CKD-731
CKD-731 is a MetAP2 inhibitor (IC50 = 0.96 nM) that inhibits methionine aminopeptidase 2 through covalent binding to His-231 and inhibits endothelial cell growth and proliferation. CKD-731 has poor aqueous solubility and can be used in cancer research.
For research use only. We do not sell to patients.
- CAS No.: 251111-15-6
- Formula: C28H38O8
- Molecular Weight:502.60
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[2]|
MetAp2 0.96 nM (IC50) |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HUVEC | EC50 |
2.6 nM
|
Inhibition of HUVEC proliferation assessed by SRB assay.
Inhibition of HUVEC proliferation assessed by SRB assay.
|
14604668 |
In Vitro
CKD-731 (compound 1) inhibits MetAP2 with an IC50 of 0.96 nM in a cell-free enzymatic assay[2].
CKD-731 inhibits HUVEC proliferation with an EC50 of 2.6 nM in the SRB assay[2].
CKD-731 inhibits endothelial cell proliferation with 1000-fold higher potency than TNP-470[3].
CKD-731 inhibits endothelial cell proliferation with 1000-fold higher potency than TNP-470[4].
CKD-731 (compound 9) potently inhibits porcine pulmonary artery endothelial cell proliferation with an IC50 of 0.03 pg/mL, being 1000-fold more potent than TNP-470[5].
CKD-731 (compound 1c) inhibits calf endothelial cell proliferation with an IC50 of 0.03 pg/mL[6].
CKD-731 inhibits endothelial cell proliferation with 1000-fold higher potency than TNP-470[7].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS No. 251111-15-6
-
Molecular Weight 502.60
-
Formula C28H38O8
-
SMILES
O=C(O[C@H](CC1)[C@@H](OC)[C@H]([C@@]2(C)O[C@@H]2C/C=C(C)\C)[C@]31CO3)/C=C/C4=CC(OC)=C(OC)C(OC)=C4
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Chun E, et al. Novel inhibitors targeted to methionine aminopeptidase 2 (MetAP2) strongly inhibit the growth of cancers in xenografted nude model. International journal of cancer. 2005 Mar 10;114(1):124-30. [Content Brief]
[5]. Yin SQ, et al. The development of MetAP-2 inhibitors in cancer treatment. Current medicinal chemistry. 2012;19(7):1021-35. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)