1. Metabolic Enzyme/Protease
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  3. SHIN1

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.

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

CAS No. : 2146095-85-2

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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10 mM * 1 mL in DMSO In-stock
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Customer Review

Based on 20 publication(s) in Google Scholar

Other Forms of SHIN1:

Top Publications Citing Use of Products

    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.

    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.

    View All SHMT Isoform Specific Products:

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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]

    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.

    Molecular Weight

    400.47

    Formula

    C24H24N4O2

    CAS No.
    Appearance

    Solid

    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

    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 : 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)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.4971 mL 12.4853 mL 24.9707 mL
    5 mM 0.4994 mL 2.4971 mL 4.9941 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
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    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    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.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • 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.

      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.

    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

    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

    Purity: 98.73%

    References
    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].

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

    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 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
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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:
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    Cat. No.:
    HY-112066
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