| Size | Price | Stock | Qty |
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| Targets |
SUMO1[1]
SUMO1 (Small Ubiquitin-related Modifier 1). HB007 is a SUMO1 degrader. It does not directly inhibit an enzyme but rather promotes the ubiquitination and proteasomal degradation of the SUMO1 protein itself, leading to a reduction in global SUMOylation levels. |
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| ln Vitro |
HB007 (compound 24) (0.1-100 μM) - inhibits the growth of LN229 cells in a concentration-dependent manner [1]. HB007 (10-25 μM) decreases SUM01 conjugation and total SUM01 protein levels in LN229 cells, but not SUM02/3 or UB[1].
In vitro, HB007 (compound 24) inhibits the proliferation of LN229 glioblastoma cells in a concentration-dependent manner (0.1-100 uM). HB007 (10-25 uM) decreases SUMO1 conjugation and total SUMO1 protein levels in LN229 cells, but it has no significant effect on SUMO2/3 or ubiquitin (UB) expression. By degrading SUMO1, it increases ER stress and ROS production, leading to reduced cell viability. |
| ln Vivo |
Although it had no effect on the body weights of the mice, HB007 (compound 24) (25–50 mg/kg; ip for 15 d) significantly reduces the growth of tumors in lung and colon cancer[1].
In vivo, HB007 (25-50 mg/kg, administered intraperitoneally for 15 days) significantly suppresses the growth of colon and lung cancer in mouse xenograft models. Importantly, it has no effect on the body weights of the mice, suggesting a favorable safety profile. The tumor growth inhibition is mediated by SUMO1 degradation, which leads to ER stress and ROS-mediated cell death. |
| Enzyme Assay |
For non-cellular assays, the binding interaction of HB007 with SUMO1 could be assessed by surface plasmon resonance (SPR). The purified SUMO1 protein is immobilized on a sensor chip, and HB007 is flowed over at increasing concentrations (0.1-100 uM) to determine the binding affinity. For functional assays, a cell-free ubiquitination system with purified components (E1, E2, E3, ubiquitin, and SUMO1) can be used to test if HB007 directly promotes SUMO1 ubiquitination.
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| Cell Assay |
LN229 cells are treated with HB007 (0.1-100 uM) for 24-48 hours. Cell proliferation is measured by MTT assay. SUMO1, SUMO2/3, and ubiquitin levels are assessed by Western blot. The levels of ER stress markers (e.g., GRP78, CHOP) and ROS production (by DCFH-DA staining) are measured. Cellular SUMOylation levels can be assessed using an antibody specific for SUMO2/3-ylated proteins or by detecting higher molecular weight smears of target proteins.
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| Animal Protocol |
In vivo studies are conducted in mouse xenograft models of colon and lung cancer. HB007 is formulated in a suitable vehicle (e.g., DMSO/PEG300/Tween-80/saline) and administered intraperitoneally at 25-50 mg/kg daily for 15 days. Tumor volume is measured with calipers. At the end of the study, tumors are harvested for Western blot analysis of SUMO1 levels and markers of ER stress and apoptosis. Tissue sections are stained for Ki-67 to assess proliferation. Body weight is monitored to assess tolerability.
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| ADME/Pharmacokinetics |
HB007 has a molecular weight of 328.78 g/mol and a molecular formula of C15H9ClN4OS. It is soluble in DMSO (24 mg/mL, 73 mM). For in vivo administration, it is typically formulated for intraperitoneal injection. Detailed pharmacokinetic parameters (half-life, Cmax, AUC) are not reported in the supplier literature. It is stored as a solid at -20degC. The powder is stable for up to three years under these conditions.
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| Toxicity/Toxicokinetics |
No detailed toxicological data are reported in the supplier literature. In animal studies, HB007 at doses of 25-50 mg/kg (i.p., daily for 15 days) had no effect on mouse body weight, indicating a favorable safety margin. As a research compound, it is not for human use. Standard safety precautions for handling chemicals should be followed, including the use of gloves and eye protection.
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| References | |
| Additional Infomation |
HB007 is also known as compound 24. It is a first-in-class SUMO1 degrader and a research-grade chemical only. It is not an FDA-approved drug. The mechanism of action involves inducing the ubiquitination and proteasomal degradation of SUMO1, which may be mediated by activating specific E3 ligases or disrupting SUMO1's interaction with deubiquitinating enzymes. It is a tool for studying the role of SUMOylation in cancer.
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| Molecular Formula |
C15H9CLN4OS
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|---|---|
| Molecular Weight |
328.776160001755
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| Exact Mass |
328.018
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| CAS # |
2387821-46-5
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| PubChem CID |
146255136
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
3.6
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
22
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| Complexity |
468
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC1=CC=CC(=C1)NC(NC1=NC2C=CC(C#N)=CC=2S1)=O
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| InChi Key |
URCZUKFRZQNQSQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H9ClN4OS/c16-10-2-1-3-11(7-10)18-14(21)20-15-19-12-5-4-9(8-17)6-13(12)22-15/h1-7H,(H2,18,19,20,21)
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| Chemical Name |
1-(3-chlorophenyl)-3-(6-cyano-1,3-benzothiazol-2-yl)urea
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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) |
DMSO: 31.25 mg/mL (95.05 mM)
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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 | 3.0415 mL | 15.2077 mL | 30.4155 mL | |
| 5 mM | 0.6083 mL | 3.0415 mL | 6.0831 mL | |
| 10 mM | 0.3042 mL | 1.5208 mL | 3.0415 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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