T-5224

SKU: orb1301807

Description

T-5224 is a selective small-molecule inhibitor that blocks the DNA-binding activity of the AP-1 transcription factor complex (c-Fos/c-Jun). It is utilized in both in vitro and in vivo research to investigate AP-1-mediated processes in inflammation, oncology, and cellular proliferation.

Research Area

Cell Biology, Molecular Biology, Protein Biochemistry

Images & Validation

−

Key Properties

−

CAS Number	530141-72-1
MW	517.53
Purity	99.29% (May vary between batches)
Formula	C₂₉H₂₇NO₈
SMILES	OC(=O)CCc1cc(ccc1OCc1ccc2c(c1)o[nH]c2=O)C(=O)c1ccc(OC2CCCC2)cc1O
Target	MMP,DNA/RNA Synthesis
Solubility	DMSO:240 mg/mL (463.74 mM);H2O:Insoluble;10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (9.66 mM)

Bioactivity

−

Target IC50	MMP1 (SW982 cells):10 μM\|β-hexosaminidase (RBL-2H3 cells):18.30 ± 1.48 µM\|AP-1 (NIH3T3 cells):10 μM
In Vivo	T-5224 efficiently inhibited the development of collagen-induced arthritis (CIA) when administered once daily from day 21, before the onset of arthritis. Arthritis on day 50 was inhibited by 64% and 91%, by 3 and 30 mg/kg of T-5224, respectively. The body weight of mice treated with T-5224 steadily recovered. X-ray studies showed that joint destruction was inhibited in treated but not in untreated arthritis controls, and notably, the joint was totally protected from destruction by 30 mg/kg of T-5224 . Administration of T-5224 (300 mg/kg, p.o.) after intraperitoneal injection of LPS imparted appreciable protection against acute elevations in serum levels of TNFα, HMGB1, ALT/AST as well as in liver tissue levels of MIP-1α and MCP-1, and reduced the lethality (27 %) . T-5224 (150 mg/kg) or vehicle was given orally every day for 4 weeks. The rate of cervical lymph node metastasis in the model was 40.0% in the T-5224-treated group versus 74.1% in the vehicle-treated group . Read more...
In Vitro	In vitro production of the synovial cell mediators MMP-1, MMP-3, IL-6 and TNFα by IL-1b–stimulated human synovial SW982 cells was inhibited by T-5224. This was also the case for the chondrocyte inflammatory mediators MMP-3 and MMP-13 in IL-1b–stimulated human chondrocyte SW1353 cells. The IC50 values were ~10 μM for most of the cellular assays . Vasopressin selectively stimulates an increase CDS1 mRNA that is dependent on protein kinase C and can be inhibited by the AP-1 inhibitor, T-5224 . T-5224 significantly inhibited the invasion, migration, and MMP activity of HNSCC cells in a dose-dependent manner; there was no significant influence on cell proliferation . Read more...
Cell Research	NIH/3T3 cells were transiently transfected with the luciferase reporter plasmids pAP-1-Luc (× 7 TGACTAA), pNF-kB-Luc (× 5 TGGGGACTTTCCGC) or control phRL-TK, and cultured overnight. Cells were incubated in 0.5% FBS/DMEM containing T-5224 for 1 h, and then stimulated with PMA (10 ng/ml) or TNFa (10 ng/ml), and then cultured for 3 h, followed by measurement of lysate by using dual-luciferase reporter assay system . Read more...
Animal Research	Mice were housed in an SPF (specific pathogen-free) grade environment and provided food and water ad libitum with a 12 h:12 h light/dark cycle. Male 8-week-old DBA/1J mice were immunized with bovine type II collagen emulsified in Freund's complete adjuvant on days 0 and 21. T-5224, MTX and LEF were orally administered once per day. Arthritis was assessed in a blind fashion for four paws per mouse using the following score: 0, uninvolved; 1, swelling of ≤2 toes or slight swelling in ankles and wrists; 2, swelling of ≥3 toes or moderate swelling in ankles and wrists; 3, extensive swelling of total paw. X-ray films of four paws taken using Softex were assessed for joint destruction in 2nd to 5th proximal interphalangeal joints and five metatarsophalangeal joints of four paws, the carpal joints of the forepaws, and the tarsal and calcaneal joints of the hind paws. Score was: 0, no change; 1, partial erosion; 2, complete erosion for joints; and 0, negative; 0.5, positive for osteoporosis. IL-1β (500 ng per unilateral hind paw) was administered into the footpads. The mice with ≥1 arthritis score were treated with either anti-TNFα antibody at 50 or 250 μg/mouse, intraperitoneally (i.p.) twice a week and/or with 3 mg/kg T-5224, orally once daily . Read more...

Storage & Handling

−

Storage	store at low temperature \| Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

−

inhibit, Inhibitor, MMP, Matrix metalloproteinases, c-Fos/AP-1, AP-1, Activator Protein 1, T 5224, T5224, T-5224

Quality Guarantee

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our Terms & Conditions and Buying Guide. Contact us at support@biorbyt.com.

Compound Identifiers

PubChem CID

23626877 ↗

Key Properties

−

No computed properties available.

Documents Download

Datasheet

Product Information

Download

Request a Document

Protocol Information

Find More Protocols

T-5224 (orb1301807)

Based on 0 reviews

Participating in our Biorbyt product reviews program enables you to support fellow scientists by sharing your firsthand experience with our products.

No reviews yet

Purity:	>98% (HPLC)
CAS Number:	530141-72-1
MW:	517.5266
Formula:	C₂₉H₂₇NO₈

T-5224

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

Similar Products

FOSL1 degrader 1 [orb2663915]

T-5224 [orb1224787]

Quality Guarantee

Compound Identifiers

Key Properties

Documents Download

Request a Document

Protocol Information

T-5224 (orb1301807)

Step 1: Enter information below

Step 2: Enter the in vivo formulation

Available Sizes

Email

UK Office

US Office

CN Office

Distributors