SAICAR (Synonyms: Succino-AICAR) |
Catalog No.GC44867
One-Click Copy Product Info
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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.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 3031-95-6
Sample solution is provided at 25 µL, 10mM.
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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.
| 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: | |
| Cas No. | 3031-95-6 | SDF | |
| Synonyms | Succino-AICAR | ||
| Chemical Name | N-[[5-amino-1-(5-O-phosphono-β-D-ribofuranosyl)-1H-imidazol-4-yl]carbonyl]-L-aspartic acid | ||
| Canonical 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 | ||
| Formula | C13H19N4O12P | M.Wt | 454.3 |
| Solubility | Slightly soluble in methanol | Storage | 4°C, away from moisture and light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.2012 mL | 11.0059 mL | 22.0119 mL |
| 5 mM | 440.2 μL | 2.2012 mL | 4.4024 mL |
| 10 mM | 220.1 μL | 1.1006 mL | 2.2012 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 11 reference(s) in Google Scholar.)