2. Cell Cycle/DNA Damage Epigenetics
  3. HDAC CDK
  4. CDK/HDAC-IN-3

CDK/HDAC-IN-3 is an orally active HDACs/CDKs dual inhibitor. CDK/HDAC-IN-3 has potent and selective inhibition of CDK9, CDK12, CDK13, HDAC1, HDAC2 and HDAC3 with IC50 values of 98.32 nM, 98.85 nM, 100 nM, 62.12 nM, 93.28nM and 82.87 nM. CDK/HDAC-IN-3 can be used for the acute myeloid leukemia (AML) .

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CDK/HDAC-IN-3 Chemical Structure

CDK/HDAC-IN-3 Chemical Structure

CAS No. : 2944087-54-9

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5 mg USD 455 In-stock
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Based on 1 publication(s) in Google Scholar

CDK/HDAC-IN-3 Related Antibodies

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Description

CDK/HDAC-IN-3 is an orally active HDACs/CDKs dual inhibitor. CDK/HDAC-IN-3 has potent and selective inhibition of CDK9, CDK12, CDK13, HDAC1, HDAC2 and HDAC3 with IC50 values of 98.32 nM, 98.85 nM, 100 nM, 62.12 nM, 93.28nM and 82.87 nM. CDK/HDAC-IN-3 can be used for the acute myeloid leukemia (AML) [1].
IC50 & Target

IC50: 98.32 nM (CDK9), 98.85 nM (CDK12), 100 nM (CDK13), 62.12 nM (HDAC1), 93.28nM (HDAC2) and 82.87 nM (HDAC3), 0.72 μM (U937 cell), 1.43μM (HL-60 cell), 1.63μM (SKNO-1 cell) and 0.89 μM (Kaumi-1 cell)[1].
In Vitro

CDK/HDAC-IN-3 (compound 33a) (1μM) has potent and selective inhibition of CDK9, CDK12, CDK13, HDAC1, HDAC2 and HDAC3 with IC50 values of 98.32 nM, 98.85 nM, 100 nM, 62.12 nM, 93.28nM and 82.87 nM, respectively[1].
CDK/HDAC-IN-3 (0.5 μM, 1.0 μM) significantly induces differentiation of leukemic stem-like cells and inhibits AML proliferation[1].
CDK/HDAC-IN-3 (0.5 μM, 1.0 μM, 2.0 μM) significantly induced differentiation of LSCs[1].
CDK/HDAC-IN-3 has inhibitory effect for U937, HL-60, SKNO-1 and Kaumi-1 cell with IC50 values of 0.72 μM, 1.43μM, 1.63μM and 0.89 μM, respectively[1].

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

CDK/HDAC-IN-3 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: Human leukemia cell lines Kaumi-1, Skno-1, HL-60 and U937
Concentration: At different concentrations
Incubation Time: 72 h
Result: Showed strong growth inhibitory potency against AML cells.

Western Blot Analysis[1]

Cell Line: HL-60 cell
Concentration: 0, 30, 100, 300, 1000 nM
Incubation Time: 6 h
Result: Inhibited the downstream signaling of HDAC and CDK9 in a dose-dependent manner.

Apoptosis Analysis[1]

Cell Line: HL-60 and U937 cell
Concentration: 0.2, 0.5, 1.0, 2.0 μM
Incubation Time: 48 h
Result: Induced apoptosis of AML cells.
In Vivo

CDK/HDAC-IN-3 (compound 33a) (i.v., p.o.; 5, 25 mg/kg) has relatively adequate oral bioavailability[1].

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

Animal Model: Sprague-Dawley male rats (220-350 g)[1]
Dosage: 5 mg/kg and 25 mg/kg
Administration: IV and PO
Result:
PK parameters i.v (5 mg/Kg) p.o (25 mg/Kg)
Cmax(ng/L) 3644.00 1426.00
T1/2(h) 0.11 1.37
TMax(h) NA 0.75
Clearance (mL/h/kg) 5307.00 1726.00
MRT (h) 0.39 1.27
AUC (ng.h/mL) 836.00 2368.00
F% NA 56.70%
Molecular Weight

509.34

Formula

C24H18Cl2N6O3
CAS No.
Appearance

Solid

Color

Yellow to brown

SMILES

NC1=C(C=CC=C1)NC(C2=CC=C(C=C2)NC(C3=NNC=C3NC(C4=C(C=CC=C4Cl)Cl)=O)=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (245.42 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9633 mL 9.8166 mL 19.6333 mL
5 mM 0.3927 mL 1.9633 mL 3.9267 mL
View the Complete Stock Solution Preparation Table

* 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.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* 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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9633 mL 9.8166 mL 19.6333 mL 49.0831 mL
5 mM 0.3927 mL 1.9633 mL 3.9267 mL 9.8166 mL
10 mM 0.1963 mL 0.9817 mL 1.9633 mL 4.9083 mL
15 mM 0.1309 mL 0.6544 mL 1.3089 mL 3.2722 mL
20 mM 0.0982 mL 0.4908 mL 0.9817 mL 2.4542 mL
25 mM 0.0785 mL 0.3927 mL 0.7853 mL 1.9633 mL
30 mM 0.0654 mL 0.3272 mL 0.6544 mL 1.6361 mL
40 mM 0.0491 mL 0.2454 mL 0.4908 mL 1.2271 mL
50 mM 0.0393 mL 0.1963 mL 0.3927 mL 0.9817 mL
60 mM 0.0327 mL 0.1636 mL 0.3272 mL 0.8181 mL
80 mM 0.0245 mL 0.1227 mL 0.2454 mL 0.6135 mL
100 mM 0.0196 mL 0.0982 mL 0.1963 mL 0.4908 mL
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CDK/HDAC-IN-3 Related Classifications

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  • 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:

CDK/HDAC-IN-32944087-54-9HDACCDKHistone deacetylasesCyclin dependent kinaseacute myeloid leukemia (AML)Leukemic stem cellscell differentiationInhibitorinhibitorinhibit

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