GLPBio

SAICAR

Catalog No.: GC44867Purity:>99.00%Synonyms: Succino-AICAR
COASDSData Sheet
SAICAR is an intermediate metabolite in the de novo synthesis pathway of purine nucleotides. SAICAR can selectively activate the pyruvate kinase M2 isoform (PKM2; EC50=0.3mM) in an isoform-specific manner.

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SAICAR
Cas No.: 3031-95-6
10mM (in 1mL DMSO)In Stock
$612.00
1
500 µgIn Stock
$180.00
1
1 mgIn Stock
$306.00
1
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Description

SAICAR is an intermediate metabolite in the de novo synthesis pathway of purine nucleotides. SAICAR can selectively activate the pyruvate kinase M2 isoform (PKM2; EC50=0.3mM) in an isoform-specific manner[1-2]. The accumulation of SAICAR induces nuclear translocation of PKM2, phosphorylates and activates Erk1/2 signaling via PKM2, thereby promoting cell proliferation, including cancer cells[3-4].

In vitro, treatment of HeLa cells with SAICAR (0.5mM) for 30 minutes, SAICAR promotes phosphorylation of histone H3 and enhances c-Myc gene expression[5]. Under glucose deprivation conditions, exposure of HeLa, A549, U87, and H1299 cells to SAICAR (0–0.5mM) for 30 minutes. SAICAR promotes cancer cell survival under glucose-limited conditions while regulating glucose uptake and lactate production[6].

In vivo, SAICAR (100μM; 100μL) was topically injected into wounds of db/db diabetic mice once daily for 7 consecutive days. SAICAR significantly increased COL17 expression at the wound edge and the proportion of PCNA-positive proliferating epithelial cells, promoted wound re-epithelialization, accelerated wound closure, and improved delayed healing phenotypes[7].

References:
[1] Yan M, Chakravarthy S, Tokuda JM, et al. Succinyl-5-aminoimidazole-4-carboxamide-1-ribose 5'-Phosphate (SAICAR) Activates Pyruvate Kinase Isoform M2 (PKM2) in Its Dimeric Form. Biochemistry. 2016 Aug 23;55(33):4731-6.
[2] Ray SP, Duval N, Wilkinson TG 2nd, et al. Inherent properties of adenylosuccinate lyase could explain S-Ado/SAICAr ratio due to homozygous R426H and R303C mutations. Biochim Biophys Acta. 2013 Aug;1834(8):1545-53.
[3] Huo A, Xiong X. PAICS as a potential target for cancer therapy linking purine biosynthesis to cancer progression. Life Sci. 2023 Oct 15;331:122070.
[4] Yan M, Chakravarthy S, Tokuda JM, et al. Succinyl-5-aminoimidazole-4-carboxamide-1-ribose 5'-Phosphate (SAICAR) Activates Pyruvate Kinase Isoform M2 (PKM2) in Its Dimeric Form. Biochemistry. 2016 Aug 23;55(33):4731-6.
[5] Keller KE, Doctor ZM, Dwyer ZW, et al. SAICAR induces protein kinase activity of PKM2 that is necessary for sustained proliferative signaling of cancer cells. Mol Cell. 2014 Mar 6;53(5):700-9.
[6] Keller KE, Tan IS, Lee YS. SAICAR stimulates pyruvate kinase isoform M2 and promotes cancer cell survival in glucose-limited conditions. Science. 2012 Nov 23;338(6110):1069-72.
[7] Liu Y, Ho C, Wen D, et al. PKM2-mediated collagen XVII expression is critical for wound repair. JCI Insight. 2025 Jan 21;10(4):e184457.

Protocol

Cell experiment [1]:

Cell lines

HeLa cells (human cervical cancer cell line), A549 (human lung cancer cell line), U87 (human glioblastoma cell line), and H1299 (non-small cell lung cancer cell line)

Preparation Method

HeLa cells were maintained in Dulbecco’s minimal essential medium (DMEM) supplemented with 10% dialyzed fetal bovine serum (FBS) at 37°C, 5% CO₂. Cells were subjected to glucose deprivation by incubation in glucose-free DMEM and treated with SAICAR (0–0.5mM) for 0.5 hours.

Reaction Conditions

0–0.5mM; 0.5h

Applications

SAICAR promoted the survival of cancer cells under glucose-limited conditions while regulating glucose uptake and lactate production.

Animal experiment [2]:

Animal models

C57BL/6J mice and C57BL/6J-db/db mice

Preparation Method

Mice were subjected to full-thickness excisional wounds (8mm diameter) on the dorsal skin. SAICAR (100μM in 100μL 0.9% saline) was topically injected around the wound edge once daily from post-wound day (PWD) 1 until tissue collection. Control groups received vehicle (0.9% saline with DMSO).

Dosage form

100μM; topical injection; daily for 7 days.

Applications

SAICAR treatment significantly accelerated wound closure and re-epithelialization in both normal and diabetic mice by promoting PKM2 nuclear translocation, STAT3 phosphorylation, and COL17 expression. SAICAR enhanced keratinocyte proliferation (increased PCNA-positive cells) and restored impaired healing in diabetic wounds, demonstrating therapeutic potential for chronic wound repair

References:
[1] Keller KE, Tan IS, Lee YS. SAICAR stimulates pyruvate kinase isoform M2 and promotes cancer cell survival in glucose-limited conditions. Science. 2012 Nov 23;338(6110):1069-72.
[2] Liu Y, Ho C, Wen D, et al. PKM2-mediated collagen XVII expression is critical for wound repair. JCI Insight. 2025 Jan 21;10(4):e184457.

Product Documents

Purity:>99.00%Appearance:A solid
COASDSData Sheet

Chemical Properties

CAS No.
3031-95-6
Synonyms
Succino-AICAR
Chemical Name
N-[[5-amino-1-(5-O-phosphono-β-D-ribofuranosyl)-1H-imidazol-4-yl]carbonyl]-L-aspartic acid
SMILES
NC1=C(C(N[C@H](C(O)=O)CC(O)=O)=O)N=CN1[C@H]2[C@H](O)[C@H](O)[C@@H](COP(O)(O)=O)O2
Molecular Formula
C13H19N4O12P
Molecular Weight
454.3
Solubility
Slightly soluble in methanol
Storage
4°C, away from moisture and light
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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