IC50: 5 nM (SHMT1), 13 nM (SHMT2)^[1]

Alle SHMT Isoform-spezifische Produkte anzeigen :

SHMT1
SHMT2

In Vitro

SHIN1 (RZ-2994) inhibits human SHIN1 SHMT1/2 with IC₅₀s of 5 and 13 nM, respectively in an in vitro assay. SHIN1 inhibits the growth of SHMT2 deletion HCT-116 cells with an IC₅₀ of 10 nM. SHIN1 (RZ-2994) inhibits SHMT1/2 in HCT-116 cells. SHIN1 (RZ-2994) is particularly active against B-cell malignancies. SHIN1 blocks cell growth through a progressive depletion of purines, leading to loss of nucleotide triphosphates^[1].

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

Chemical Information

CAS. Nr. 2146095-85-2
Appearance Solid
Molecular Weight 400.47
Formel C₂₄H₂₄N₄O₂
Color White to off-white
SMILES

OCC1=CC(C2=CC=CC=C2)=CC(C3(C(C(C)=NN4)=C4OC(N)=C3C#N)C(C)C)=C1
Synonyms

RZ-2994
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Publications (23)

All In Vivo Efficacy StudyCell Imaging/StainingBio/Physico-chemical AssayCell Proliferation/Viability AssayHistological Imaging/Staining

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Journal Impact Factor

Mol Cancer

ZNF526 drives tumor growth by enhancing SHMT1-dependent serine metabolism and antioxidant capability in TNBC. [Abstract]

2025 Nov 20;24(1):295. PMID: 41267037

SHIN1 purchased from MedChemExpress. Usage Cited in: Mol Cancer. 2025 Nov 20;24(1):295. [Abstract]

SHIN1 (10 nM; 48 h) impaired ZNF526's ability to suppress ROS levels in MDA-MB-468 cells.

SHIN1 purchased from MedChemExpress. Usage Cited in: Mol Cancer. 2025 Nov 20;24(1):295. [Abstract]

SHIN1 (10 nM; 72 h) profoundly suppressed ZNF526-mediated growth promotion in MDA-MB-231 cells.
Nat Metab

Concurrent loss of LKB1 and KEAP1 enhances SHMT-mediated antioxidant defence in KRAS-mutant lung cancer. [Abstract]

2024 Jul;6(7):1310-1328. PMID: 38877143

SHIN1 purchased from MedChemExpress. Usage Cited in: Nat Metab. 2024 Jul;6(7):1310-1328. [Abstract]

Growth of KL xenografts following treatment with SHIN1 (100 mg/kg; i.p.; once daily) or vehicle (Veh).

SHIN1 purchased from MedChemExpress. Usage Cited in: Nat Metab. 2024 Jul;6(7):1310-1328. [Abstract]

SHIN1 (100 mg/kg; i.p.; once daily) inhibited SHMT activity and decreased incorporation of ¹³C into glycine from [U-¹³C] serine in SHIN1-injected mice than in control mice.

SHIN1 purchased from MedChemExpress. Usage Cited in: Nat Metab. 2024 Jul;6(7):1310-1328. [Abstract]

SHIN1 (100 mg/kg; i.p.; once daily) increased apoptosis and decreased proliferation of KL tumours in athymic nude mice.
Cell Mol Immunol

Vitamin B6 regulates IL-33 homeostasis to alleviate type 2 inflammation. [Abstract]

2023 Jul;20(7):794-807. PMID: 37217797
Mol Cell

Microprotein SMIM26 drives oxidative metabolism via serine-responsive mitochondrial translation. [Abstract]

2025 Jul 17;85(14):2759-2775.e12. PMID: 40578345
Mol Cell

PAICS ubiquitination recruits UBAP2 to trigger phase separation for purinosome assembly. [Abstract]

2023 Nov 16;83(22):4123-4140.e12. PMID: 37848033
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

SHMT2 deficiency disrupts transcriptional regulation through homocysteine-mediated suppression of histone lactylation in Huntington's disease models. [Abstract]

2026 Mar 10;136(9):e196094. PMID: 41805887
J Clin Invest

Therapeutic targeting of metabolic vulnerabilities in cancers with MLL3/4-COMPASS epigenetic regulator mutations. [Abstract]

2023 Jul 3;133(13):e169993. PMID: 37252797
Sci Adv

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

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

Targeting serine/glycine metabolism to attenuate IFN-γ- and IL-22-driven inflammation and hyperproliferation in psoriasis. [Abstract]

2026 May 8;12(1):289. PMID: 42103703
Cell Mol Life Sci

Lys-63-specific deubiquitinase BRCC36 enhances the sensitivity of multiple myeloma cells to lenalidomide by inhibiting lysosomal degradation of cereblon. [Abstract]

2024 Aug 13;81(1):349. PMID: 39136771
Cancer Metab

The conversion of formate into purines stimulates mTORC1 leading to CAD-dependent activation of pyrimidine synthesis. [Abstract]

2020 Sep 21:8:20. PMID: 32974014
Commun Biol

Serine hydroxymethyltransferase as a potential target of antibacterial agents acting synergistically with one-carbon metabolism-related inhibitors. [Abstract]

2022 Jun 23;5(1):619. PMID: 35739195
J Biol Chem

Mitochondrial folate metabolism-mediated α-linolenic acid exhaustion masks liver fibrosis resolution. [Abstract]

2023 Jul;299(7):104909. PMID: 37307917
J Reprod Dev

Supplementation with serine-enriched non-essential amino acids from minimum essential medium promotes blastocyst development of in vitro-fertilized bovine embryos. [Abstract]

2025 Feb 5;71(1):55-61. PMID: 39756999
Res Sq

2026 Jun 15.
Harvard University

2026.
Res Sq

2026 Mar 5.
bioRxiv

2025 July 11.
Biomed Pharmacother

Cereblon mediates macrophage differentiation and microglial phagocytosis by regulating calpain protease activity. [Abstract]

2024 Nov:180:117606. PMID: 39454366
bioRxiv

Phosphoglycerate mutase regulates Treg differentiation through control of serine synthesis and one-carbon metabolism. [Abstract]

2024 Jun 28:2024.06.23.600101. PMID: 38979375
Research Square Preprint

2023 Jul 7.
Research Square Preprint

2023 Mar 29.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 66.67 mg/mL (166.48 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

2.4971 mL

12.4853 mL

24.9707 mL

5 mM

0.4994 mL

2.4971 mL

4.9941 mL

10 mM

0.2497 mL

1.2485 mL

2.4971 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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 1.25 mg/mL (3.12 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 1.25 mg/mL (3.12 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

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

Solubility: ≥ 1.25 mg/mL (3.12 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 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 (12.5 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: 50% PEG300 50% Saline

Solubility: 2.5 mg/mL (6.24 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

Protokoll

Cell Assay^[1]

For proliferation assays, HCT-116 cells are treated with SHIN1 (1, 10, 100, 1000, 10000 nM) for 24-72 hours. Cell number was counted directly using Trypan blue and the Countess system^[1].

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 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)
Handling Instructions (2659 KB)

Verweise

[1]. Ducker GS, et al. Human SHMT inhibitors reveal defective glycine import as a targetable metabolic vulnerability of diffuse large B-cell lymphoma. Proc Natl Acad Sci U S A. 2017 Oct 24;114(43):11404-11409. [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	2.4971 mL	12.4853 mL	24.9707 mL	62.4266 mL
	5 mM	0.4994 mL	2.4971 mL	4.9941 mL	12.4853 mL
	10 mM	0.2497 mL	1.2485 mL	2.4971 mL	6.2427 mL
	15 mM	0.1665 mL	0.8324 mL	1.6647 mL	4.1618 mL
	20 mM	0.1249 mL	0.6243 mL	1.2485 mL	3.1213 mL
	25 mM	0.0999 mL	0.4994 mL	0.9988 mL	2.4971 mL
	30 mM	0.0832 mL	0.4162 mL	0.8324 mL	2.0809 mL
	40 mM	0.0624 mL	0.3121 mL	0.6243 mL	1.5607 mL
	50 mM	0.0499 mL	0.2497 mL	0.4994 mL	1.2485 mL
	60 mM	0.0416 mL	0.2081 mL	0.4162 mL	1.0404 mL
	80 mM	0.0312 mL	0.1561 mL	0.3121 mL	0.7803 mL
	100 mM	0.0250 mL	0.1249 mL	0.2497 mL	0.6243 mL

Keywords

SHIN1

23 Cited Publications

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SHIN1

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Heterocyclic Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) SHIN1

Alle SHMT Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (23)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

SHIN1

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Heterocyclic Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) SHIN1

Alle SHMT Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (23)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

SHIN1 Related Classifications

HY-112066 Related Classifications