ACT001 | CAS#1403357-81-2

MedKoo Cat#: 471148 | Name: ACT001

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

ACT001 is orally active PAI-1 inhibitor by inhibiting the phosphorylation of PI3K and AKT. ACT001 inhibits PD-L1 transcription and modulates anti-tumor immune response in glioma bearing mice, and played a critical role in microglia-mediated neuroinflammatory response and might be a novel potential chemotherapeutic drug for TBI. Additionally, ACT001 suppressed cell proliferation and induced cell death of pituitary tumor cells in vitro and in vivo, and was also effective in suppressing the growth of different subtypes of human pituitary adenomas.

Chemical Structure

ACT001

CAS#1403357-81-2 (free base)

Theoretical Analysis

MedKoo Cat#: 471148

Name: ACT001

CAS#: 1403357-81-2 (free base)

Chemical Formula: C16H25NO3

Exact Mass: 279.1830

Molecular Weight: 279.38

Elemental Analysis: C, 68.79; H, 9.02; N, 5.01; O, 17.18

Price and Availability

Size	Price	Availability	Quantity
5mg	USD 550.00	2 Weeks
25mg	USD 1,650.00	2 Weeks

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Related CAS #

1403357-81-2 (free base) 1582289-91-5 (fumarate)

Synonym

ACT001; ACT 001; ACT-001; DMAMCL; Dimethylaminomicheliolide

IUPAC/Chemical Name

(3R,3aS,9R,9aS,9bS)-3-((dimethylamino)methyl)-9-hydroxy-9-methyl-3a,4,5,7,8,9,9a,9b-octahydroazuleno[4,5-b]furan-2(3H)-one

InChi Key

GIVYVHVOKXPXEC-SMSYFYOWSA-N

InChi Code

InChI=1S/C16H25NO3/c1-16(19)8-7-10-5-4-6-11-12(9-17(2)3)15(18)20-14(11)13(10)16/h5,11-14,19H,4,6-9H2,1-3H3/t11-,12-,13-,14-,16+/m0/s1

SMILES Code

O=C1[C@@H](CN(C)C)[C@@]2([H])[C@]([C@@]3([H])[C@](C)(O)CCC3=CCC2)([H])O1

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

To be determined

Shelf Life

>2 years if stored properly

Drug Formulation

To be determined

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 279.38 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

1: Cai L, Gong Q, Qi L, Xu T, Suo Q, Li X, Wang W, Jing Y, Yang D, Xu Z, Yuan F, Tang Y, Yang G, Ding J, Chen H, Tian H. ACT001 attenuates microglia-mediated neuroinflammation after traumatic brain injury via inhibiting AKT/NFκB/NLRP3 pathway. Cell Commun Signal. 2022 Apr 23;20(1):56. doi: 10.1186/s12964-022-00862-y. PMID: 35461293; PMCID: PMC9035258. 2: Tong L, Li J, Li Q, Wang X, Medikonda R, Zhao T, Li T, Ma H, Yi L, Liu P, Xie Y, Choi J, Yu S, Lin Y, Dong J, Huang Q, Jin X, Lim M, Yang X. ACT001 reduces the expression of PD-L1 by inhibiting the phosphorylation of STAT3 in glioblastoma. Theranostics. 2020 May 1;10(13):5943-5956. doi: 10.7150/thno.41498. PMID: 32483429; PMCID: PMC7254983. 3: Guo H, Song Y, Li F, Fan Y, Li Y, Zhang C, Hou H, Shi M, Zhao Z, Chen Z. ACT001 suppressing M1 polarization against inflammation via NF-κB and STAT1 signaling pathways alleviates acute lung injury in mice. Int Immunopharmacol. 2022 Sep;110:108944. doi: 10.1016/j.intimp.2022.108944. Epub 2022 Jun 18. PMID: 35728304. 4: Hou Y, Sun B, Liu W, Yu B, Shi Q, Luo F, Bai Y, Feng H. Targeting of glioma stem-like cells with a parthenolide derivative ACT001 through inhibition of AEBP1/PI3K/AKT signaling. Theranostics. 2021 Jan 1;11(2):555-566. doi: 10.7150/thno.49250. PMID: 33391492; PMCID: PMC7738851. 5: Cai L, Wu ZR, Cao L, Xu JD, Lu JL, Wang CD, Jin JH, Wu ZB, Su ZP. ACT001 inhibits pituitary tumor growth by inducing autophagic cell death via MEK4/MAPK pathway. Acta Pharmacol Sin. 2022 Sep;43(9):2386-2396. doi: 10.1038/s41401-021-00856-5. Epub 2022 Jan 26. PMID: 35082393; PMCID: PMC9433416. 6: Zhang T, Lin C, Wu S, Jin S, Li X, Peng Y, Wang X. ACT001 Inhibits TLR4 Signaling by Targeting Co-Receptor MD2 and Attenuates Neuropathic Pain. Front Immunol. 2022 Jun 9;13:873054. doi: 10.3389/fimmu.2022.873054. PMID: 35757727; PMCID: PMC9218074. 7: Zhao M, Qin T, Huang D. ACT001 inhibits the proliferation of non-small cell lung cancer cells by upregulating NKTR expression. Thorac Cancer. 2022 Jun;13(12):1772-1782. doi: 10.1111/1759-7714.14453. Epub 2022 May 10. PMID: 35537816; PMCID: PMC9200889. 8: Li Q, Sun Y, Liu B, Li J, Hao X, Ge W, Zhang X, Bao S, Gong J, Jiang Z, Qiu C, Zhao L, Zhao Y, Chen Y, Yang X, Ding Y, Wu Z. ACT001 modulates the NF- κB/MnSOD/ROS axis by targeting IKKβ to inhibit glioblastoma cell growth. J Mol Med (Berl). 2020 Feb;98(2):263-277. doi: 10.1007/s00109-019-01839-0. Epub 2020 Jan 4. PMID: 31901951. 9: Zhu J, Tang C, Cong Z, Yuan F, Cai X, Yang J, Ma C. ACT001 reverses resistance of prolactinomas via AMPK-mediated EGR1 and mTOR pathways. Endocr Relat Cancer. 2021 Dec 13;29(2):33-46. doi: 10.1530/ERC-21-0215. PMID: 34821219. 10: Li H, Yang M, Song H, Sun M, Zhou H, Fu J, Zhou D, Bai W, Chen B, Lai M, Kang H, Wei S. ACT001 Relieves NMOSD Symptoms by Reducing Astrocyte Damage with an Autoimmune Antibody. Molecules. 2023 Feb 2;28(3):1412. doi: 10.3390/molecules28031412. PMID: 36771078; PMCID: PMC9918908. 11: Xi X, Liu N, Wang Q, Chu Y, Yin Z, Ding Y, Lu Y. ACT001, a novel PAI-1 inhibitor, exerts synergistic effects in combination with cisplatin by inhibiting PI3K/AKT pathway in glioma. Cell Death Dis. 2019 Oct 7;10(10):757. doi: 10.1038/s41419-019-1986-2. PMID: 31591377; PMCID: PMC6779874. 12: Yang J, Li Y, Han X, Pei X, Lin Z, Li C. The antitumor effect of the novel agent MCL/ACT001 in pancreatic ductal adenocarcinoma. J Cancer Res Clin Oncol. 2022 Dec 22. doi: 10.1007/s00432-022-04542-9. Epub ahead of print. PMID: 36547690. 13: Liu Y, Wang L, Liu J, Xie X, Hu H, Luo F. Anticancer Effects of ACT001 via NF-κB Suppression in Murine Triple-Negative Breast Cancer Cell Line 4T1. Cancer Manag Res. 2020 Jun 26;12:5131-5139. doi: 10.2147/CMAR.S244748. PMID: 32617021; PMCID: PMC7326172. 14: Liu Q, Zhang S, Zhu D, Tang X, Che Y, Feng X. The parthenolide derivative ACT001 synergizes with low doses of L-DOPA to improve MPTP-induced Parkinson's disease in mice. Behav Brain Res. 2020 Feb 3;379:112337. doi: 10.1016/j.bbr.2019.112337. Epub 2019 Nov 4. PMID: 31697983. 15: Luo H, Liu X, Liu H, Wang Y, Xu K, Li J, Liu M, Guo J, Qin X. ACT001 Ameliorates ionizing radiation-induced lung injury by inhibiting NLRP3 inflammasome pathway. Biomed Pharmacother. 2023 Jul;163:114808. doi: 10.1016/j.biopha.2023.114808. Epub 2023 May 3. PMID: 37146417. 16: Jin XH, Jia YS, Shi YH, Li QY, Bao SQ, Lu WP, Tong ZS. ACT001 can prevent and reverse tamoxifen resistance in human breast cancer cell lines by inhibiting NF-κB activation. J Cell Biochem. 2019 Feb;120(2):1386-1397. doi: 10.1002/jcb.27146. Epub 2018 Nov 18. PMID: 30450651. 17: Deng H, Liu H, Yang G, Wang D, Luo Y, Li C, Qi Z, Liu Z, Wang P, Jia Y, Gao Y, Ding Y. ACT001 inhibited CD133 transcription by targeting and inducing Olig2 ubiquitination degradation. Oncogenesis. 2023 Mar 30;12(1):19. doi: 10.1038/s41389-023-00462-6. PMID: 36990974; PMCID: PMC10060425. 18: Jaffar J, Glaspole I, Symons K, Westall G. Inhibition of NF-κB by ACT001 reduces fibroblast activity in idiopathic pulmonary fibrosis. Biomed Pharmacother. 2021 Jun;138:111471. doi: 10.1016/j.biopha.2021.111471. Epub 2021 Mar 15. PMID: 33730605. 19: Xi XN, Liu N, Wang QQ, Wu HT, He HB, Wang LL, Zhang TJ, Sun L, Yin Z, Chen Y, Lu YX. Pharmacokinetics, tissue distribution and excretion of ACT001 in Sprague-Dawley rats and metabolism of ACT001. J Chromatogr B Analyt Technol Biomed Life Sci. 2019 Jan 1;1104:29-39. doi: 10.1016/j.jchromb.2018.11.004. Epub 2018 Nov 6. PMID: 30423524. 20: Liu Q, Guo X, Huang Z, He Q, Zhu D, Zhang S, Peng Z, Che Y, Feng X. Anti- neuroinflammatory effects of dimethylaminomylide (DMAMCL, i.e., ACT001) are associated with attenuating the NLRP3 inﬂammasome in MPTP-induced Parkinson disease in mice. Behav Brain Res. 2020 Apr 6;383:112539. doi: 10.1016/j.bbr.2020.112539. Epub 2020 Feb 4. PMID: 32032741.

View History

ACT-660602