2. PROTAC Cell Cycle/DNA Damage Apoptosis Epigenetics
  3. PROTACs CDK Caspase PARP Apoptosis
  4. dCDK9-202

dCDK9-202 a potent CDK9 PROTAC degrader with an DC50 value of 3.5 nM. dCDK9-202 exhibits broad-spectrum anti-tumor activity and extensively disrupts the oncogenic transcriptome. dCDK9-202 can activate Caspase-3/7, increase the level of cleaved PARP, and directly induce apoptosis of tumor cells. dCDK9-202 effectively inhibits TC-71 tumor growth without any signs of toxicity in mice. dCDK9-202 can be used for the study of EGFR-driven cancers such as sarcoma (Pink: CDK9 ligand (HY-178862); Blue: CRBN ligand (HY-W248665); Black: Linker (HY-N8015)).

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dCDK9-202

dCDK9-202 Chemical Structure

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dCDK9-202 Related Antibodies

Top Publications Citing Use of Products

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

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PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

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Description

dCDK9-202 a potent CDK9 PROTAC degrader with an DC50 value of 3.5 nM. dCDK9-202 exhibits broad-spectrum anti-tumor activity and extensively disrupts the oncogenic transcriptome. dCDK9-202 can activate Caspase-3/7, increase the level of cleaved PARP, and directly induce apoptosis of tumor cells. dCDK9-202 effectively inhibits TC-71 tumor growth without any signs of toxicity in mice. dCDK9-202 can be used for the study of EGFR-driven cancers such as sarcoma (Pink: CDK9 ligand (HY-178862); Blue: CRBN ligand (HY-W248665); Black: Linker (HY-N8015))[1].

IC50 & Target[1]

CDK9

3.5 nM (DC50)

Caspase-3

 

Caspase-7

 

Cereblon

 

In Vitro

dCDK9-202 (10 nM, 0-24 h) treatment of TC-71 cells within 2 hours can significantly reduce the CDK9 protein level, and complete and nearly continuous degradation was achieved within 8 hours[1].
dCDK9-202 (0.1 nM-1 μM, 24 h) exhibitx nanomolar levels of proliferation inhibitory activity in 12 cancer cell lines derived from various tissues such as lung, liver, bone, and brain. For instance, in TC-71 cells, the IC₅₀ is 8.5 nM[1].
dCDK9-202 (10-50 nM, 24 h) activates Caspase-3/7, increases the level of cleaved PARP, and directly induces apoptosis of TC-71 cells[1].
dCDK9-202 (0.25-25 nM, 6 h) significantly reduces the phosphorylation of Ser2 in the CTD domain of RNA polymerase II (p-Rpb1 Ser2) and downregulates a variety of short half-life proteins that are regulated by CDK9 and are closely related to cancer occurrence in TC-71 cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

dCDK9-202 Related Antibodies

Western Blot Analysis[1]

Cell Line: TC-71 cells
Concentration: 10 and 50 nM
Incubation Time: 24 h
Result: Activated Caspase-3/7, increased the level of cleaved PARP.

Western Blot Analysis[1]

Cell Line: TC-71 cells
Concentration: 0.25, 2.5 and 25 nM
Incubation Time: 6 h
Result: Significantly reduced the phosphorylation of Ser2 in the CTD domain of RNA polymerase II (p-Rpb1 Ser2). Strongly down-regulated a variety of short half-life proteins that are regulated by CDK9 and are closely related to cancer occurrence, such as MYC, MCL1, BCL-xL, etc.
In Vivo

dCDK9-202 (10 mg/kg, i.v., once every other days for 7 doses) significantly inhibits the tumor volume and weight in the mouse xenograft tumor model established in the TC-71 cell line[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: TC-71 cells xenografts model established in NCG mice (female, 6-8 weeks)[1]
Dosage: 10 mg/kg
Administration: Intravenous injection (i.v.), once every other days for 7 doses
Result: Significantly inhibited the tumor volume and weight.
Effectively reduced the level of CDK9 protein in tumor tissues after a single administration 2 hours later.
Did not show any weight loss or other obvious signs of toxicity in mice.
Molecular Weight

803.99

Formula

C40H49N7O7S2
SMILES

CC(C)(C1=CN=C(O1)CSC2=CN=C(S2)NC(C3CCN(CC3)C(CCCCCCCN4CC5=C(C4)C=C6C(N(C(C6=C5)=O)C7CCC(NC7=O)=O)=O)=O)=O)C
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
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dCDK9-202 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

dCDK9-202PROTACsCDKCaspasePARPApoptosisCyclin dependent kinasepoly ADP ribose polymerase PROTACCDK9 degraderTC-71 cell linein vivo antitumor activitykinase selectivitytranscriptional addictionInhibitorinhibitorinhibit

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