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| Targets |
CR-1-30-B is an inactive enantiomer and does not target eIF4A. The active enantiomer, CR-1-31-B, potently inhibits eIF4A by clamping it onto mRNA, a process requiring specific pi-pi stacking interactions with both the protein and the RNA substrate. The three-dimensional configuration of rocaglates is critical for their biological activity, and CR-1-30-B has the opposite stereochemistry, making it unable to engage with eIF4A in the same manner. As a result, CR-1-30-B has no effect on cap-dependent translation, MUC1-C translation, or other eIF4A-dependent processes, making it an ideal negative control for establishing target specificity.
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| ln Vitro |
CR-1-30-B is inactive in vitro and has no effect on eIF4A or translation. In contrast, the active enantiomer CR-1-31-B (50 nM) induces apoptosis in multiple cancer cell lines by inhibiting eIF4A-dependent translation, leading to the downregulation of short-lived oncoproteins (e.g., MCL-1, BCL-2, c-MYC). CR-1-30-B serves as a crucial negative control to demonstrate that the biological effects observed with CR-1-31-B are specifically due to eIF4A inhibition and not non-specific effects. The compound has no effect on the induction of MUC1-C translation, and its activity is limited to serving as an analytical reference.
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| ln Vivo |
CR-1-30-B is an inactive enantiomer and is not intended for in vivo studies as a therapeutic agent. It is used exclusively as a negative control in animal studies investigating the activity of the active enantiomer CR-1-31-B. For example, in xenograft models of multiple myeloma or lung cancer, treatment with the active enantiomer reduces tumor growth and induces apoptosis, while treatment with CR-1-30-B has no effect on tumor growth or survival compared to vehicle controls. The inactive compound helps confirm that the observed antitumor effects are specifically due to eIF4A inhibition and not non-specific off-target effects.
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| Enzyme Assay |
A typical non-cellular (cell-free) protocol for evaluating the activity of CR-1-30-B as a negative control involves an eIF4A ATPase or helicase assay. Recombinant eIF4A protein is expressed and purified. In a 96-well plate, eIF4A (50 nM) is incubated with increasing concentrations of CR-1-31-B (active) or CR-1-30-B (inactive) (0.1-1000 nM) in assay buffer containing 20 mM Tris-HCl (pH 7.5), 50 mM KCl, 2 mM MgCl2, 1 mM DTT, and 1 microM RNA substrate. The ATPase reaction is initiated by adding 0.5 mM ATP. After 30 minutes at 37degC, the amount of inorganic phosphate released is measured using a malachite green phosphate detection kit. The IC50 is calculated for CR-1-31-B, while CR-1-30-B is expected to show no inhibition of eIF4A ATPase activity. For helicase assays, similar conditions are used, and the unwinding of a duplex RNA substrate is monitored by fluorescence.
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| Cell Assay |
An in vitro cellular protocol for using CR-1-30-B as a negative control involves MUC1-C translation assays. Multiple myeloma cells (e.g., MM.1S, H929) are seeded in 6-well plates at 2×10⁵ cells/well and cultured overnight. The next day, cells are treated with CR-1-31-B (10-100 nM) or CR-1-30-B (10-100 nM) for 4-24 hours. After treatment, cells are harvested and lysed in RIPA buffer. The lysates are separated by SDS-PAGE, transferred to PVDF membranes, and immunoblotted with antibodies against MUC1-C, eIF4A, and a loading control (e.g., beta-actin or GAPDH). CR-1-31-B reduces MUC1-C protein levels in a concentration-dependent manner, while CR-1-30-B has no effect. For translation studies, cells are treated with the compounds for 2-4 hours, and 50-100 microg/mL of cycloheximide is added to arrest translation. The rate of translation is measured by the incorporation of [3⁵S]-methionine into newly synthesized proteins.
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| Animal Protocol |
An in vivo animal protocol for using CR-1-30-B as a negative control involves a xenograft model of multiple myeloma. Female NCr nu/nu mice (6-8 weeks old) are subcutaneously injected with 5×10⁶ MM.1S cells mixed 1:1 with Matrigel in the right flank. When tumors reach approximately 100-150 mm3, mice are randomized into treatment groups (n=8-10 per group). CR-1-31-B (active) and CR-1-30-B (inactive) are formulated in a suitable vehicle (e.g., 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline). The compounds are administered intraperitoneally once daily at 10 mg/kg. A vehicle control group is included. Tumor volumes are measured twice weekly with calipers. Body weights are monitored. At the end of the study (typically 21-28 days), tumors are harvested, weighed, and processed for immunoblotting (MUC1-C, MCL-1, BCL-2) and immunohistochemistry (Ki67, cleaved caspase-3). CR-1-31-B significantly reduces tumor growth and induces apoptosis, while CR-1-30-B has no effect compared to the vehicle control.
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| ADME/Pharmacokinetics |
CR-1-30-B is an inactive epimer and is not characterized by typical pharmacokinetic parameters. As a negative control, it is not intended to have biological activity or specific PK properties. However, as an enantiomer of CR-1-31-B, the physical and chemical properties (solubility, stability, lipophilicity) are similar. In vitro metabolic stability in liver microsomes and plasma protein binding would likely be comparable. The compound is expected to be cleared from the body similarly to its active epimer, but PK studies are rarely conducted because it serves only as a control. Researchers using CR-1-30-B should store it under recommended conditions and consult the supplier for handling instructions.
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| Toxicity/Toxicokinetics |
Toxicity data specific to CR-1-30-B are not available, as it is an inactive negative control used in research. It is expected to have low toxicity due to its lack of target engagement, but formal toxicology studies have not been conducted. The active enantiomer CR-1-31-B has been evaluated for toxicity in preclinical models and is generally well-tolerated at therapeutic doses. CR-1-30-B is for research use only and should be handled with standard laboratory safety precautions (gloves, lab coat, safety glasses). The compound should be stored at -20degC, protected from light and moisture. It should not be used in humans or animals for therapeutic or diagnostic purposes without regulatory approval.
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| References | |
| Additional Infomation |
CR-1-30-B (CAS 1352914-53-4) is the inactive enantiomer of CR-1-31-B, a synthetic rocaglate compound. The active enantiomer CR-1-31-B potently inhibits eIF4A, a key component of the translation initiation complex, by clamping it onto mRNA and blocking cap-dependent translation. This leads to downregulation of short-lived oncoproteins and apoptosis in cancer cells. In contrast, CR-1-30-B has no effect on eIF4A and no effect on MUC1-C translation, making it an ideal negative control for validating rocaglate mechanisms. CR-1-30-B is useful for establishing that the observed biological effects are specifically due to the target (eIF4A) and not due to other structural features. It is a valuable research tool for studying translation regulation, cancer biology, and the mechanism of action of eIF4A inhibitors. This product is for research use only and is not approved for clinical or veterinary use.
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| Molecular Formula |
C28H29NO8
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| Molecular Weight |
507.53
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| Exact Mass |
507.189
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| CAS # |
1352914-53-4
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| PubChem CID |
56946531
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| Appearance |
White to off-white solid powder
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| LogP |
2.7
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
37
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| Complexity |
799
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| Defined Atom Stereocenter Count |
5
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| SMILES |
COC1=CC=C(C=C1)[C@@]23[C@H]([C@@H]([C@@H]([C@@]2(C4=C(O3)C=C(C=C4OC)OC)O)O)C(=O)NOC)C5=CC=CC=C5
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| InChi Key |
KLSIFOJPWJBRFH-DFEWDZLZSA-N
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| InChi Code |
InChI=1S/C28H29NO8/c1-33-18-12-10-17(11-13-18)28-23(16-8-6-5-7-9-16)22(26(31)29-36-4)25(30)27(28,32)24-20(35-3)14-19(34-2)15-21(24)37-28/h5-15,22-23,25,30,32H,1-4H3,(H,29,31)/t22-,23-,25-,27+,28+/m0/s1
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| Chemical Name |
(1S,2S,3R,3aS,8bR)-1,8b-dihydroxy-N,6,8-trimethoxy-3a-(4-methoxyphenyl)-3-phenyl-2,3-dihydro-1H-cyclopenta[b][1]benzofuran-2-carboxamide
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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 Note: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| 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: 200 mg/mL (394.07 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.88 mg/mL (5.67 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 28.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: 2.88 mg/mL (5.67 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 28.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 2.87 mg/mL (5.65 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9703 mL | 9.8516 mL | 19.7033 mL | |
| 5 mM | 0.3941 mL | 1.9703 mL | 3.9407 mL | |
| 10 mM | 0.1970 mL | 0.9852 mL | 1.9703 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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