research use only
Cat.No.S1569
| Related Targets | Dehydrogenase HSP Transferase P450 (e.g. CYP17) PDE phosphatase PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism |
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| Other Retinoid Receptor Inhibitors | TTNPB AM580 Tamibarotene UVI 3003 Fenretinide SR 11237 BMS493 Palovarotene CD1530 AR7 |
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In vitro |
DMSO
: 10 mg/mL
(28.45 mM)
Ethanol : 10 mg/mL Water : Insoluble |
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In vivo |
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| Molecular Weight | 351.46 | Formula | C21H21NO2S |
Storage (From the date of receipt) | |
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| CAS No. | 118292-40-3 | Download SDF | Storage of Stock Solutions |
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| Synonyms | AGN190168 | Smiles | CCOC(=O)C1=CN=C(C=C1)C#CC2=CC3=C(C=C2)SCCC3(C)C | ||
| Targets/IC50/Ki |
RAR
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|---|---|
| In vitro |
Tazarotene causes ERK activation, RB tumor suppressor protein hypophosphorylation, G0 arrest, and myeloid differentiation in HL-60 human myeloblastic leukemia cells. This compound could propel either early or late portions of the period leading to differentiation and G0 arrest and is interchangeable with an RARalpha-selective ligand. It regulates gene transcription via interaction with specific nuclear retinoic acid receptors (RARs), thereby modulating the three key pathogenic factors in psoriasis. This chemical inhibits the proliferation of fibroblasts and synthesis of DNA and collagen. It down-regulates markers of keratinocyte differentiation, keratinocyte proliferation, and inflammation. This agent also up-regulates three novel genes TIG-1 (tazarotene-induced gene-1), TIG-2, and TIG-3, which may mediate an antiproliferative effect. It causes growth suppression in retinoid-responsive breast cancer cell lines by up-regulating TIG3.
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| In vivo |
Tazarotene treatment reduces the number and size of microscopic basal cell carcinomas (BCCs) in UV-treated Ptch1+/− mice. This compound also reduces the number and size of microscopic basal cell carcinomas (BCCs) in ionizing radiation-treated Ptch1+/− mice.
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References |
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(data from https://clinicaltrials.gov, updated on 2024-05-22)
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT06015152 | Completed | Scalp Psoriasis |
Jinnah Postgraduate Medical Centre |
August 1 2022 | Not Applicable |
| NCT03988439 | Recruiting | Psoriasis |
Bausch Health Americas Inc. |
March 24 2021 | Phase 4 |
| NCT02620813 | Completed | Acne Vulgaris |
University of California Davis |
October 2015 | Early Phase 1 |
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