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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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M304758-5mg | 5mg | In stock | $44.90 | |
M304758-25mg | 25mg | In stock | $147.90 | |
M304758-100mg | 100mg | In stock | $376.90 |
Nrf2 inhibitor; phenotypically lethal
Specifications & Purity | Moligand™, ≥99% |
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Biochemical and Physiological Mechanisms | Nrf2 inhibitor. Blocks Nrf2 downstream target gene expression. Enhances cytotoxic effects ofdoxorubicin orTaxol in non-small cell lung cancer (NSCLC). Demonstrates selectivity for NSCLC cells with KEAP1 mutations. |
Storage Temp | Store at 2-8°C |
Shipped In | Wet ice |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | Inhibitor of nuclear factor; erythroid 2 like 2 |
Product Description |
ML385 is a specific nuclear factor erythroid 2-related factor 2 (NRF2) inhibitor with an IC50 of 1.9 μM.
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Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
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Pubchem Sid | 488191809 |
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Pubchem Sid Url | https://pubchem.ncbi.nlm.nih.gov/substance/488191809 |
IUPAC Name | 2-(1,3-benzodioxol-5-yl)-N-[5-methyl-4-[1-(2-methylbenzoyl)-2,3-dihydroindol-5-yl]-1,3-thiazol-2-yl]acetamide |
INCHI | InChI=1S/C29H25N3O4S/c1-17-5-3-4-6-22(17)28(34)32-12-11-20-15-21(8-9-23(20)32)27-18(2)37-29(31-27)30-26(33)14-19-7-10-24-25(13-19)36-16-35-24/h3-10,13,15H,11-12,14,16H2,1-2H3,(H,30,31,33) |
InChi Key | LINHYWKZVCNAMQ-UHFFFAOYSA-N |
Canonical SMILES | CC1=CC=CC=C1C(=O)N2CCC3=C2C=CC(=C3)C4=C(SC(=N4)NC(=O)CC5=CC6=C(C=C5)OCO6)C |
Isomeric SMILES | CC1=CC=CC=C1C(=O)N2CCC3=C2C=CC(=C3)C4=C(SC(=N4)NC(=O)CC5=CC6=C(C=C5)OCO6)C |
PubChem CID | 1383822 |
Molecular Weight | 511.59 |
PubChem CID | 1383822 |
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CAS Registry No. | 846557-71-9 |
ChEMBL Ligand | CHEMBL1479098 |
PubChem SID | 488191809 |
Enter Lot Number to search for COA:
Find and download the COA for your product by matching the lot number on the packaging.
Lot Number | Certificate Type | Date | Item |
---|---|---|---|
H2429550 | Certificate of Analysis | Jul 25, 2024 | M304758 |
H2429547 | Certificate of Analysis | Jul 25, 2024 | M304758 |
H2429545 | Certificate of Analysis | Jul 25, 2024 | M304758 |
H2106164 | Certificate of Analysis | May 11, 2024 | M304758 |
E2421319 | Certificate of Analysis | May 08, 2024 | M304758 |
E2421318 | Certificate of Analysis | May 08, 2024 | M304758 |
K2302468 | Certificate of Analysis | Oct 20, 2023 | M304758 |
K2302436 | Certificate of Analysis | Oct 20, 2023 | M304758 |
K2302435 | Certificate of Analysis | Oct 20, 2023 | M304758 |
E23291205 | Certificate of Analysis | May 17, 2023 | M304758 |
E23291204 | Certificate of Analysis | May 17, 2023 | M304758 |
E23291197 | Certificate of Analysis | May 17, 2023 | M304758 |
E23291189 | Certificate of Analysis | May 17, 2023 | M304758 |
B2309557 | Certificate of Analysis | Nov 28, 2022 | M304758 |
B2309543 | Certificate of Analysis | Nov 28, 2022 | M304758 |
B2309540 | Certificate of Analysis | Nov 28, 2022 | M304758 |
B2309485 | Certificate of Analysis | Nov 28, 2022 | M304758 |
B2309481 | Certificate of Analysis | Nov 28, 2022 | M304758 |
H2205473 | Certificate of Analysis | Jun 15, 2022 | M304758 |
H2205474 | Certificate of Analysis | Jun 15, 2022 | M304758 |
H2205475 | Certificate of Analysis | Jun 15, 2022 | M304758 |
Solubility | Solvent:DMSO, Max Conc. mg/mL: 25.58, Max Conc. mM: 50 |
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RIDADR | NONHforallmodesoftransport |
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Starting at $51.90
1. Fan Wenbo, Zhou Jianwu. (2023) Icariside II Suppresses Ferroptosis to Protect Against MPP+-Induced Parkinson's Disease through Keap1/Nrf2/GPX4 Signaling. CHINESE JOURNAL OF PHYSIOLOGY, 66 (6): (437). [PMID:38149556] [10.4103/cjop.CJOP-D-23-00107] |
2. Bing-hao Lin, Run-xun Ma, Jing-tao Wu, Shi-qi Du, Yi-yun Lv, Hao-nan Yu, Wei Zhang, Shu-ming Mao, Guang-yao Liu, Yi-tian Bu, Zi-hao Chen, Chen Jin, Zong-yi Wu, Lei Yang. (2023) Cinnamaldehyde Alleviates Bone Loss by Targeting Oxidative Stress and Mitochondrial Damage via the Nrf2/HO-1 Pathway in BMSCs and Ovariectomized Mice. JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY, 71 (45): (17362–17378). [PMID:37917162] [10.1021/acs.jafc.3c03501] |
3. Yue Tang, Yueyue Kang, Xinru Zhang, Caiyi Cheng. (2023) Mesenchymal stem cell exosomes as nanotherapeutics for dry age-related macular degeneration. JOURNAL OF CONTROLLED RELEASE, 357 (356). [PMID:37028452] [10.1016/j.jconrel.2023.04.003] |
4. Hengju Ge, Jiaxin Li, Yang Xu, Jiahong Xie, Naymul Karim, Fujie Yan, Jianling Mo, Wei Chen. (2023) Ameliorative effect of Fructus Gardeniae against lipotoxicity associated hepatocytes injury through activating Nrf2 signaling pathway. Food Bioscience, 53 (102596). [PMID:] [10.1016/j.fbio.2023.102596] |
5. Yun Zhang, Maihuan Wang, Kebin Zhang, Junze Zhang, Xinpu Yuan, Guijun Zou, Zhen Cao, Chaojun Zhang. (2022) 6′-O-Galloylpaeoniflorin attenuates Helicobacter pylori-associated gastritis via modulating Nrf2 pathway. INTERNATIONAL IMMUNOPHARMACOLOGY, 111 (109122). [PMID:35964411] [10.1016/j.intimp.2022.109122] |
1. Singh A, Misra V, Thimmulappa RK, Lee H, Ames S, Hoque MO, Herman JG, Baylin SB, Sidransky D, Gabrielson E et al.. (2006) Dysfunctional KEAP1-NRF2 interaction in non-small-cell lung cancer.. PLoS Med, 3 (10): (e420). [PMID:17020408] [10.1021/op500134e] |
2. Ohta T, Iijima K, Miyamoto M, Nakahara I, Tanaka H, Ohtsuji M, Suzuki T, Kobayashi A, Yokota J, Sakiyama T et al.. (2008) Loss of Keap1 function activates Nrf2 and provides advantages for lung cancer cell growth.. Cancer Res, 68 (5): (1303-9). [PMID:18316592] [10.1021/op500134e] |
3. Shibata T, Kokubu A, Gotoh M, Ojima H, Ohta T, Yamamoto M, Hirohashi S. (2008) Genetic alteration of Keap1 confers constitutive Nrf2 activation and resistance to chemotherapy in gallbladder cancer.. Gastroenterology, 135 (4): (1358-1368, 1368.e1-4). [PMID:18692501] [10.1021/op500134e] |
4. Shibata T, Ohta T, Tong KI, Kokubu A, Odogawa R, Tsuta K, Asamura H, Yamamoto M, Hirohashi S. (2008) Cancer related mutations in NRF2 impair its recognition by Keap1-Cul3 E3 ligase and promote malignancy.. Proc Natl Acad Sci USA, 105 (36): (13568-73). [PMID:18757741] [10.1021/op500134e] |
5. Solis LM, Behrens C, Dong W, Suraokar M, Ozburn NC, Moran CA, Corvalan AH, Biswal S, Swisher SG, Bekele BN et al.. (2010) Nrf2 and Keap1 abnormalities in non-small cell lung carcinoma and association with clinicopathologic features.. Clin Cancer Res, 16 (14): (3743-53). [PMID:20534738] [10.1021/op500134e] |
6. Konstantinopoulos PA, Spentzos D, Fountzilas E, Francoeur N, Sanisetty S, Grammatikos AP, Hecht JL, Cannistra SA. (2011) Keap1 mutations and Nrf2 pathway activation in epithelial ovarian cancer.. Cancer Res, 71 (15): (5081-9). [PMID:21676886] [10.1021/op500134e] |
7. Tsvetkova E, Goss GD. (2012) Drug resistance and its significance for treatment decisions in non-small-cell lung cancer.. Curr Oncol, 19 (Suppl 1): (S45-51). [PMID:22787410] [10.1021/op500134e] |
8. Tian Y, Wu K, Liu Q, Han N, Zhang L, Chu Q, Chen Y. (2016) Modification of platinum sensitivity by KEAP1/NRF2 signals in non-small cell lung cancer.. J Hematol Oncol, 9 (1): (83). [PMID:27601007] [10.1021/op500134e] |
9. Singh A, Venkannagari S, Oh KH, Zhang YQ, Rohde JM, Liu L, Nimmagadda S, Sudini K, Brimacombe KR, Gajghate S et al.. (2016) Small Molecule Inhibitor of NRF2 Selectively Intervenes Therapeutic Resistance in KEAP1-Deficient NSCLC Tumors.. ACS Chem Biol, 11 (11): (3214-3225). [PMID:27552339] [10.1021/op500134e] |
10. Fan Wenbo, Zhou Jianwu. (2023) Icariside II Suppresses Ferroptosis to Protect Against MPP+-Induced Parkinson's Disease through Keap1/Nrf2/GPX4 Signaling. CHINESE JOURNAL OF PHYSIOLOGY, 66 (6): (437). [PMID:38149556] [10.4103/cjop.CJOP-D-23-00107] |
11. Bing-hao Lin, Run-xun Ma, Jing-tao Wu, Shi-qi Du, Yi-yun Lv, Hao-nan Yu, Wei Zhang, Shu-ming Mao, Guang-yao Liu, Yi-tian Bu, Zi-hao Chen, Chen Jin, Zong-yi Wu, Lei Yang. (2023) Cinnamaldehyde Alleviates Bone Loss by Targeting Oxidative Stress and Mitochondrial Damage via the Nrf2/HO-1 Pathway in BMSCs and Ovariectomized Mice. JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY, 71 (45): (17362–17378). [PMID:37917162] [10.1021/acs.jafc.3c03501] |
12. Yue Tang, Yueyue Kang, Xinru Zhang, Caiyi Cheng. (2023) Mesenchymal stem cell exosomes as nanotherapeutics for dry age-related macular degeneration. JOURNAL OF CONTROLLED RELEASE, 357 (356). [PMID:37028452] [10.1016/j.jconrel.2023.04.003] |
13. Hengju Ge, Jiaxin Li, Yang Xu, Jiahong Xie, Naymul Karim, Fujie Yan, Jianling Mo, Wei Chen. (2023) Ameliorative effect of Fructus Gardeniae against lipotoxicity associated hepatocytes injury through activating Nrf2 signaling pathway. Food Bioscience, 53 (102596). [PMID:] [10.1016/j.fbio.2023.102596] |
14. Yun Zhang, Maihuan Wang, Kebin Zhang, Junze Zhang, Xinpu Yuan, Guijun Zou, Zhen Cao, Chaojun Zhang. (2022) 6′-O-Galloylpaeoniflorin attenuates Helicobacter pylori-associated gastritis via modulating Nrf2 pathway. INTERNATIONAL IMMUNOPHARMACOLOGY, 111 (109122). [PMID:35964411] [10.1016/j.intimp.2022.109122] |