CDK12 ligand-3
CDK12 ligand-3 is a monovalent CDK12/13 and cyclin K molecular glue degrader. CDK12 ligand-3 recruits DDB1, a core component of CUL4-based E3 ubiquitin ligase complexes, to drive ubiquitination and degradation of its targets.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- CAS No.: 3093763-27-7
- 화학식: C25H28ClN5O3S
- 분자량:514.04
-
보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- 순도&문서
- References
-
Help & FAQs
Biological Activity
제품 설명
IC50 & Target
[1]|
CDK12/Cyclin K |
CDK13/Cyclin K |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HEK-293T | DC50 |
35 nM
|
Degradation of CDK12 in CRISPR/Cas9-modified HEK293T cells after 6 h incubation measured by HiBiT-CDK12 degradation assay.
Degradation of CDK12 in CRISPR/Cas9-modified HEK293T cells after 6 h incubation measured by HiBiT-CDK12 degradation assay.
|
40626960 |
| HEK-293T | DC50 |
>10 μM
|
Degradation of CDK12 in DDB1-knockout HEK293T cells after 3 h incubation measured by HiBiT-CDK12 degradation assay.
Degradation of CDK12 in DDB1-knockout HEK293T cells after 3 h incubation measured by HiBiT-CDK12 degradation assay.
|
40626960 |
| HEK-293T | DC50 |
57 nM
|
Degradation of CDK13 in CRISPR/Cas9-modified HEK293T cells after 6 h incubation measured by HiBiT-CDK13 degradation assay.
Degradation of CDK13 in CRISPR/Cas9-modified HEK293T cells after 6 h incubation measured by HiBiT-CDK13 degradation assay.
|
40626960 |
| Jurkat | IC50 |
22 nM
|
Antiproliferative activity against Jurkat cells after 72 h incubation measured by cell viability antiproliferative assay.
Antiproliferative activity against Jurkat cells after 72 h incubation measured by cell viability antiproliferative assay.
|
40626960 |
| Jurkat | IC50 |
580 nM
|
Antiproliferative activity against Jurkat cells pretreated with NAE inhibitor MLN-4924 for 1 h followed by 72 h of compound treatment measured by cell viability antiproliferative assay.
Antiproliferative activity against Jurkat cells pretreated with NAE inhibitor MLN-4924 for 1 h followed by 72 h of compound treatment measured by cell viability antiproliferative assay.
|
40626960 |
In Vitro
CDK12 ligand-3 (10-10000 nM; 6 h) potently degrades CDK12 in HEK293T cells via a DDB1- and ubiquitin-proteasome system-dependent mechanism, with a DC50 of 35 nM after 6 h treatment[1].
CDK12 ligand-3 (10-10000 nM; 6 h) potently degrades CDK13 in HEK293T cells with a DC50 of 57 nM after 6 h treatment[1].
CDK12 ligand-3 (0.01-10 μM; 6 h) induces dose-dependent degradation of CDK12, CDK13, and Cyclin K, and inhibits RNA polymerase II phosphorylation in Jurkat cells after 6 h treatment, with complete cyclin K depletion at 1 μM after 0.5 h[1].
CDK12 ligand-3 (100 nM; 3 h) selectively degrades CDK12, CDK13, and Cyclin K in Jurkat cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:Jurkat cells
-
Concentration:0.01-10 μM (6 h incubation); 1 μM (0.5 h incubation for cyclin K depletion)
-
Incubation Time:6 h (direct treatment); 0.5 h (time-dependent cyclin K depletion)
-
Result:Induced dose-dependent degradation of CDK12, CDK13, and Cyclin K.
Induced dose-dependent inhibition of RNA polymerase II phosphorylation (p-Rpb1 CTD Ser2).
Achieved complete depletion of cyclin K at 1 μM for 0.5 h.
-
Cell Line:Jurkat cells
-
Concentration:10-10000 nM (72 h incubation)
-
Incubation Time:72 h (direct treatment); 1 h (MLN-4924 pre-incubation) followed by 72 h
-
Result:Exhibited potent antiproliferative activity with an IC50 of 22 nM.
Reduced antiproliferative activity when cells were pretreated with MLN-4924, resulting in an IC50 of 580 nM.
Chemical Information
-
CAS No. 3093763-27-7
-
분자량 514.04
-
화학식 C25H28ClN5O3S
-
SMILES
ClC1=CN=C(N[C@H]2CN(CCC2)C(C3=CC=CC=C3)=O)N=C1NC4=CC=CC=C4S(=O)(C(C)C)=O
-
선적
Room temperature in continental US; may vary elsewhere.
-
보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CDK12 ligand-3 Related Classifications
HY-177786 Related Classifications
Powered by Bioz