Art. -Nr.: HY-173523

KI-CDK9d-32

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KI-CDK9d-32 is a selective CDK9 PROTAC degrader (IC₅₀ = 3 nM; DC₅₀ = 0.89 nM). KI-CDK9d-32 induces CDK9 degradation via the ubiquitin-proteasome pathway to abrogates CDK9 enzymatic and scaffolding functions, downregulates MYC expression and MYC-dependent signaling, represses TNF-alpha signaling pathways activity and pre-rRNA levels. KI-CDK9d-32 disrupts nucleolar homeostasis, blocks cell cycle progression and cellular translation by reducing 4EBP1 phosphorylation, and elicits cancer cell cytotoxicity in a CRBN-dependent manner, while high ABCB1 activity attenuates the efficacy. KI-CDK9d-32 can be used for the research of acute lymphoblastic leukemia, rhabdomyosarcoma, pancreatic adenocarcinoma.
(Pink: CDK9 ligand (HY-153718); Blue: Cereblon ligand (HY-163233); Black: linker (HY-W011657)).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 99.03%
CAS. Nr.: 3054009-82-1
Formel: C₃₉H₄₅N₉O₄
Molecular Weight:703.83

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

KI-CDK9d-32 Chemical Structure

CAS. Nr.: 3054009-82-1

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

KI-CDK9d-32 is a selective CDK9 PROTAC degrader (IC₅₀ = 3 nM; DC₅₀ = 0.89 nM). KI-CDK9d-32 induces CDK9 degradation via the ubiquitin-proteasome pathway to abrogates CDK9 enzymatic and scaffolding functions, downregulates MYC expression and MYC-dependent signaling, represses TNF-alpha signaling pathways activity and pre-rRNA levels. KI-CDK9d-32 disrupts nucleolar homeostasis, blocks cell cycle progression and cellular translation by reducing 4EBP1 phosphorylation, and elicits cancer cell cytotoxicity in a CRBN-dependent manner, while high ABCB1 activity attenuates the efficacy. KI-CDK9d-32 can be used for the research of acute lymphoblastic leukemia, rhabdomyosarcoma, pancreatic adenocarcinoma^[1]. (Pink: CDK9 ligand (HY-153718); Blue: Cereblon ligand (HY-163233); Black: linker (HY-W011657)).

IC₅₀ & Target

CDK9

0.89 nM (DC₅₀)

CDK9

3 nM (IC₅₀)

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle CDK Isoform-spezifische Produkte anzeigen :

In Vitro

KI-CDK9d-32 (0.004-5000 nM; 1-12 h) potently degrades CDK9 in MOLT-4 cells with a DC₅₀ of 0.89 nM after 4 h, achieves near-complete degradation sustained for at least 12 h, and exhibits a maximal degradation rate of 1.04 h^-1 at 126 nM^[1].
KI-CDK9d-32 (50 nM; 4 h) reduces CDK9 protein levels 5-fold and MYC protein levels 3-fold in MOLT-4 cells, along with downregulating MYC-regulated kinases and disrupting cell cycle and ribosome biogenesis pathways^[1].
KI-CDK9d-32 (50 nM; 4 h) selectively inhibits CDK9-mediated phosphorylation in MOLT-4 cells, reduces 4EBP1 phosphorylation to inhibit translation, and disrupts phosphosites linked to mRNA and ribosome-related processes^[1].
KI-CDK9d-32 (15-125 nM; 2-8 h) dose- and time-dependently suppresses MYC mRNA levels in MOLT-4 cells, bypassing the compensatory MYC increase seen with CDK9 inhibition, and reduces CDK9 mRNA levels by 5-fold at 8 h^[1].
KI-CDK9d-32 (15 nM; 2-8 h) induces rapid, sustained downregulation of MYC mRNA (over 6-fold relative to inhibition) in MOLT-4 cells, downregulates TNF-α signaling via NF-κB across MOLT-4, PSN-1, and RH-4 cells, and disrupts MYC target pathways linked to ribosome biogenesis^[1].
KI-CDK9d-32 (up to 1.5 μM; 120 h) has a mean IC₅₀ of 82.6 nM across ~800 human cancer cell lines, with sensitivity driven by CRBN expression and resistance driven by ABCB1 expression^[1].
KI-CDK9d-32 (2 h) induces rapid (within 2 h) disruption of nucleolar homeostasis in HeLa cells by compromising the NPM1-marked nucleolar rim, without affecting the DDX21-marked core granular compartment^[1].
KI-CDK9d-32 (0.1-10 μM) potently inhibits CDK9/cyclin T1 with a biochemical IC₅₀ of 3 nM at 10 mM ATP, exhibits >1403-fold selectivity over most tested kinases, and inhibits ~90% of CDK9 activity at 100 nM with no off-target kinase inhibition^[1].
KI-CDK9d-32 (10-100 nM; 4 h) destabilizes nucleolar homeostasis in HeLa cells^[1].
KI-CDK9d-32 (100 nM; 4 h) induces significant disruption and dissolution of nucleolar structure in HeLa cells^[1].
KI-CDK9d-32 (100 nM; 4 h) significantly reduces pre-rRNA (5'-ETS) levels in HeLa cells^[1].
KI-CDK9d-32 (15 nM; 4-8 h) significantly downregulates multiple core regulatory circuitry gene transcripts in MOLT-4, PSN-1, and RH-4 cells, with stronger effects observed at 8 h^[1].
KI-CDK9d-32 (50 nM; 4 h) induces potent degradation of CDK9 (fold change -4.81), with no detectable degradation of other tested kinase targets in a quantitative mass spectrometry assay^[1].
KI-CDK9d-32 (50 nM; 4 h) induces degradation of CDK9 and c-MYC, and reduces pSer2, POLR2A levels in PSN-1, RH-4, and HeLa cells, with degradation reversed by MG-132 (HY-13259) co-treatment^[1].
KI-CDK9d-32 (50 nM; 4 h) does not affect CDK7 protein levels in MOLT-4 cells, demonstrating selectivity for CDK9 over its homologue CDK7^[1].
KI-CDK9d-32 (15-125 nM; 4 h) induces dose-dependent degradation of CDK9 and MYC in MOLT-4 cells^[1].
KI-CDK9d-32 (15 nM; 4 h) induces significant enrichment of HALLMARK MYC TARGETS V2 and HALLMARK TNFA via NFKB gene sets in MOLT-4 cells, enrichment of these sets in PSN-1 cells, and enrichment of HALLMARK DNA REPAIR in RH-4 cells^[1].
KI-CDK9d-32 (0.69 nM-1.5 µM) reduces viability of ~800 tested cancer cell lines in a dose-dependent manner, with cell line sensitivity correlated with CRBN expression and resistance correlated with ABCB1 expression, as measured via the Broad Institute PRISM high-throughput platform^[1].

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

Real Time qPCR^[1]

Cell Line:

MOLT-4 human acute lymphoblastic leukemia cells
Concentration:

15; 50; 125 nM
Incubation Time:

2, 4, 8 h
Result:

Significantly suppressed MYC mRNA transcription in a dose- and time-dependent manner at all tested concentrations, in contrast to the compensatory MYC mRNA increase induced by CDK9 inhibition with KB-0742.
Reduced CDK9 mRNA levels by 5-fold at 8 h, while effects on CDK9 transcript levels were not clearly distinct from inhibition at early time points.

Cell Viability Assay^[1]

Cell Line:

MOLT-4 human acute lymphoblastic leukemia cells, PSN-1 human pancreatic adenocarcinoma cells, RH-4 human rhabdomyosarcoma cells
Concentration:

Up to 500 nM
Incubation Time:

72, 120 h
Result:

Exhibited potent cytotoxicity with IC₅₀ values of 2.8 nM (72 h) and 1.70 nM (120 h) in MOLT-4 cells; 21.3 nM (72 h) and 73.85 nM (120 h) in PSN-1 cells; 52.9 nM (72 h) and 81.94 nM (120 h) in RH-4 cells.

Western Blot Analysis^[1]

Cell Line:

PSN-1, RH-4, HeLa cells
Concentration:

50 nM
Incubation Time:

4 h
Result:

Induced degradation of CDK9 and c-MYC, and reduced levels of pSer2, POLR2A in PSN-1, RH-4, and HeLa cells.
Degradation was rescued by co-treatment with MG-132.

Western Blot Analysis^[1]

Cell Line:

MOLT-4 cells
Concentration:

50 nM
Incubation Time:

4 h
Result:

Did not alter CDK7 protein levels relative to control.

Real Time qPCR^[1]

Cell Line:

unspecified cell line
Concentration:

50 nM
Incubation Time:

4 h
Result:

Reduced relative expression of CDK9, MYC, AURKA, and PLK1 compared to DMSO control.

Western Blot Analysis^[1]

Cell Line:

MOLT-4 cells
Concentration:

15; 50; 125 nM
Incubation Time:

4 h
Result:

Induced degradation of CDK9 and MYC at all tested concentrations.

Immunofluorescence^[1]

Cell Line:

HeLa cells
Concentration:

10; 50; 100 nM
Incubation Time:

4 h
Result:

Compromised nucleolar rim structure and altered NPM1 and DDX21 localization at all tested concentrations, with effects visible at the lowest concentration of 10 nM.

Real Time qPCR^[1]

Cell Line:

HeLa cells
Concentration:

100 nM
Incubation Time:

4 h
Result:

Induced a significant reduction in pre-rRNA (5'-ETS) levels compared to DMSO control.

Chemical Information

CAS. Nr. 3054009-82-1
Appearance Solid
Molecular Weight 703.83
Formel C₃₉H₄₅N₉O₄
Color White to off-white
SMILES

O=C(N[C@H]1C[C@H](NC2=CC(CCC)=NC3=CC=NN23)CC1)C4=CC=C(CN5CCN(C6=CC7=C(C(N(C(CC8)C(NC8=O)=O)C7)=O)C=C6)CC5)C=C4
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (142.08 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.4208 mL

7.1040 mL

14.2080 mL

5 mM

0.2842 mL

1.4208 mL

2.8416 mL

10 mM

0.1421 mL

0.7104 mL

1.4208 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (3.55 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (3.55 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (3.55 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (283 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Toure MA, et al. Targeted degradation of CDK9 potently disrupts the MYC-regulated network. Cell chemical biology. 2025 Apr 17;32(4):542-555.e10. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.4208 mL	7.1040 mL	14.2080 mL	35.5199 mL
	5 mM	0.2842 mL	1.4208 mL	2.8416 mL	7.1040 mL
	10 mM	0.1421 mL	0.7104 mL	1.4208 mL	3.5520 mL
	15 mM	0.0947 mL	0.4736 mL	0.9472 mL	2.3680 mL
	20 mM	0.0710 mL	0.3552 mL	0.7104 mL	1.7760 mL
	25 mM	0.0568 mL	0.2842 mL	0.5683 mL	1.4208 mL
	30 mM	0.0474 mL	0.2368 mL	0.4736 mL	1.1840 mL
	40 mM	0.0355 mL	0.1776 mL	0.3552 mL	0.8880 mL
	50 mM	0.0284 mL	0.1421 mL	0.2842 mL	0.7104 mL
	60 mM	0.0237 mL	0.1184 mL	0.2368 mL	0.5920 mL
	80 mM	0.0178 mL	0.0888 mL	0.1776 mL	0.4440 mL
	100 mM	0.0142 mL	0.0710 mL	0.1421 mL	0.3552 mL

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KI-CDK9d-32

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle CDK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

KI-CDK9d-32 Related Classifications

HY-173523 Related Classifications