| Size | Price | Stock | Qty |
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| 1mg |
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| 50mg | |||
| Other Sizes |
| Targets |
SD-1029 targets Janus kinase 2 (JAK2) and the signal transducer and activator of transcription 3 (STAT3). It is a JAK2-selective inhibitor that exhibits much less effect on the cellular phosphorylation levels of Jak1 and Src and shows no significant inhibition towards a panel of 49 other protein kinases in cell-free kinase assays. SD-1029 inhibits the phosphorylation of JAK2, which in turn inhibits the activation of STAT3. It also inhibits the nuclear translocation of STAT3, disrupting the JAK-STAT signaling pathway.
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| ln Vitro |
SD-1029 (10 μM) reduces EGFP-Stat3 nuclear translocation in BHK-21 and U-2OS cells [1]. SD-1029 (5 and 10 μM; 24 hours) inhibits cell growth and induces apoptosis in OVCAR8TR ovarian cancer cells [1]. SD-1029 (10 μM; 24 hours) inhibits p-Stat3 levels in human breast and ovarian cancer cell lines [1]. SD-1029 not only inhibits JAK2 phosphorylation, but also inhibits STAT1 and STAT3 phosphorylation. SD-1029 strongly inhibits Tyk2 phosphorylation, indicating that both JAK2 and Tyk2 are upstream requirements for IL-23-induced IL-23R expression [2].
In vitro, SD-1029 is a JAK2-selective inhibitor that effectively inhibits cell proliferation in JAK-activated BA/F3 cell lines. It inhibits the phosphorylation and nuclear translocation of cellular Stat3. SD-1029 inhibits EGFP-Stat3 nuclear translocation in BHK-21 and U-2OS cells. It suppresses p-Stat3 levels in human breast and ovarian cancer cell lines, inhibits cell growth, and induces apoptosis in OVCAR8TR ovarian cancer cells. These in vitro studies confirm SD-1029's activity as a JAK2/STAT3 inhibitor. |
| ln Vivo |
In vivo activity data for SD-1029 is limited, as the compound is primarily used as a research tool in in vitro studies. However, its mechanism of action—inhibiting JAK2 and STAT3 signaling—suggests potential in vivo applications in cancer research. The compound could be used in animal models of cancer to study the effects of JAK-STAT inhibition on tumor growth. However, specific in vivo protocols and results are not detailed in standard product descriptions.
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| Enzyme Assay |
In vitro enzyme assays for SD-1029 measure its inhibition of JAK2 kinase activity. JAK2 enzyme is incubated with a peptide substrate and ATP in the presence of varying concentrations of SD-1029. The incorporation of phosphate into the substrate is measured, and the IC50 is determined from the dose-response curve. Selectivity is assessed by testing the compound against a panel of other kinases, including Jak1 and Src. These assays confirm SD-1029's potency and selectivity as a JAK2 inhibitor.
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| Cell Assay |
Cell proliferation assay [1]
Cell Types: OVCAR8TR ovarian cancer cells Tested Concentrations: 5 and 10 μM Incubation Duration: 24 hrs (hours) Experimental Results: Down-regulate cell proliferation and induce apoptosis. Treatment resulted in a significant 20-fold induction of apoptosis in OVCAR8TR cells expressing constitutively activated Stat3. Western Blot Analysis[1] Cell Types: MDA-MB-468 and MDA435 (breast cancer), OV1063 (ovarian cancer), and paclitaxel-resistant ovarian cancer sublines SKOV-3TR and OVCAR8TR. Tested Concentrations: 10 μM Incubation Duration: 24 hrs (hours) Experimental Results: Result in diminished pStat3 levels. In vitro cell-based assays for SD-1029 are used to study its effects on JAK-STAT signaling and cancer cell biology. Cancer cell lines (e.g., breast, ovarian) are treated with SD-1029 at various concentrations. The phosphorylation of STAT3 is measured by Western blotting using phospho-specific antibodies. The nuclear translocation of STAT3 is assessed by immunofluorescence. Cell proliferation is measured using assays such as MTT or CellTiter-Glo. Apoptosis is measured using Annexin V staining or caspase-3/7 activation assays. These assays confirm the compound's activity as a JAK2/STAT3 inhibitor. |
| Animal Protocol |
In vivo animal experiments for SD-1029 are not extensively described in the available literature. As a research compound, its use in vivo would be determined by the specific research question being addressed. A typical protocol for studying a JAK2 inhibitor would involve its administration to animal models of cancer or inflammatory diseases. The compound would be formulated for injection, and endpoints such as tumor growth or inflammatory markers would be assessed. However, specific protocols for SD-1029 are not detailed.
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| ADME/Pharmacokinetics |
SD-1029 has a molecular weight of 639.25 g/mol. It is a solid compound with a purity of >80% by HPLC (sum of isomers). It is soluble in DMSO and other organic solvents. For storage, it is recommended to keep the powder at -20°C. Detailed pharmacokinetic properties such as absorption, distribution, metabolism, and excretion (ADME) have not been extensively characterized. As a research compound, its stability is maintained by proper storage as a dry powder.
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| Toxicity/Toxicokinetics |
Detailed toxicity data for SD-1029 is not provided in standard product descriptions. As a research compound, its toxicity profile has not been extensively characterized. SD-1029 is a JAK2 inhibitor, and its toxicity would be related to its effects on JAK-STAT signaling in normal tissues. However, comprehensive toxicological studies have not been reported. As with all research chemicals, standard laboratory safety precautions should be followed when handling SD-1029. Its use is limited to research applications.
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| References |
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| Additional Infomation |
SD-1029 is a research compound and is not approved for any clinical or therapeutic use. It is a cell-permeable xanthenedione compound that acts as a JAK2-selective inhibitor. SD-1029 inhibits the phosphorylation of JAK2, thereby inhibiting the activation of STAT3. It has been shown to inhibit the nuclear translocation of STAT3. SD-1029 effectively inhibits cell proliferation in JAK-activated cell lines and induces apoptosis in ovarian cancer cells. It is a valuable research tool for studying JAK-STAT signaling in cancer and other diseases.
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| Molecular Formula |
C25H32BR2CL2N2O3
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| Molecular Weight |
639.25
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| Exact Mass |
636.015
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| CAS # |
118372-34-2
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| PubChem CID |
44543754
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| Appearance |
Typically exists as solid at room temperature
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
34
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| Complexity |
781
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1(C2=CC=C(Cl)C(Cl)=C2)C2=C(CCC(CN(C)C)C2=O)OC2=C1C(=O)C(CN(C)C)CC2.[H]Br.[H]Br
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| InChi Key |
INKLAKXQHDQKKZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H30Cl2N2O3.2BrH/c1-28(2)12-15-6-9-19-22(24(15)30)21(14-5-8-17(26)18(27)11-14)23-20(32-19)10-7-16(25(23)31)13-29(3)4;;/h5,8,11,15-16,21H,6-7,9-10,12-13H2,1-4H3;2*1H
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| Chemical Name |
9-(3,4-dichlorophenyl)-2,7-bis[(dimethylamino)methyl]-3,4,5,6,7,9-hexahydro-2H-xanthene-1,8-dione;dihydrobromide
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| Synonyms |
SD-1029 SD1029 SD 1029
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.5643 mL | 7.8217 mL | 15.6433 mL | |
| 5 mM | 0.3129 mL | 1.5643 mL | 3.1287 mL | |
| 10 mM | 0.1564 mL | 0.7822 mL | 1.5643 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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