2. Metabolic Enzyme/Protease
  3. SHMT
  4. (+)SHIN2

(+)SHIN2 is a serine hydroxymethyltransferase (SHMT) inhibitor, whose target can be traced with 13C-serine. (+)SHIN2 increases survival in NOTCH1-driven mouse primary acute lymphoblastic leukemia (T-ALL) in vivo with a synergistic effect with Methotrexate (HY-14519). (+)SHIN2 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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

(+)SHIN2 Chemical Structure

(+)SHIN2 Chemical Structure

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1 mg USD 320 In-stock
5 mg USD 680 In-stock
10 mg USD 1080 In-stock
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50 mg USD 3650 In-stock
100 mg USD 5800 In-stock
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Based on 1 publication(s) in Google Scholar

Other Forms of (+)SHIN2:

(+)SHIN2 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE (+)SHIN2

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

(+)SHIN2 is a serine hydroxymethyltransferase (SHMT) inhibitor, whose target can be traced with 13C-serine. (+)SHIN2 increases survival in NOTCH1-driven mouse primary acute lymphoblastic leukemia (T-ALL) in vivo with a synergistic effect with Methotrexate (HY-14519)[1]. (+)SHIN2 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

IC50 & Target

Serine hydroxymethyltransferase (SHMT)[1]
In Vitro

(+)SHIN2 (0-10 μM; 24 h) blocks proliferation of HCT116 Ras-driven colon cancer cells, in a stereoselective manner with an IC50 value of 300 nM[1].
(+)SHIN2 (0-100 μM; 48 h) achieves a nearly complete blockade of SHMT activity as evidenced by the decrease in M+1 and M+2 serine, M+2 glycine, and the incorporation of serine-derived glycine and 1C units into ATP, GTP, and dTTP (M+1-M+4 ATP and GTP and M+1 dTTP), and inhibits human T-ALL cell line Molt4 growth with a IC50 value of 89 nM[1].
(+)SHIN2 (2 μM; 24 h) arrests cell cycle at S phase[1].

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

(+)SHIN2 Related Antibodies
In Vivo

(+)SHIN2 (200 mg/kg; i.p.; single dose) shows therapeutic activity in mouse primary T-ALL in vivo[1].

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

Animal Model: Male C57BL/6 mice (10-14 weeks old) with mouse primary T-ALL[1]
Dosage: 200 mg/kg
Administration: Intraperitoneal injection; prepared with 30 mM U-13C-Serine (0.1 μL/min/g; infusion by catheter implanted on the right jugular vein); tested at 8 hr after treatment
Result: Decreased thymus weight and cellularity, which normalized after treatment discontinuation.
Showed generally well tolerated activity with modest hematological toxicity.
Molecular Weight

406.48

Formula

C23H26N4O3
Appearance

Solid

Color

White to light yellow

SMILES

N#CC([C@@]1(C2=CC(C#CCCCO)=CC(CO)=C2)C(C)C)=C(N)OC3=C1C(C)=NN3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (246.01 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 2.4601 mL 12.3007 mL 24.6015 mL
5 mM 0.4920 mL 2.4601 mL 4.9203 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4601 mL 12.3007 mL 24.6015 mL 61.5036 mL
5 mM 0.4920 mL 2.4601 mL 4.9203 mL 12.3007 mL
10 mM 0.2460 mL 1.2301 mL 2.4601 mL 6.1504 mL
15 mM 0.1640 mL 0.8200 mL 1.6401 mL 4.1002 mL
20 mM 0.1230 mL 0.6150 mL 1.2301 mL 3.0752 mL
25 mM 0.0984 mL 0.4920 mL 0.9841 mL 2.4601 mL
30 mM 0.0820 mL 0.4100 mL 0.8200 mL 2.0501 mL
40 mM 0.0615 mL 0.3075 mL 0.6150 mL 1.5376 mL
50 mM 0.0492 mL 0.2460 mL 0.4920 mL 1.2301 mL
60 mM 0.0410 mL 0.2050 mL 0.4100 mL 1.0251 mL
80 mM 0.0308 mL 0.1538 mL 0.3075 mL 0.7688 mL
100 mM 0.0246 mL 0.1230 mL 0.2460 mL 0.6150 mL
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(+)SHIN2 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:

(+)SHIN2SHMTSerine hydroxymethyltransferaseNOTCH1-driven mouseprimary T-ALLMolt4HCT116 Ras-driven colon cancer cellInhibitorinhibitorinhibit

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