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Chemical Structure| 2146095-85-2 Chemical Structure| 2146095-85-2

Structure of SHIN1
CAS No.: 2146095-85-2

Chemical Structure| 2146095-85-2

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

Synonyms: RZ-2994

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Product Details of SHIN1

CAS No. :2146095-85-2
Formula : C24H24N4O2
M.W : 400.47
SMILES Code : N#CC(C1(C2=CC(C3=CC=CC=C3)=CC(CO)=C2)C(C)C)=C(N)OC4=C1C(C)=NN4
Synonyms :
RZ-2994
MDL No. :MFCD31657406

Safety of SHIN1

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319
Precautionary Statements:P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Myeloma cell lines (LP1, RPMI-8226, ARH-77, U266) 10 µM 24 hours To investigate the effect of SHIN1 on CRBN protein levels in myeloma cells. Results showed that SHIN1 increased CRBN protein levels. Cell Mol Life Sci. 2024 Aug 13;81(1):349
HeLa cells 10 µM 24 hours To investigate the effect of SHIN1 on CRBN protein levels. Results showed that SHIN1 significantly increased CRBN protein levels. Cell Mol Life Sci. 2024 Aug 13;81(1):349
LUAD cells (A549 and H1299) 10 µM 48 hours Evaluate the effect of SHIN1 on cell viability, results showed SHIN1 significantly inhibited LUAD cells Adv Sci (Weinh). 2024 May;11(18):e2307834
Human bronchial epithelial cells (BEAS-2B) 10 µM 48 hours Evaluate the effect of SHIN1 on cell viability, results showed SHIN1 had a low inhibition rate on human bronchial epithelial cells Adv Sci (Weinh). 2024 May;11(18):e2307834
HEL cells 1.25 µM 6 days SHIN1 treatment up-regulated ALAS2 expression, promoting erythroid differentiation. Sci Adv. 2024 Feb 2;10(5):eadj9479
MEL cells 1.25 µM 6 days SHIN1 treatment resulted in AICAR accumulation and induced erythroid differentiation. Sci Adv. 2024 Feb 2;10(5):eadj9479
K562 cells 1.25 µM 6 days SHIN1 inhibits SHMT1 and SHMT2, lowers intracellular levels of reduced folate, mimics nutritional folate deprivation, increases AICAR levels, and induces erythroid differentiation. Sci Adv. 2024 Feb 2;10(5):eadj9479
Lung adenocarcinoma organoids 20 µM 7 days Evaluate the effect of SHIN1 on organoid growth, results showed SHIN1 significantly inhibited the growth of lung adenocarcinoma organoids Adv Sci (Weinh). 2024 May;11(18):e2307834

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Waxworm (Galleria mellonella) Waxworm infection model Injection 0.5 µg/waxworm Single injection, observed up to 80 hours To evaluate the protective effect of SHIN1 against S. aureus USA300 infection Int J Mol Sci. 2020 Nov 30;21(23):9135
Nude mice NCI-H1299 xenograft model Intraperitoneal injection 100 mg/kg 3 times per week for 3-4 weeks Evaluate the tumor inhibitory effect of SHIN1 on FRAT1-overexpressing tumors, showing increased sensitivity in FRAT1-overexpressing tumors. Sci Adv. 2022 May 20;8(20):eabm8786
BALB/c nude mice LP1 cell xenograft model Intraperitoneal injection 50 mg/kg/day Every other day for three times To investigate the effect of SHIN1 and Len combination therapy on myeloma xenograft model. Results showed that SHIN1 and Len combination significantly decreased LP1 tumor growth rate. Cell Mol Life Sci. 2024 Aug 13;81(1):349

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.50mL

0.50mL

0.25mL

12.49mL

2.50mL

1.25mL

24.97mL

4.99mL

2.50mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2
 

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