SD-208

Catalog No.S7624 Batch:S762404

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Technical Data

Formula

C17H10ClFN6
Molecular Weight 352.75 CAS No. 627536-09-8
Solubility (25°C)* In vitro DMSO 17 mg/mL (48.19 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description SD-208 is a selective TGF-βRI (ALK5) inhibitor with IC50 of 48 nM, >100-fold selectivity over TGF-βRII.
Targets
TGF-βRI (ALK5) [1]
(Cell-free assay)
48 nM
In vitro SD-208 inhibits the cell growth and constitutive and TGF-beta-evoked migration and invasion, and enhances immunogenicity in murine SMA-560 and human LN-308 glioma cells. [1] SD-208 blocka TGF-beta-induced phosphorylation of the receptor-associated Smads, Smad2 and Smad3, and stimulates epithelial-to-mesenchymal transdifferentiation, migration, and invasiveness into Matrigel in vitro. [2] SD-208 also abolishes the promoting effect of TGF-β on neointimal smooth muscle-like cell (SMLC) proliferation and migration in vitro. [3]
In vivo SD-208 (1 mg/mL, p.o.) significantly prolongs the median survival of SMA-560 glioma-bearing mice. [1] In syngeneic 129S1 mice, SD-208 (60 mg/kg/d, p.o.) inhibits primary R3T tumor growth, and reduces the number and the size of lung metastases. [2] In the murine aortic allograft model, SD-208 effectively reduces the formation of intimal hyperplasia of transplant arteriosclerosis (TA). [3]

Protocol (from reference)

Kinase Assay:[1]
  • Kinase assay

    Various kinase activities are assayed by measuring the incorporation of radiolabeled ATP into a peptide or protein substrate. The reactions are performed in 96-well plates and included the relevant kinase, substrate, ATP, and appropriate cofactors. The reactions are incubated and then stopped by the addition of phosphoric acid. Substrate is captured onto a phosphocellulose filter, which is washed free of unreacted ATP. The counts incorporated are determined by counting on a microplate scintillation counter. The ability of SD-208 to inhibit the respective kinase is determined by comparing counts incorporated in the presence of compound with those incorporated in the absence of compound.
Cell Assay:[1]
  • Cell lines

    Murine SMA-560 and human LN-308 glioma cells

  • Concentrations

    1 μM

  • Incubation Time

    48 hours

  • Method

    Glioma cells are cultured in the absence or presence of SD-208 (1 μM) for 48 hours. The cells are pulsed for the last 24 hours with [methyl-3H]thymidine (0.5 μCi) and harvested, and incorporated radioactivity is determined in a liquid scintillation counter.
Animal Study:[1]
  • Animal Models

    VM/Dk mice bearing SMA-560 tumors

  • Dosages

    1 mg/mL

  • Administration

    p.o.

Selleck's SD-208 has been cited by 23 publications

Nudifloside, a Secoiridoid Glucoside Derived from Callicarpa nudiflora, Inhibits Endothelial-to-Mesenchymal Transition and Angiogenesis in Endothelial Cells by Suppressing Ezrin Phosphorylation [ J Cancer, 2024, 15(9):2448-2459] PubMed: 38577590
Protein phosphatase PPM1A inhibition attenuates osteoarthritis via regulating TGF-β/Smad2 signaling in chondrocytes [ JCI Insight, 2023, 8(3)e166688] PubMed: 36752205
MicroRNA Expression Patterns Reveal a Role of the TGF-β Family Signaling in AML Chemo-Resistance [ Cancers (Basel), 2023, 10.3390/cancers15205086] PubMed: 37894453
MicroRNA Expression Patterns Reveal a Role of the TGF-β Family Signaling in AML Chemo-Resistance [ Cancers (Basel), 2023, 15(20)5086] PubMed: 37894453
Exosome-Mediated Delivery of Transforming Growth Factor-β Receptor 1 Kinase Inhibitors and Toll-Like Receptor 7/8 Agonists for Combination Therapy of Tumors [ Acta Biomater, 2022, S1742-7061(22)00004-6] PubMed: 35007784
Induction of Pro-Fibrotic CLIC4 in Dermal Fibroblasts by TGF-β/Wnt3a Is Mediated by GLI2 Upregulation [ Cells, 2022, 11(3)530] PubMed: 35159339
Berberine Suppresses Lung Metastasis of Cancer via Inhibiting Endothelial Transforming Growth Factor Beta Receptor 1 [ Front Pharmacol, 2022, 13:917827] PubMed: 35784732
TGFβ signaling is required for sclerotome resegmentation during development of the spinal column in Gallus gallus [ Dev Biol, 2022, 488:120-130] PubMed: 35644252
Loss of Yap/taz in cardiac fibroblasts attenuates adverse remodeling and improves cardiac function [ Cardiovasc Res, 2021, cvab205] PubMed: 34132780
Co-inhibition of SMAD and MAPK signaling enhances 124I uptake in BRAF-mutant thyroid cancers [ Endocr Relat Cancer, 2021, 28(6):391-402] PubMed: 33890869

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.