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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Based on 1 publication(s) in Google Scholar

Other Forms of (+)SHIN2:

(+)SHIN2 Related Antibodies

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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
Purity & Documentation
References
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(+)SHIN2 Related Classifications

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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.

Keywords:

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

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