SAICAR
(Synonyms: Succino-AICAR) 目录号 : GC44867
SAICAR是嘌呤核苷酸从头合成途径中的一种中间代谢产物，SAICAR能够以同工酶选择性的方式激活丙酮酸激酶M2亚型（PKM2；EC50=0.3mM）。
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.
SAICAR是嘌呤核苷酸从头合成途径中的一种中间代谢产物，SAICAR能够以同工酶选择性的方式激活丙酮酸激酶M2亚型（PKM2；EC50=0.3mM）[1-2]。SAICAR的积累可诱导PKM2发生核定位，并通过PKM2磷酸化并激活Erk1/2信号，诱导的细胞增殖，包括癌细胞[3-4]。
在体外，SAICAR（0.5mM）处理HeLa细胞30分钟，可促进细胞中组蛋白H3的磷酸化，并促进c-Myc基因表达[5]。SAICAR（0–0.5mM）在处理培养与葡萄糖剥夺条件的HeLa、A549、U87和H1299细胞30分钟，SAICAR进癌细胞在葡萄糖受限条件下的存活，同时调节葡萄糖摄取和乳酸生成[6]。
在体内，SAICAR（100μM；100μL）局部注射处理db/db糖尿病小鼠创面，每日一次，连续7天。SAICAR显著增加创缘COL17表达和上皮细胞增殖标志物PCNA阳性细胞比例，促进创面再上皮化进程，加速创面闭合速度，并改善延迟愈合表型[7]。
| 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 | |
| 别名 | Succino-AICAR | ||
| 化学名 | 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 | ||
| 分子式 | C13H19N4O12P | 分子量 | 454.3 |
| 溶解度 | Slightly soluble in methanol | 储存条件 | 4°C, away from moisture and light |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet