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cdks

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1146

Inhibitors & Agonists

5

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1

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4

Biochemical Assay Reagents

16

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50

Natural
Products

17

Isotope-Labeled Compounds

8

Click Chemistry

73

Oligonucleotides

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-13914
    Roniciclib
    2 Publications Verification

    BAY 1000394

    		 CDK Cancer
    Roniciclib is an orally bioavailable pan-cyclin dependent kinase (CDK) inhibitor, with IC50s of 5-25 nM for CDK1, CDK2, CDK3, CDK4, CDK7 and CDK9.
    Roniciclib
  • HY-130665
    TL12-186
    1 Publications Verification

    		 PROTACs CDK Cancer
    TL12-186 is a Cereblon-dependent multi-kinase PROTAC degrader. Multi-kinases include CDK, BTK, FLT3, Aurora kinases, TEC, ULK, ITK, et al. TL12-186 inhibits CDK2/cyclin A (IC50=73 nM) and CDK9/cyclin T1 (IC50=55 nM) .
    TL12-186
  • HY-10014
    R547
    2 Publications Verification

    		 CDK GSK-3 Apoptosis Cancer
    R547 is a potent, selective and orally active ATP-competitive CDK inhibitor, with Kis of 2 nM, 3 nM and 1 nM for CDK1/cyclin B, CDK2/cyclin E and CDK4/cyclin D1, respectively .
    R547
  • HY-116035
    Nimbolide
    2 Publications Verification

    		 Wnt NF-κB CDK Apoptosis Cancer
    Nimbolide is a triterpene compound that can be isolated from neem (Azadirachta indica), possesses anticancer and antiproliferative activity. Nimbolide induces tumor cell apoptosis by inhibiting NF-κB and CDK4/CDK6 kinase. Nimbolide suppresses the Wnt, PI3K-Akt, MAPK and JAK-STAT signaling pathways .
    Nimbolide
  • HY-108359
    Alsterpaullone
    1 Publications Verification

    9-Nitropaullone; NSC 705701

    		 CDK GSK-3 Apoptosis Cancer
    Alsterpaullone (9-Nitropaullone) is a potent CDK inhibitor, with IC50s of 35 nM, 15 nM, 200 nM and 40 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E and CDK5/p35, respectively. Alsterpaullone also competes with ATP for binding to GSK-3alpha/GSK-3beta with IC50s of both 4 nM. Alsterpaullone has antitumor activity, and possesses potential for the study in neurodegenerative and proliferative disorders . Alsterpaullone induces apoptosis in leukemia cell line .
    Alsterpaullone
  • HY-18299A
    Purvalanol A
    4 Publications Verification

    NG-60

    		 CDK Autophagy Apoptosis Cancer
    Purvalanol A is a potent CDK inhibitor, which inhibits cdc2-cyclin B, cdk2-cyclin A, cdk2-cyclin E, cdk4-cyclin D1, and cdk5-p35 with IC50s of 4, 70, 35, 850, 75 nM, resepctively.
    Purvalanol A
  • HY-11009
    CGP60474
    5+ Cited Publications

    		 CDK PKC Cancer
    CGP60474, a highly potent anti-endotoxemic agent, is a potent cyclin-dependent kinase (CDK) inhibitor (IC50 values are 26, 3, 4, 216, 10, 200 and 13 nM for CDK1/B, CDK2/E, CDK2/A, CDK4/D, CDK5/p25, CDK7/H and CDK9/T, respectively). CGP60474 is a selective and ATP-competitive PKC inhibitor .
    CGP60474
  • HY-164664
    CDK2-IN-30

    		CDK Cancer
    CDK2-IN-30 is a CDK2 inhibitor with an IC50 value ≤20 nM. CDK2-IN-30 modulates CDK2 activity to influence cell cycle regulation. CDK2-IN-30 can be used for the research of cancer .
    CDK2-IN-30
  • HY-50914
    AZD5597

    		CDK Cancer
    AZD5597 is an inhibitor of CDK with IC50 values of both 2 nM for CDK1 and CDK2. AZD5597 can inhibit the proliferation of tumor cells and has anti-tumor activity .
    AZD5597
  • HY-104013
    Aminopurvalanol A
    1 Publications Verification

    		 CDK Apoptosis Cancer
    Aminopurvalanol A is a potent, selective, and cell permeable inhibitor of Cyclins/Cdk complexes. Aminopurvalanol A preferentially targets the G2/M-phase transition inhibiting cancer cell differentiation. Aminopurvalanol A causes the inhibition of sperm fertilizing ability via the inhibition of physiological capacitation-dependent actin polymerization .
    Aminopurvalanol A
  • HY-112626
    CDK12-IN-2
    1 Publications Verification

    		 CDK Cancer
    CDK12-IN-2 is a potent, selective and nanomolar CDK12 inhibitor (IC50=52 nM) with good physicochemical properties. CDK12-IN-2 is also a strong CDK13 inhibitor due to CDK13 is the closest homologue of CDK12. CDK12-IN-2 shows excellent kinase selectivity for CDK12 over CDK2, 9, 8, and 7. CDK12-IN-2 inhibits the phosphorylation of Ser2 in the C-terminal domain of RNA polymerase II. CDK12-IN-2 can be used an excellent chemical probe for functional studies of CDK12 .
    CDK12-IN-2
  • HY-50943
    AT7519 Hydrochloride
    10+ Cited Publications

    		 CDK Apoptosis Cancer
    AT7519 Hydrochloride is a potent inhibitor of CDKs, with IC50s of 210, 47, 100, 13, 170, and <10 nM for CDK1, CDK2, CDK4 to CDK6, and CDK9, respectively.
    AT7519 Hydrochloride
  • HY-111427
    CDK8/19-IN-1

    		CDK Cancer
    CDK8/19-IN-1 is a potent, selective and oral bioavailable CDK8/19 dual inhibitor, with IC50s of 0.46 nM, 0.99 nM and 270 nM for CDK8, CDK19 and CDK9, respectively.
    CDK8/19-IN-1
  • HY-46568
    CDK7/12-IN-1

    		CDK Cancer
    CDK7/12-IN-1 is a selective CDK7/12 inhibitor with IC50s of 3 and 277 nM for CDK7 and CDK 12, respectively. CDK7 and CDK12 inhibition is an effective strategy to inhibit tumour growth .
    CDK7/12-IN-1
  • HY-112272A
    Lerociclib dihydrochloride
    2 Publications Verification

    G1T38 dihydrochloride

    		 CDK Cancer
    Lerociclib dihydrochloride (G1T38 dihydrochloride) is a potent and selective inhibitor of CDK4/CDK6, with IC50s of 1 nM and 2 nM for CDK4/CyclinD1 and CDK6/CyclinD3, respectively.
    Lerociclib dihydrochloride
  • HY-145694
    CDK5-IN-3

    		CDK Others
    CDK5-IN-3 (compound 11) is a potent CDK5 inhibitor, with IC50s of 0.6 nM and 18 nM for CDK5/p25 and CDK2/CycA, respectively. CDK5-IN-3 can be used for the research of autosomal dominant polycystic kidney disease (ADPKD) .
    CDK5-IN-3
  • HY-W478102
    CDK2-IN-13

    		CDK Cancer
    CDK2-IN-13 (Compound 15) is a CDK2 inhibitor with an IC50 of 12 µM. CDK2-IN-13 can be used in research of cancer .
    CDK2-IN-13
  • HY-W007367
    2,6-Dichloropurine

    		Drug Intermediate Others
    2,6-Dichloropurine is a pharmaceutical intermediate. 2,6-Dichloropurine can be used to synthesize various PDE inhibitors, human A3 adenosine receptor (AR) antagonists, and CDK inhibitors .
    2,6-Dichloropurine
  • HY-146213
    CDK4/6-IN-12

    		CDK Cancer
    CDK4/6-IN-12 is a potent cyclin-dependent kinase 4/6 (CDK4/6) inhibitor. CDK4/6-IN-12 has enzymatic inhibitory activity for CDK4 and CDK6 with IC50 of 592.3 nM and 3090 nM, respectively. CDK4/6-IN-12 can be used for the research of cancer .
    CDK4/6-IN-12
  • HY-139725
    CDK5-IN-1
    1 Publications Verification

    		 CDK Metabolic Disease
    CDK5-IN-1 is a potent CDK5 inhibitor with an IC50 less than 10 nM. CDK5-IN-1 is greater than 100-fold more active against CDK5 than CDK2. CDK5-IN-1 is used for kidney diseases research .
    CDK5-IN-1
  • HY-145693
    CDK5-IN-2

    		CDK Others
    CDK5-IN-2 (compound 15) is a highly selective CDK5 inhibitor with IC50s of 0.2 and 23 for CDK5/p25 and CDK2/CycA, respectively .
    CDK5-IN-2
  • HY-151069
    TMX-2039

    		Ligands for Target Protein for PROTAC CDK Cancer
    TMX-2039 is a pan-CDK inhibitor for both cell cycle CDKs (CDK1, CDK2, CDK4, CDK5 and CDK6) and transcriptional CDKs (CDK7 and CDK9), with IC50s of 2.6, 1.0, 52.1, 0.5, 35.0, 32.5 and 25 nM, respectively. TMX-2039 acts as a Ligands for Target Protein for PROTACs .
    TMX-2039
  • HY-158170
    CDK7-IN-28

    		CDK Cancer
    CDK7-IN-28 (CDK7-1276) is a potent CDK7 inhibitor(IC50＜5 nM). CDK7-IN-28 can inhibit proliferation of MDA-MB-468 cell line by blocking cell cycle and inhibiting DNA replication .
    CDK7-IN-28
  • HY-153336
    PRT3645

    		CDK Cancer
    PRT3645 (Example 20) is a CDK Inhibitor. CDK-IN-12 Inhibits CDK4/6 with IC50 values less than 20 nM .
    PRT3645
  • HY-149819
    CDK/HDAC-IN-3

    		HDAC CDK Cancer
    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) .
    CDK/HDAC-IN-3
  • HY-153088
    CDK4/6-IN-16

    		CDK Cancer
    CDK4/6-IN-16 (example 195) is a potent CDK4 and CDK6 inhibitor, with an IC50 of 0.013 μM for CDK4. CDK4/6-IN-16 can be used for the research of CDK4-mediated disorders, such as cancer .
    CDK4/6-IN-16
  • HY-115992
    CDK4/6-IN-9

    		CDK Cancer
    CDK4/6-IN-9 (compound 10) is a selective CDK4/6 inhibitor with an IC50 of 905 nM for CDK6/cyclin D1. CDK4/6-IN-9 has the potential for multiple myeloma (MM) research .
    CDK4/6-IN-9
  • HY-134622
    GSK-3/CDK5/CDK2-IN-1

    		CDK GSK-3 Neurological Disease Cancer
    GSK-3/CDK5/CDK2-IN-1, an imidazole derivative, is an inhibitor of cdk5, cdk2, and GSK-3 extracted from patent WO2002010141A1, example 9a. GSK-3/CDK5/CDK2-IN-1 can be used for the research of cancer, and neurodegenerative diseases .
    GSK-3/CDK5/CDK2-IN-1
  • HY-P2559
    CDK7/9 tide

    		CDK Cancer
    CDK7/9 tide is peptide substrate for CDK7 or CDK9 .
    CDK7/9 tide
  • HY-179023
    CDK9-IN-45

    		CDK Apoptosis Reactive Oxygen Species (ROS) Caspase Bcl-2 Family c-Myc IAP Cancer
    CDK9-IN-45 (Compound B11) is a highly selective CDK9 inhibitor with IC50 values for CDK9 and CDK1 of 7.13 and 489.5 nM respectively. CDK9-IN-45 exhibits a potent inhibitory effect on colorectal cancer cells. CDK9-IN-45 induces cell apoptosis and leads to significant accumulation of ROS. CDK9-IN-45 activates Caspase-3, downregulates Mcl-1, XIAP, and c-Myc. CDK9-IN-45 can be used for research on colorectal cancer .
    CDK9-IN-45
  • HY-157297
    CDK-IN-13

    		CDK Cancer
    CDK-IN-13 (compound 32E) is a potent and selective inhibitor of CDK12/cyclinK with an IC50 of 3 nM. CDK-IN-13 inhibits the growth of the HER2-positive breast cancer cell lines .
    CDK-IN-13
  • HY-112371
    (S)-CR8

    		CDK Cancer
    (S)-CR8 is the S-isomer of CR8. (S)-CR8 is a potent and selective CDK inhibitor with IC50s of 0.060, 0.080, 0.11, 0.12, and 0.15 μM for CDK2/cyclin E, CDK2/cyclin A, CDK9/cyclin T, CDK5/p25, and CDK1/cyclin B, respectively. (S)-CR8 reduces SH-SY5Y cells survival (IC50 0.40 μM) .
    (S)-CR8
  • HY-108420
    INK4C-IN-2
    1 Publications Verification

    		 CDK Cancer
    INK4C-IN-2 is a p18 INK4C inhibitor. NK4C-IN-2 promotes hematopoietic stem cells (HSCs) division by inhibiting INK4C and activating CDK4/6, with an ED50 of 5.21 nM. INK4C-IN-2 shows no cytotoxic to normal 32D cells, HSCs, leukemia cell lines and myeloma cell lines .
    INK4C-IN-2
  • HY-177743
    TR-213

    		Molecular Glues CDK DNA/RNA Synthesis Cancer
    TR-213 is a potent molecular glue degrader that targets Cyclin K (CDK). TR-213 induces 91% and 56% decrease in CDK12 and Cyclin at 1 μM. TR-213 can inhibit RNA polymerase II activity and regulates alternative polyadenylation (APA) activity. TR-213 can be used for the research of cancer .
    TR-213
  • HY-151878
    CDK7-IN-20

    		CDK GSK-3 Metabolic Disease
    CDK7-IN-20 is a potent, selective and irreversible CDK7 (CDK) inhibitor with an IC50 value of 4 nM. CDK7-IN-20 displays >206-fold selectivity for CDK7 over CDK1, CDK2, CDK3, CDK5, CDK6, CDK9 and CDK12 . CDK7-IN-20 has the potential for autosomal dominant polycystic kidney disease (ADPKD) research .
    CDK7-IN-20
  • HY-145655
    CDK7-IN-11

    		CDK Cancer
    CDK7-IN-11 is an orally active CDK7 inhibitor. CDK7-IN-11 exhibits high CDK7 inhibitory activity with IC50 value of 4.2 nM. CDK7-IN-11 can be effectively used for the research of diseases associated with CDK7 .
    CDK7-IN-11
  • HY-151984
    CDK9-IN-22

    		CDK Cancer
    CDK9-IN-22 is a potent CDK9 inhibitor with IC50s of 10.4, 876.2 nM for CDK9, CDK, respectively. CDK9-IN-22 induces apoptosis and cell cycle arrests at G2/M phase. CDK9-IN-22 decreases the expression of p-RNAPII (S2) and CDK9 protein. CDK9-IN-22 shows antiproliferative and aiti-tumor activity .
    CDK9-IN-22
  • HY-112450
    Olomoucine II

    		CDK Cancer
    Olomoucine II is a potent CDK inhibitor with IC50 values of 0.06, 0.1, 0.45, 7.6, 19.8 µM for CDK9/cyclin T, CDK2/cyclin E, CDK7/cyclin H, CDK1/cyclin B, CDK4/cyclin D1, respectively. Olomoucine II shows antiproliferative activity .
    Olomoucine II
  • HY-161708
    PROTAC FLT3/CDKs degrader-1

    		PROTACs CDK FLT3 Cancer
    PROTAC FLT3/CDKs degrader-1 (Compound C3) is a degrader for cyclin-dependent kinases (DC50 is 18.73 nM for CDK2) and the FMS-like tyrosine kinase 3 (FLT3). PROTAC FLT3/CDKs degrader-1 induces differentation of HL-60 (72.77% differentation at 6.25 nM), inhibits proliferation of AML cells, with IC50s of 2.9-37 nM. PROTAC FLT3/CDKs degrader-1 is potential for ameliorating acute myeloid leukemia. (Pink: ligand for target protein FLT3/CDKs ligand-1 (HY-161709); Black: linker (HY-W012935); Black: ligand for E3 ligase Thalidomide 5-fluoride (HY-W087383))
    PROTAC FLT3/CDKs degrader-1
  • HY-169048
    CDK2/4-IN-2

    		CDK Cancer
    CDK2/4-IN-2 (compound 56) is a CDK2 and CDK4 dual inhibitor with IC50s less than 100 nM. CDK2/4-IN-2 can be used in the study of cancer .
    CDK2/4-IN-2
  • HY-147386
    CDK-IN-10

    		CDK Cancer
    CDK-IN-10 (example 54) is a cyclin dependent kinase (CDK) inhibitor that can be used in cancer research .
    CDK-IN-10
  • HY-146253
    CDK1/2/4-IN-1

    		CDK Apoptosis Bcl-2 Family Caspase Cancer
    CDK1/2/4-IN-1 (compound 3a) is a potent CDK inhibitor with IC50 values of 1.47, 0.78 and 0.87 μM for CDK1, CDK2 and CDK4, respectively. CDK1/2/4-IN-1 arrests cell cycle at G2/M phase and induces apoptosis. CDK1/2/4-IN-1 elevates Bax, caspase-3, P53 levels and decreases Bcl-2 level. CDK1/2/4-IN-1 can be used for cancer research .
    CDK1/2/4-IN-1
  • HY-P11013
    p27

    		CDK Cancer
    p27, a CDK inhibitor, is a SCFSkp2/Cks1 substrate. p27 can be used for the study of cancer .
    p27
  • HY-114248
    AGM-130

    		CDK Cancer
    AGM-130 is a cyclin-dependent kinase (CDK) inhibitor. AGM-130 exhibits antitumor activity .
    AGM-130
  • HY-126244
    CDK4/6-IN-3

    		CDK Cancer
    CDK4/6-IN-3 is a brain-penetrant CDK4/CDK6 inhibitor with Kis of <0.3 nM and 2.2 nM, respectively. CDK4/6-IN-3 inhibits CDK1 with a Ki of 110 nM. CDK4/6-IN-3 can be used for the treatment of glioblastoma .
    CDK4/6-IN-3
  • HY-176736
    CDK9-IN-40

    		CDK Apoptosis Cancer
    CDK9-IN-40 is a potent and orally active CDK9 inhibitor with an IC50 of 5.5 nM. CDK9-IN-40 shows high selectivity for CDK9 versus CDK1, CDK2, CDK4, and CDK6, respectively. CDK9-IN-40 can arrest cell cycle, induce cell apoptosis and inhibit tumor growth. CDK9-IN-40 exhibits strong anti-cancer activity .
    CDK9-IN-40
  • HY-178756
    CDK2-IN-48

    		CDK Cancer
    CDK2-IN-48 (Compound 109) is a CDK2 inhibitor with IC50 values for CDK2 and CDK1 of respectively < 0.05 and > 1 μM. CDK2-IN-48 can be used for the study of CDK2-dependent cancers .
    CDK2-IN-48
  • HY-175013
    CDK6/9-IN-2

    		CDK STAT Interleukin Related Inflammation/Immunology
    CDK6/9-IN-2 is a highly active dual inhibitor of CDK6 (IC50 = 15 nM) and CDK9 (IC50 = 22 nM). CDK6/9-IN-2 is selective for CDK2, CDK8, and CDK11. CDK6/9-IN-2 inhibits the proliferation of HaCaT cells induced by IFN-γ/TNF-α and suppresses the STAT3 pathway and the expression of inflammatory factors. CDK6/9-IN-2 can alleviate psoriatic dermatitis and is useful in psoriasis research .
    CDK6/9-IN-2
  • HY-153950
    CDK7-IN-22

    		CDK Cancer
    CDK7-IN-22 (compound 101) is an CDK7 inhibitor with antitumor activity. CDK7-IN-22 shows selectivity on CDK7 .
    CDK7-IN-22
  • HY-145408
    CDK7/9-IN-1

    		CDK Cancer
    CDK7/9-IN-1 is a cyclin-dependent kinases 7/9 (CDK7/9) inhibitor. CDK7/9-IN-1 selectively inhibits CDK7 over CDK9. CDK7/9-IN-1 inhibits CDK7 with IC50s of 0.0656 μM and 0.00574 μM without pre-incubation and after 3 hours pre-incubation, respectively. CDK7/9-IN-1 inhibits CDK9 with an IC50 of 2.14 μM after 3 hours pre-incubation. CDK7/9-IN-1 can be used for the research of cancer .
    CDK7/9-IN-1

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