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Targets Recommended: CDK
Results for "

CDK

" in MCE Product Catalog:

231

Inhibitors & Agonists

3

Screening Libraries

7

Peptides

9

Natural
Products

3

Recombinant Proteins

4

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas
  • HY-P2559
    CDK7/9 tide

    CDK Cancer
    CDK7/9 tide is peptide substrate for CDK7 or CDK9.
  • HY-112626
    CDK12-IN-2

    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.
  • HY-13033
    CDK-IN-2

    CDK inhibitor II

    CDK Cancer
    CDK-IN-2 is a potent and specific CDK9 inhibitor with IC50 of <8 nM, extracted from reference 1, example 4.
  • HY-138293
    CDK7-IN-3

    CDK Apoptosis Cancer
    CDK7-IN-3 is a selective CDK7 inhibitor with a KD of 0.059 nM. CDK7-IN-3 shows poor inhibition on CDK2 (Ki=390 nM), CDK9 (Ki=290 nM), CDK12 (Ki=78 nM). CDK7-IN-3 induce apoptosis in tumor cells and has antitumor activity.
  • HY-130001
    CDK9-IN-9

    CDK Cancer
    CDK9-IN-9 (example 2) is a potent and selective CDK9 inhibitor with an IC50 of 1.8 nM. CDK9-IN-9 inhibits CDK2 with an IC50 of 155 nM. CDK9-IN-9 has anti-cancer activity.
  • HY-130852
    CDK9-IN-11

    CDK Ligand for Target Protein for PROTAC Cancer
    CDK9-IN-11 is a potent CDK9 inhibitor. CDK9-IN-11 is the ligand for the PROTAC CDK9 Degrader-1 (HY-103628).
  • HY-130850
    CDK9-IN-10

    CDK Ligand for Target Protein for PROTAC Cancer
    CDK9-IN-10 is a potent CDK9 inhibitor. CDK9-IN-10 is the ligand for the PROTAC CDK9 degrader-2 (HY-112811).
  • HY-126251
    CDK9-IN-7

    CDK Apoptosis Cancer
    CDK9-IN-7 (compound 21e) is a selective, highly potent, and orally active CDK9/cyclin T inhibitor (IC50=11 nM), which exhibits more potent over other CDKs (CDK4/cyclinD=148 nM; CDK6/cyclinD=145 nM). CDK9-IN-7 shows antitumor activity without obvious toxicity. CDK9-IN-7 induces NSCLC cell apoptosis, arrests the cell cycle in the G2 phase, and suppresses the stemness properties of NSCLC.
  • HY-117535
    CDK2-IN-4

    CDK Cancer
    CDK2-IN-4 is a potent and selective CDK2 inhibitor with an IC50 of 44 nM for CDK2/cyclin A, shows 2,000-fold selectivity over CDK1/cyclin B (IC50=86 uM).
  • HY-139328
    CDK12-IN-5

    CDK Cancer
    CDK12-IN-5, a pyrazolotriazine, is a potent CDK12 inhibitor with an IC50 of 23.9 nM at high ATP (2 mM). CDK12-IN-5 has no effect on CDK2/Cyclin E (IC50=173 μM) and CDK9/Cyclin T1 (IC50=127 μM) at high ATP (2 mM) (WO2021116178A1).
  • HY-136711
    CDK7-IN-2 hydrochloride hydrate

    CDK Cancer
    CDK7-IN-2 hydrochloride hydrate (Example 6) is a potent and selective CDK7 inhibitor. CDK7-IN-2 has potent anti-cancer activity.
  • 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.
  • HY-139450
    CDK4/6-IN-6

    CDK Cancer
    CDK4/6-IN-6 (example A94) is a potent CDK4/CDK6 inhibitor with a Ki of 0.6 nM and 13.9 nM for CDK4/Cyclin D1 and CDK6/Cyclin D3, respectively.
  • HY-139329
    CDK12-IN-6

    CDK Cancer
    CDK12-IN-6, a pyrazolotriazine, is a potent CDK12 inhibitor with an IC50 of 1.19 μM at high ATP (2 mM). CDK12-IN-6 has no effect on CDK2/Cyclin E (IC50>20 μM) and CDK9/Cyclin T1 (IC50>20 μM) at high ATP (2 mM) (WO2021116178A1).
  • HY-139327
    CDK12-IN-4

    CDK Cancer
    CDK12-IN-4, a pyrazolotriazine, is a potent CDK12 inhibitor with an IC50 of 0.641 μM at high ATP (2 mM). CDK12-IN-4 has no effect on CDK2/Cyclin E (IC50>20 μM) and CDK9/Cyclin T1 (IC50>20 μM) at high ATP (2 mM) (WO2021116178A1).
  • HY-13231
    CDK9-IN-1

    CDK HIV Infection
    CDK9-IN-1 is a novel, selective CDK9 inhibitor for the treatment of HIV infection, with an IC50 of 39 nM for CDK9/CycT1, extracted from reference, compound 87.
  • HY-103492
    CDK8-IN-1

    CDK Cancer
    CDK8-IN-1 is a potent and selective CDK8 inhibitor with an IC50 of 3 nM.
  • HY-102039
    CDK9-IN-8

    CDK Cancer
    CDK9-IN-8 is a highly effective and selective CDK9 inhibitor with an IC50 of 12 nM.
  • HY-112462
    Cdk1/2 Inhibitor III

    CDK Cancer
    Cdk1/2 Inhibitor III is a selective Cdk1/2 inhibitor, with an IC50 of 2.1 μM for CDK1/cyclin B.
  • HY-112261
    CDK12-IN-3

    CDK Cancer
    CDK12-IN-3 is a potent and selective CDK12 inhibitor with an IC50 of 491 nM in enzymatic assay.
  • 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.
  • HY-139449
    CDK4/6-IN-5

    CDK Cancer
    CDK4/6-IN-5 is a potent CDK4 and CDK6 inhibitor with Kis of 0.2 and 4.4 nM for CDK4/Cyclin D1 and CDK6/Cyclin D3, respectively. (from patent WO2019207463A1 example A93).
  • HY-131063
    CDK6/9-IN-1

    CDK Cancer
    CDK6/9-IN-1 (compound 66) is an orally active active and dual CDK 6 and CDK 9 inhibitor, with IC50 values of 40.5 nM and 39.5 nM for CDK6 anmd CDK9, respectively.
  • HY-117203A
    CDK12-IN-E9

    CDK Cancer
    CDK12-IN-E9 is a potent and selective covalent CDK12 inhibitor and a non-covalent CDK9 inhibitor, while avoiding ABC transporter-mediated efflux. CDK12-IN-E9 has weak binding ability to CDK7/CyclinH complex with an IC50> 1 μM.
  • HY-112280
    CDK4/6/1 Inhibitor

    CDK Cancer
    CDK4/6/1 Inhibitor is a CDK4/6 inhibitor with IC50s of 3 and 1 nM, respectively.
  • HY-111463
    CDK8-IN-3

    CDK Cancer Metabolic Disease Inflammation/Immunology
    CDK8-IN-3 is an inhibitor of CDK8 extracted from patent WO2016041618A1, compound example 1.7.
  • HY-114339
    CDK4/6-IN-2

    CDK Cancer
    CDK4/6-IN-2 is a potent CDK4 and CDK6 inhibitor extracted from patent US20180000819A1, Compound 1, has IC50s of 2.7 and 16 nM for CDK4 and CDK6, respectively.
  • HY-111465
    CDK8-IN-4

    CDK Cancer
    CDK8-IN-4 is an inhibitor of CDK8 extracted from patent WO2014090692A1, compound example 16, with an IC50 of 0.2 nM.
  • HY-78428
    CDK-IN-6

    CDK Cancer
    CDK-IN-6, a class of pyrazolo[1,5-a]pyrimidine compound, is a CDK inhibitor with anticancer activities.
  • HY-123772
    CDK5 inhibitor 20-223

    CDK Cancer
    CDK5 inhibitor 20-223 is a potent CDK2 and CDK5 inhibitor with IC50s of 6.0 and 8.8 nM, respectively. CDK5 inhibitor 20-223 is an effective anti-colorectal cancer (CRC) agent.
  • HY-101257A
    CDK7-IN-1

    CDK Cancer
    CDK7-IN-1, an analog of YKL-5-124, is a cyclin-dependent kinase 7 (cdk7) inhibitor, with an IC50 of less than 100 nM, extracted from patent WO 2016105528 A2, Compound 215.
  • HY-16462
    CDK9-IN-2

    CDK Cancer
    CDK9-IN-2 is a special cyclin-dependent kinase 9 (CDK9) inhibitor, extracted from patent WO/2012131594A1, compound CDKI(8), has an IC50 of 5 nM and 7 nM in H929 multiple myeloma(MM) cell line (72 hours) and A2058 skin cell line (72 hours), respectively.
  • HY-15339
    CVT-313

    CDK2 Inhibitor III

    CDK Cancer
    CVT-313 (Cdk2 Inhibitor III) is a potent, selective, reversible, and ATP-competitive inhibitor of CDK2 with IC50 of 0.5 μM. CVT-313 inhibits CDC5L phosphorylation.
  • HY-12445
    CDKI-73

    LS-007

    CDK Apoptosis Cancer Inflammation/Immunology
    CDKI-73 (LS-007) is an orally active and highly efficacious CDK9 inhibitor, with Ki values of 4 nM, 4 nM and 3 nM for CDK9, CDK1 and CDK2, respectively. CDKI-73 down-regulates the RNAPII phosphorylation. CDKI-73 is also a novel pharmacological inhibitor of Rab11 cargo delivery and innate immune secretion.
  • HY-134622
    GSK-3/CDK5/CDK2-IN-1

    CDK GSK-3 Cancer Neurological Disease
    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.
  • HY-10014
    R547

    CDK GSK-3 Apoptosis Cancer
    R547 is a potent, selective and oral orally bioavailable 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.
  • HY-P1906
    [pThr3]-CDK5 Substrate

    CDK Neurological Disease
    [pThr3]-CDK5 Substrate is an effective Phospho-Thr3CDK5 Substrate. [pThr3]-CDK5 Substrate is derived from the sequence of the histone H1 peptide that docks in the active site of CDK5. [pThr3]-CDK5 Substrate is phosphorylated by CDK5 with a Km value of 6 µM.
  • HY-P1906A
    [pThr3]-CDK5 Substrate TFA

    CDK Neurological Disease
    [pThr3]-CDK5 Substrate TFA is an effective Phospho-Thr3CDK5 Substrate. [pThr3]-CDK5 Substrate is derived from the sequence of the histone H1 peptide that docks in the active site of CDK5. [pThr3]-CDK5 Substrate is phosphorylated by CDK5 with a Km value of 6 µM.
  • HY-103628
    PROTAC CDK9 Degrader-1

    PROTAC and Building Blocks CDK Cancer
    PROTAC CDK9 Degrader-1 is a selective CDK9 degrader.
  • HY-130709
    PROTAC CDK2/9 Degrader-1

    PROTAC and Building Blocks CDK Cancer
    PROTAC CDK2/9 Degrader-1 (Compound F3) is a potent dual degrader for CDK2 (DC50=62 nM) and CDK9 (DC50=33 nM). PROTAC CDK2/9 Degrader-1 suppresses prostate cancer PC-3 cell proliferation (IC50=0.12 µM) by effectively blocking the cell cycle in S and G2/M phases. PROTAC CDK2/9 Degrader-1 is a PROTAC by tethering CDK inhibitor with CRBN ligand.
  • HY-112811
    PROTAC CDK9 degrader-2

    PROTAC and Building Blocks CDK Cancer
    PROTAC CDK9 degrader-2 (compounds 11c) is a potent and selective CDK9 degrader based on PROTAC, with an IC50 of 17 μM in MCF-7 cell lines. Natural product Wogonin binds ubiquitin E3 ligase cereblon (CRBN) via a linker to form PROTAC.
  • HY-130296
    Palbociclib-propargyl

    PROTAC CDK6 ligand 1

    Ligand for Target Protein for PROTAC Cancer
    Palbociclib-propargyl is a ligand for target protein CDK6 for PROTAC, and binds to CRBN ligand via a PEG linker to make a PROTAC CP-10. CP-10 shows a DC50 of 2.1 nM for CDK6.
  • HY-108359
    Alsterpaullone

    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.
  • HY-130665
    TL12-186

    PROTAC and Building Blocks CDK Cancer
    TL12-186 is a CRBN-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).
  • HY-11009
    CGP60474

    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.
  • HY-13914
    Roniciclib

    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.
  • HY-138946
    XY028-140

    CDK PROTAC and Building Blocks Cancer
    XY028-140 is a selective CDK4/CDK6 degrader. XY028-140 inhibits both CDK4/6 expression and CDK4/6 activity in cancer cells.
  • HY-112272A
    Lerociclib dihydrochloride

    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.
  • HY-50943
    AT7519 Hydrochloride

    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.
  • HY-15275
    BMS-265246

    CDK Cancer
    BMS-265246 is a potent and selective CDK1/2 inhibitor for CDK1/cyclin B and CDK2/cyclin E with IC50 of 6 nM and 9 nM, respectively.
  • HY-18299A
    Purvalanol A

    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.
  • HY-50940
    AT7519

    AT7519M

    CDK Apoptosis Cancer
    AT7519 (AT7519M) as 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.
  • HY-12529
    Ro-3306

    CDK Apoptosis Cancer
    Ro-3306 is a potent and selective inhibitor of CDK1, with Kis of 20 nM, 35 nM and 340 nM for CDK1, CDK1/cyclin B1 and CDK2/cyclin E, respectively.
  • HY-50940A
    AT7519 TFA

    AT7519M TFA

    CDK Cancer
    AT7519 (AT7519M) TFA as 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.
  • HY-10006
    Flavopiridol Hydrochloride

    Alvocidib Hydrochloride; L86-8275 Hydrochloride; HMR-1275 Hydrochloride

    CDK Autophagy HIV Cancer
    Flavopiridol Hydrochloride (Alvocidib Hydrochloride) is a broad inhibitor of CDK, competing with ATP to inhibit CDKs including CDK1, CDK2, CDK4 with IC50s of 30, 170, 100 nM, respectively.
  • HY-111356
    IIIM-290

    CDK Cancer
    IIIM-290 is a potent and oral CDK inhibitor with IC50s of 90 and 94 nM for CDK2/A and CDK9/T1.
  • HY-101467
    Trilaciclib

    G1T28

    CDK Cancer
    Trilaciclib is a CDK4/6 inhibitor with IC50s of 1 nM and 4 nM for CDK4 and CDK6, respectively.
  • HY-10492
    Dinaciclib

    SCH 727965

    CDK Apoptosis Cancer
    Dinaciclib (SCH 727965) is a potent inhibitor of CDK, with IC50s of 1 nM, 1 nM, 3 nM, and 4 nM for CDK2, CDK5, CDK1, and CDK9, respectively.
  • HY-15569
    NU6102

    CDK Cancer
    NU6102 is a potent CDK1 and CDK2 inhibitor with IC50s of 9.5 nM and 5.4 nM for CDK1/cyclinB and CDK2/cyclinA3, respectively. NU6102 shows selectivity for CDK1/CDK2 over CDK4 (IC50 of 1.6 μM), DYRK1A (IC50 of 0.9 μM), PDK1 (IC50 of 0.8 μM) and ROCKII (IC50 of 0.6 μM).
  • HY-111932
    Indirubin-5-sulfonate

    CDK GSK-3 Cancer
    Indirubin-5-sulfonate is a cyclin-dependent kinase (CDK) inhibitor, with IC50 values of 55 nM, 35 nM, 150 nM, 300 nM and 65 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E, CDK4/cyclin D1, and CDK5/p35, respectively. Indirubin-5-sulfonate also shows inhibitory activity against GSK-3β.
  • HY-112272
    Lerociclib

    G1T38

    CDK Cancer
    Lerociclib (G1T38) is a potent and selective inhibitor of CDK4/6, with IC50s of 1 nM, 2 nM for CDK4/CyclinD1 and CDK6/CyclinD3, respectively.
  • HY-103380
    NSC 625987

    CDK Cancer
    NSC 625987 is a specific and high-affinity CDK4 inhibitor with an IC50 of 0.2 μM for CDK4:cyclin D1. NSC 625987 shows >500-fold selectivity for CDK4 over CDK2.
  • HY-16297A
    Abemaciclib

    LY2835219

    CDK Cancer
    Abemaciclib (LY2835219) is a selective CDK4/6 inhibitor with IC50 values of 2 nM and 10 nM for CDK4 and CDK6, respectively.
  • HY-12843
    Bohemine

    CDK ERK Cancer
    Bohemine is a purine analogue and is a synthetic and selective CDK inhibitor with IC50s of 4.6 μM, 83 μM, and 2.7 μM for Cdk2/cyclin E, Cdk2/cyclin A, and Cdk9/cyclin T1, respectively. Bohemine also inhibits ERK2 with an IC50 of 52 μM and has less inhibitory effect on CDK1, CDK4 and CDK6. Bohemine has a broad spectrum anti-cancer activities.
  • HY-15504A
    RGB-286638 free base

    CDK GSK-3 MEK JAK Cancer
    RGB-286638 is a CDK inhibitor that inhibits the kinase activity of cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5 with IC50s of 1, 2, 3, 4, 5 and 5 nM, respectively; also inhibits GSK-3β, TAK1, Jak2 and MEK1, with IC50s of 3, 5, 50, and 54 nM.
  • HY-15504
    RGB-286638

    CDK GSK-3 MEK JAK Cancer
    RGB-286638 is a CDK inhibitor that inhibits the kinase activity of cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5 with IC50s of 1, 2, 3, 4, 5 and 5 nM, respectively; also inhibits GSK-3β, TAK1, Jak2 and MEK1, with IC50s of 3, 5, 50, and 54 nM.
  • HY-10005
    Flavopiridol

    HMR-1275; Alvocidib; L86-8275

    CDK Autophagy HIV Apoptosis Cancer
    Flavopiridol (Alvocidib) is a broad spectrum and competitive inhibitor of CDKs, inhibiting CDK1, CDK2, CDK4 with IC50s of 30, 170, 100 nM, respectively.
  • HY-111361
    FN-1501

    CDK FLT3 Cancer
    FN-1501 is a potent inhibitor of FLT3 and CDK, with IC50s of 2.47, 0.85, 1.96, and 0.28 nM for CDK2/cyclin A, CDK4/cyclin D1, CDK6/cyclin D1 and FLT3, respectively. FN-1501 has anticancer activity.
  • HY-12214A
    NVP-2

    CDK Apoptosis Cancer
    NVP-2 is a potent and selective ATP-competitive cyclin dependent kinase 9 (CDK9) probe, inhibits CDK9/CycT activity with an IC50 of 0.514 nM. NVP-2 displays inhibitory effcts on CDK1/CycB, CDK2/CycA and CDK16/CycY kinases with IC50 values of 0.584 µM, 0.706 µM, and 0.605 µM, respectively. NVP-2 induces cell apoptosis.
  • HY-101467A
    Trilaciclib hydrochloride

    G1T28 hydrochloride

    CDK Cancer
    Trilaciclib hydrochloride (G1T28 hydrochloride) is a CDK4/6 inhibitor with IC50s of 1 nM and 4 nM for CDK4 and CDK6, respectively.
  • HY-15241
    NVP-LCQ195

    LCQ-195; AT9311

    CDK Cancer
    NVP-LCQ195 (AT9311; LCQ195) is a small molecule heterocyclic inhibitor of CDK1, CDK2, CDK3 and CDK5 with IC50 of 1-42 nM.
  • HY-18340
    (R)​-​CR8

    CR8, (R)-Isomer

    CDK Apoptosis Cancer Neurological Disease
    (R)​-​CR8 (CR8), a second-generation analog of Roscovitine, is a potent CDK1/2/5/7/9 inhibitor. (R)​-​CR8 inhibits CDK1/cyclin B (IC50=0.09 μM), CDK2/cyclin A (0.072 μM), CDK2/cyclin E (0.041 μM), CDK5/p25 (0.11 μM), CDK7/cyclin H (1.1 μM), CDK9/cyclin T (0.18 μM) and CK1δ/ε (0.4 μM). (R)​-​CR8 induces apoptosis and has neuroprotective effect. (R)-CR8 acts as a molecular glue degrader that depletes cyclin K.
  • HY-18340A
    (R)-CR8 trihydrochloride

    CR8, (R)-Isomer trihydrochloride

    CDK Apoptosis Cancer Neurological Disease
    (R)-CR8 (CR8) trihydrochloride, a second-generation analog of Roscovitine, is a potent CDK1/2/5/7/9 inhibitor. (R)-CR8 trihydrochloride inhibits CDK1/cyclin B (IC50=0.09 μM), CDK2/cyclin A (0.072 μM), CDK2/cyclin E (0.041 μM), CDK5/p25 (0.11 μM), CDK7/cyclin H (1.1 μM), CDK9/cyclin T (0.18 μM) and CK1δ/ε (0.4 μM). (R)-CR8 trihydrochloride induces apoptosis and has neuroprotective effect. (R)-CR8 trihydrochloride acts as a molecular glue degrader that depletes cyclin K.
  • HY-10424
    Milciclib

    PHA-848125

    CDK Autophagy Cancer
    Milciclib (PHA-848125) is a potent, ATP-competitive and dual inhibitor of CDK and Tropomyosin receptor kinase (TRK), with IC50s of 45, 150, 160, 363, 398 nM and 53 nM for cyclin A/CDK2, cyclin H/CDK7, cyclin D1/CDK4, cyclin E/CDK2, cyclin B/CDK1 and TRKA, respectively.
  • HY-16559A
    Riviciclib

    P276-00 free base

    CDK Cancer
    Riviciclib (P276-00 free base) is a potent cyclin-dependent kinase (CDK) inhibitor, which inhibits CDK9-cyclinT1, CDK4-cyclin D1, and CDK1-cyclinB with IC50s of 20 nM, 63 nM, and 79 nM, respectively. Riviciclib shows antitumor activity on cisplatin-resistant cells.
  • HY-111388
    SEL120-34A

    CDK Cancer
    SEL120-34A is a potent, selective, orally available, ATP-competitive CDK8 inhibitor, with IC50s of 4.4 nM and 10.4 nM for CDK8/CycC and CDK19/CycC, respectively, with antitumor activity.
  • HY-111388B
    SEL120-34A HCl

    CDK Cancer
    SEL120-34A HCl is a potent, selective, orally available, ATP-competitive CDK8 inhibitor, with IC50s of 4.4 nM and 10.4 nM for CDK8/CycC and CDK19/CycC, respectively, with antitumor activity.
  • HY-16297
    Abemaciclib methanesulfonate

    LY2835219 methanesulfonate

    CDK Cancer
    Abemaciclib methanesulfonate (LY2835219 methanesulfonate) is a selective CDK4/6 inhibitor with IC50s of 2 nM and 10 nM for CDK4 and CDK6, respectively.
  • HY-11001
    PHA-793887

    CDK Apoptosis Cancer
    PHA-793887 is a potent, ATP-competitive CDK inhibitor, can inhibit Cdk2, Cdk1, Cdk4, and Cdk9 with IC50s of 8 nM, 60 nM, 62 nM and 138 nM, respectively, and also inhibits glycogen synthase kinase 3β with an IC50 of 79 nM.
  • HY-16559
    Riviciclib hydrochloride

    P276-00

    CDK Apoptosis Cancer
    Riviciclib hydrochloride (P276-00) is a potent cyclin-dependent kinase (CDK) inhibitor, which inhibits CDK9-cyclinT1, CDK4-cyclin D1, and CDK1-cyclinB with IC50s of 20 nM, 63 nM, and 79 nM, respectively. Riviciclib hydrochloride (P276-00) shows antitumor activity on cisplatin-resistant cells.
  • HY-112468
    PNU112455A hydrochloride

    CDK Cancer
    PNU112455A hydrochloride is an ATP-competitive CDK2 and CDK5 inhibitor. PNU112455A hydrochloride binds to the ATP site of CDK2 and CDK5 with Kms of 3.6 and 3.2 μM, respectively.
  • HY-10012
    AZD-5438

    CDK Cancer
    AZD-5438 is a potent CDK1, CDK2, and CDK9 inhibitor, with IC50s of 16 nM, 6 nM, and 20 nM in cell-free assays, respectively. AZD-5438 shows less inhibition activity against GSK3β, CDK5 and CDK6 .
  • HY-12302
    Kenpaullone

    9-Bromopaullone; NSC-664704

    CDK GSK-3 Cancer
    Kenpaullone is a potent inhibitor of CDK1/cyclin B and GSK-3β, with IC50s of 0.4 μM and 23 nM, and also inhibits CDK2/cyclin A, CDK2/cyclin E, and CDK5/p25 with IC50s of 0.68 μM, 7.5 μM, 0.85 μM, respectively. Kenpaullone, a small molecule inhibitor of KLF4, reduces self-renewal of breast cancer stem cells and cell motility in vitro.
  • HY-18299
    Purvalanol B

    NG 95

    CDK Parasite Cancer Infection
    Purvalanol B (NG 95) is a potent, selective, reversible and ATP-competitive inhibitor CDK, with IC50s of 6 nM, 6 nM, 9 nM, 6 nM for cdc2-cyclin B, CDK2-cyclin A, CDK2-cyclin E and CDK5-p35, respectively. Purvalanol B shows selectivity for CDK over a range of other protein kinases (IC50>1000 nM). Purvalanol B inhibits the growth a chloroquine-resistant strain of P. falciparum.
  • HY-101212
    Fadraciclib

    CYC065

    CDK Cancer
    Fadraciclib (CYC065) is a second-generation, orally available ATP-competitive inhibitor of CDK2/CDK9 kinases with IC50s of 5 and 26 nM, respectively.
  • HY-101257B
    YKL-5-124 TFA

    CDK Cancer
    YKL-5-124 TFA is a potent, selective, irreversible and covalent CDK7 inhibitor with IC50s of 53.5 nM and 9.7 nM for CDK7 and CDK7/Mat1/CycH, respectively. YKL-5-124 TFA is >100-fold greater selective for CDK7 than CDK9 and CDK2, and inactive against CDK12 and CDK13. YKL-5-124 TFA induces a strong cell-cycle arrest, inhibits E2F-driven gene expression, and exhibits little effect on RNA polymerase II phosphorylation status.
  • HY-101257
    YKL-5-124

    CDK Cancer
    YKL-5-124 is a potent, selective, irreversible and covalent CDK7 inhibitor with IC50s of 53.5 nM and 9.7 nM for CDK7 and CDK7/Mat1/CycH, respectively. YKL-5-124 is >100-fold greater selective for CDK7 than CDK9 and CDK2, and inactive against CDK12 and CDK13. YKL-5-124 induces a strong cell-cycle arrest, inhibits E2F-driven gene expression, and exhibits little effect on RNA polymerase II phosphorylation status.
  • HY-100429
    CAN508

    CDK Cancer
    CAN508 is a potent, ATP-competitive CDK9/cyclin T1 inhibitor with an IC50 of 0.35 μM. CAN508 exhibits a 38-fold selectivity for CDK9/cyclin T over other CDK/cyclin complexes. Antitumor activity.
  • HY-130250
    SR-4835

    CDK Apoptosis Cancer
    SR-4835 is a potent, highly selective and ATP competitive dual inhibitor of CDK12/CDK13 (CDK12: IC50=99 nM, Kd=98 nM; CDK13: Kd=4.9 nM). SR-4835 acts in synergy with DNA-damaging chemotherapy and PARP inhibitors and provokes triple-negative breast cancer (TNBC) cell death.
  • HY-103647
    K00546

    CDK VEGFR GSK-3 Cancer
    K00546 is a potent CDK1 and CDK2 inhibitor with IC50s of 0.6 nM and 0.5 nM for CDK1/cyclin B and CDK2/cyclin A, respectively. K00546 is also a potent CDC2-like kinase 1 (CLK1) and CLK3 inhibitor with IC50s of 8.9 nM and 29.2 nM, respectively.
  • HY-137478A
    KB-0742 dihydrochloride

    CDK Cancer
    KB-0742 dihydrochloride is a potent, selective and orally active CDK9 inhibitor with an IC50 of 6 nM for CDK9/cyclin T1. KB-0742 dihydrochloride is selective for CDK9/cyclin T1 with >50-fold selectivity over other CDK kinases. KB-0742 dihydrochloride has potent anti-tumor activity.
  • HY-136250
    BSJ-03-204

    PROTAC and Building Blocks CDK Cancer
    BSJ-03-204 is a potent and selective Palbociclib-based CDK4/6 dual degrader (PROTAC), with IC50s of 26.9 nM and 10.4 nM for CDK4/D1 and CDK6/D1, respectively. BSJ-03-204 does not induce IKZF1/3 degradation and has anti-cancer activity.
  • HY-130981
    FN-1501-propionic acid

    CDK Ligand for Target Protein for PROTAC Cancer
    FN-1501-propionic acid is a CDK2/9 ligand for PROTAC. FN-1501-propionic acid and a CRBN ligand have been used to design PROTAC CDK2/9 degrader (HY-130709).
  • HY-10329
    JNJ-7706621

    Aurora Kinase CDK Apoptosis Cancer
    JNJ-7706621 is a potent aurora kinase inhibitor, and also inhibits CDK1 and CDK2, with IC50s of 9 nM, 3 nM, 11 nM, and 15 nM for CDK1, CDK2, aurora-A and aurora-B, respectively.
  • HY-136252
    BSJ-04-132

    PROTAC and Building Blocks CDK Cancer
    BSJ-04-132 is a potent and selective Ribociclib-based CDK4 degrader (PROTAC), with IC50s of 50.6 nM and 30 nM for CDK4/D1 and CDK6/D1, respectively. BSJ-04-132 does not induce CDK6 and IKZF1/3 degradation. BSJ-04-132 has anti-cancer activity.
  • HY-12871C
    Atuveciclib S-Enantiomer

    BAY-1143572 S-Enantiomer

    CDK Cancer
    Atuveciclib S-Enantiomer (BAY-1143572 S-Enantiomer) is a potent and selective CDK9 inhibitor, which inhibits CDK9/CycT1 with an IC50 of 16 nM.
  • HY-18629
    SU9516

    CDK Autophagy Apoptosis Cancer
    SU9516 is a potent CDK2 inhibitor, with an IC50 of 22 nM, and also shows inhibitory effects on CDK1 and CDK4, with IC50s of 40, 200 nM, respectively.
  • HY-114177
    PF-06873600

    CDK Cancer
    PF-06873600 is a selective and orally bioavailable inhibitor of cyclin-dependent kinase (CDK), with Ki values of 0.09 nM, 0.13 nM and 0.16 nM for CDK2, CDK4 and CDK6, respectively. PF-06873600 has potential antineoplastic activity.
  • HY-112363
    Aloisine A

    RP107

    CDK GSK-3 ERK JNK CFTR Cancer Inflammation/Immunology
    Aloisine A (RP107) is a a potent cyclin-dependent kinase (CDK) inhibitor with IC50s of 0.15 μM, 0.12 μM, 0.4 μM, 0.16 μM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E, CDK5/p35, respectively. Aloisine A ininhibits GSK-3α (IC50=0.5 µM) and GSK-3β (IC50=1.5 µM). Aloisine A stimulates wild-type CFTR and mutated CFTR, with submicromolar affinity by a cAMP-independent mechanism. Aloisine A has the potential for CFTR-related diseases, including cystic fibrosis research.
  • HY-111388A
    SEL120-34A monohydrochloride

    CDK Cancer
    SEL120-34A monohydrochloride is an ATP-competitive and selective CDK8 inhibitor, inhibits kinase activities of CDK8/CycC and CDK19/CycC complexes with IC50s of 4.4 nM and 10.4 nM, respectively, with a Kd of 3 nM for CDK8. SEL120-34A monohydrochloride weakly inhibits CDK9 (calculated IC50=1070 nM), but shows no obvious activity against CDK1, 2, 4, 6, 5, 7. SEL120-34A monohydrochloride inhibits phosphorylation of STAT1 S727 and STAT5 S726. Has anti-tumor activity.
  • HY-W011428
    Olomoucine

    CDK Others
    Olomoucine is an ATP competitive inhibitor of CDKs. Olomoucine is a purine (HY-34431) derivative and inhibits CDC2/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E (both IC50=7 µM), CDK/p35 kinase (IC50=3 µM) and ERK1/p44 MAP kinase (IC50=25 µM).
  • HY-122586
    BRD6989

    CDK Interleukin Related Inflammation/Immunology
    BRD6989, an analog of the natural product cortistatin A (dCA), inhibits CDK8 and upregulates IL-10. BRD6989 selectively binds a complex of CDK8 with an IC50 of ~200 nM. BRD6989 inhibits the kinase activity of recombinant CDK8 or CDK19 complexes.
  • HY-13266A
    BS-181 hydrochloride

    CDK Cancer
    BS-181 hydrochloride is a highly selective CDK7 inhibitor with IC50 of 21 nM, and > 40-fold selective for CDK7 than CDK1, 2, 4, 5, 6, or 9.
  • HY-W010128
    6-(Dimethylamino)purine

    6-Dimethylaminopurine

    CDK Others
    6-(Dimethylamino)purine is a dual inhibitor of protein kinase and CDK.
  • HY-12293
    LY2857785

    CDK Apoptosis Cancer
    LY2857785 is a type I reversible and competitive ATP kinase inhibitor against CDK9 (IC50 11 nM) and other transcription kinases CDK8 (IC50 16 nM), and CDK7 (IC50 246 nM).
  • HY-108907
    SR-1277

    Casein Kinase Cancer
    SR-1277 is a potent, selective and ATP competitive CK1δ/ε inhibitor, with IC50s of 49 nM and 260 nM, respectively. SR-1277 also inhibits FLT3, CDK4/cyclin D1, CDK6/cyclin D3 and CDK9/cyclin K, with IC50s of 305 nM, 1340 nM, 311 nM and 109 nM, respectively. SR-1277 can be used for the research of cancer.
  • HY-30237
    Seliciclib

    Roscovitine; CYC202; R-roscovitine

    CDK Cancer
    Seliciclib (Roscovitine) is an orally bioavailable and selective CDKs inhibitor with IC50s of 0.2 μM, 0.65 μM, and 0.7 μM for CDK5, Cdc2, and CDK2, respectively.
  • HY-111518
    JH-XI-10-02

    PROTAC and Building Blocks CDK Cancer
    JH-XI-10-02 is a highly potent and selective PROTAC CDK8 degrader, with an IC50 of 159 nM. JH-XI-10-02 causes proteasomal degradation, does not affect CDK8 mRNA levels. JH-XI-10-02 shows no effect on CDK19.
  • HY-126534A
    LSN3106729 hydrochloride

    CDK Ligand for Target Protein for PROTAC Cancer
    LSN3106729 hydrochloride, the metabolite of Abemaciclib (HY-16297A), is a CDK inhibitor with antitumor activity. LSN3106729 hydrochloride and a CRBN ligand have been used to design PROTAC CDK4/6 degrader.
  • HY-126534
    LSN3106729

    CDK Ligand for Target Protein for PROTAC Cancer
    LSN3106729, the metabolite of Abemaciclib (HY-16297A), is a CDK inhibitor with antitumor activity. LSN3106729 and a CRBN ligand have been used to design PROTAC CDK4/6 degrader.
  • HY-101611
    MSC2530818

    CDK Cancer
    MSC2530818 is a potent, selective and orally available CDK8 inhibitor with an IC50 of 2.6 nM for CDK8.
  • HY-10580
    GSK 3 Inhibitor IX

    6-Bromoindirubin-3'-oxime; BIO; MLS 2052

    GSK-3 CDK Apoptosis Cancer
    GSK 3 Inhibitor IX (6-Bromoindirubin-3'-oxime; BIO) is a potent, selective, reversible and ATP-competitive inhibitor of GSK-3α/β and CDK1-cyclinB complex with IC50s of 5 nM/320 nM/80 nM for (GSK-3α/β)/CDK1/CDK5, respectively.
  • HY-12871
    Atuveciclib Racemate

    BAY-1143572 Racemate

    CDK Cancer
    Atuveciclib Racemate (BAY-1143572 Racemate) is the racemate mixture of Atuveciclib. Atuveciclib is a potent and highly selective, oral P-TEFb/CDK9 inhibitor which supresses CDK9/CycT1 with an IC50 of 13 nM.
  • HY-80013A
    THZ1 Hydrochloride

    CDK Cancer
    THZ1 Hydrochloride is a selective and potent covalent CDK7 inhibitor with an IC50 of 3.2 nM. THZ1 Hydrochloride also inhibits the closely related kinases CDK12 and CDK13 and downregulates MYC expression.
  • HY-80013
    THZ1

    CDK Cancer
    THZ1 is a selective and potent covalent CDK7 inhibitor with an IC50 of 3.2 nM. THZ1 also inhibits the closely related kinases CDK12 and CDK13 and downregulates MYC expression.
  • HY-111930
    5-Iodo-indirubin-3'-monoxime

    GSK-3 CDK Cancer
    5-Iodo-indirubin-3'-monoxime is a potent GSK-3β, CDK5/P25 and CDK1/cyclin B inhibitor, competing with ATP for binding to the catalytic site of the kinase, with IC50s of 9, 20 and 25 nM, respectively.
  • HY-111556
    BSJ-03-123

    PROTAC and Building Blocks CDK Cancer
    BSJ-03-123 is a potent and novel CDK6-selective small-molecule degrader (PROTAC).
  • HY-103712A
    Samuraciclib hydrochloride

    CT7001 hydrochloride; ICEC0942 hydrochloride

    CDK Apoptosis Cancer
    Samuraciclib hydrochloride (CT7001 hydrochloride) is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. Samuraciclib hydrochloride displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC50 of 578 nM), CDK5 and CDK9, respectively. Samuraciclib hydrochloride inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 µM. Samuraciclib hydrochloride has anti-tumor effects.
  • HY-103712B
    Samuraciclib trihydrochloride

    CT7001 trihydrochloride; ICEC0942 trihydrochloride

    CDK Apoptosis Cancer
    Samuraciclib (CT7001) trihydrochloride is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. Samuraciclib trihydrochloride displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC50 of 578 nM), CDK5 and CDK9, respectively. Samuraciclib trihydrochloride inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 µM. Samuraciclib trihydrochloride has anti-tumor effects.
  • HY-15777A
    Ribociclib hydrochloride

    LEE011 hydrochloride

    CDK Cancer
    Ribociclib hydrochloride (LEE011 hydrochloride) is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex.
  • HY-127104
    FMF-04-159-2

    CDK Cancer
    FMF-04-159-2 is a covalent CDK14 inhibitor. FMF-04-159-2 inhibits CDK14 and CDK2 with IC50s of 39.6 nM and 256 nM in NanoBRET assay, respectively.
  • HY-12871B
    Atuveciclib

    BAY-1143572

    CDK Cancer
    Atuveciclib (BAY-1143572) is a potent and highly selective, oral PTEFb/CDK9 inhibitor. Atuveciclib (BAY-1143572) inhibits CDK9/CycT1 with an IC50 of 13 nM.
  • HY-15777
    Ribociclib

    LEE011

    CDK Cancer
    Ribociclib (LEE01) is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex.
  • HY-15777C
    Ribociclib succinate hydrate

    LEE011 succinate hydrate

    CDK Cancer
    Ribociclib succinate hydrate (LEE011 succinate hydrate) is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex.
  • HY-15777B
    Ribociclib succinate

    LEE011 succinate

    CDK Cancer
    Ribociclib succinate (LEE011 succinate) is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex.
  • HY-15491
    AG-024322

    COX Apoptosis Cancer
    AG-024322 is a potent ATP-competitive pan-CDK inhibitor against cell cycle kinases CDK1, CDK2, and CDK4 with Ki values in the 1-3 nM range. AG-024322 displays broad-spectrum anti-tumor activity and clear target modulation in vivo. AG-024322 induces cell apoptosis.
  • HY-116035
    Nimbolide

    NF-κB CDK Apoptosis Cancer
    Nimbolide is a triterpene derived from the leaves and flowers of neem (Azadirachta indica L). Nimbolide induces apoptosis through inactivation of NF-κB. Nimbolide inhibits CDK4/CDK6 kinase activity. Nimbolide suppresses the NF-κB, Wnt, PI3K-Akt, MAPK and JAK-STAT signaling pathways.
  • HY-19316
    NU2058

    O6-(Cyclohexylmethyl)guanine

    CDK Cancer
    NU2058 (O6-(Cyclohexylmethyl)guanine) is a potent, competitive and guanine-based CDK inhibitor with IC50s of 17 μM and 26 μM for CDK2 and CDK1. NU2058 has anti-cancer activity.
  • HY-13461
    PHA-767491

    CAY10572

    CDK Cancer
    PHA-767491 is a dual Cdc7/Cdk9 inhibitor, with IC50s of 10 nM and 34 nM, respectively.
  • HY-129180
    XY028-133

    PROTAC and Building Blocks CDK Cancer
    XY028-133 (example 14) is a PROTAC-based CDK4/6 degrader with anti-tumor activity.
  • HY-13461A
    PHA-767491 hydrochloride

    CAY-10572 hydrochloride

    CDK Apoptosis Cancer
    PHA-767491 hydrochloride is a dual Cdc7/Cdk9 inhibitor, with IC50s of 10 nM and 34 nM, respectively.
  • HY-103618
    THZ531

    CDK Cancer
    THZ531 is a selective and covalent inhibitor of both CDK12 and CDK13 with IC50s of 158 nM and 69 nM, respectively.
  • HY-107419
    NU6140

    CDK Aurora Kinase Cancer
    NU6140 is a selective CDK2-cyclin A inhibitor (IC50, 0.41 μM), exhibits 10- to 36-fold selectivity over other CDKs. NU6140 also potently inhibits Aurora A and Aurora B, with IC50s of 67 and 35 nM, respectively. Enhances the apoptotic effect, with anti-cancer activity.
  • HY-129336
    Abemaciclib metabolite M20

    LSN3106726

    CDK Cancer
    Abemaciclib metabolite M20 (LSN3106726), the active metabolite of Abemaciclib, is a selective CDK4/6 inhibitor for the treatment of cancer.
  • HY-10008
    SNS-032

    BMS-387032

    CDK Apoptosis Cancer
    SNS-032 (BMS-387032) is a potent and selective inhibitor of CDK2, CDK7, and CDK9 with IC50s of 38 nM, 62 nM and 4 nM, respectively. SNS-032 has antitumor effect.
  • HY-125835
    CP-10

    PROTAC and Building Blocks CDK Cancer
    CP-10 is a PROTAC with highly selective, specific, and remarkable CDK6 degradation (DC50=2.1 nM). It inhibits proliferation of several haematopoietic cancer cells with impressive potency including multiple myeloma, and can still degrades mutated and overexpressed CDK6.
  • HY-19807
    Indirubin-3'-monoxime

    Indirubin-3'-oxime

    GSK-3 CDK Lipoxygenase Cancer
    Indirubin-3'-monoxime is a potent GSK-3β inhibitor, and weakly inhibits 5-Lipoxygenase, with IC50s of 22 nM and 7.8-10 µM, respectively; Indirubin-3'-monoxime also shows inhibitory activities against CDK5/p25 and CDK1/cyclin B, with IC50s of 100 and 180 nM.
  • HY-114338
    Dalpiciclib

    SHR-6390

    CDK Cancer
    Dalpiciclib (SHR-6390) is a highly selective, orally bioavailable CDK4/6 inhibitor with comparable potencies against CDK4 (IC50=12.4 nM) and CDK6 (IC50=9.9 nM). Dalpiciclib exerts potent antitumor activity in esophageal squamous cell carcinoma by inhibiting phosphorylated tumor-suppressor retinoblastoma protein (Rb) and inducing G1 cell cycle arrest.
  • HY-141685
    3-Methylthienyl-carbonyl-JNJ-7706621

    CDK GSK-3 VEGFR FGFR Cancer
    3-Methylthienyl-carbonyl-JNJ-7706621 is a potent and selective inhibitor of cyclin-dependent kinase (CDK), with IC50s of 6.4 nM and 2 nM for CDK1/cyclin B and CDK2/cyclin A, respectively. 3-Methylthienyl-carbonyl-JNJ-7706621 also shows potent inhibition of GSK-3 (IC50=0.041 μM) and modest potency against CDK4, VEGF-R2, and FGF-R2 (IC50=0.11, 0.13, 0.22 μM, respectively). 3-Methylthienyl-carbonyl-JNJ-7706621 can be used for the research of cancer.
  • HY-110368
    BS-181 dihydrochloride

    CDK Cancer
    BS-181 dihydrochloride is a potent and selective CDK7 inhibitor (IC50=21 nM) than Seliciclib (HY-30237). BS-181 is also against CDK2, CDK5 and CDK9 with IC50 values of 880 nM, 3000 nM and 4200 nM, respectively (fails to block CDK1, 4 and 6). BS-181 dihydrochloride inhibits a panel of cancer cells growth (IC50=11.5 μM-37.3 μM) and induces cell apoptosis. BS-181 dihydrochloride has the potential for the research of cancer therapy.
  • HY-13266
    BS-181

    CDK Apoptosis Cancer
    BS-181 is a potent and selective CDK7 inhibitor (IC50=21 nM) than Seliciclib (HY-30237). BS-181 is also against CDK2, CDK5 and CDK9 with IC50 values of 880, 3000 and 4200 nM, respectively (fails to block CDK1, 4 and 6). BS-181 inhibits a panel of cancer cells growth (IC50=11.5 μM-37.3 μM) and induces cell apoptosis. BS-181 has the potential for the research of cancer therapy.
  • HY-119940
    MC180295

    (rel)-MC180295

    CDK Cancer
    MC180295 ((rel)-MC180295) is a potent and selective CDK9-Cyclin T1 inhibitor, with an IC50 of 5 nM, at least 22-fold more selective for CDK9 over other CDKs. MC180295 also inhibits GSK-3α and GSK-3β. MC180295 ((rel)-MC180295) has potent anti-tumor effect.
  • HY-15777S
    Ribociclib D6

    LEE011 D6

    CDK Cancer
    Ribociclib D6 (LEE011 D6) is a deuterium labeled Ribociclib. Ribociclib is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex.
  • HY-15777AS
    Ribociclib D6 hydrochloride

    LEE011 D6 hydrochloride

    CDK Cancer
    Ribociclib D6 (LEE011 D6) hydrochloride is a deuterium labeled Ribociclib. Ribociclib is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex.
  • HY-15004
    AUZ 454

    K03861

    CDK Cancer
    AUZ 454 (K03861) is a type II CDK2 inhibitor with Kd of 8.2 nM. AUZ 454 (K03861) inhibits CDK2 activity by competing with binding of activating cyclins.
  • HY-15889A
    AMG 925 HCl

    FLT3 CDK Cancer
    AMG 925 HCl is a potent, selective, and orally available FLT3/CDK4 dual inhibitor with IC50s of 2±1 nM and 3±1 nM, respectively.
  • HY-15889
    AMG 925

    FLT3 CDK Cancer
    AMG 925 is a potent, selective, and orally available FLT3/CDK4 dual inhibitor with IC50s of 2±1 nM and 3±1 nM, respectively.
  • HY-126675A
    AS2863619

    CDK STAT Inflammation/Immunology
    AS2863619 enables conversion of antigen-specific effector/memory T cells into Foxp3 + regulatory T (Treg) cells for the treatment of various immunological diseases. AS2863619 is a potent, orally active cyclin-dependent kinase 8 (CDK8) and CDK19 inhibitor with IC50s of 0.61 nM and 4.28 nM, respectively. STAT5 activation enhanced by AS2863619 inhibition of CDK8/19, which consequently activates the Foxp3 gene.
  • HY-124760
    hSMG-1 inhibitor 11e

    mTOR PI3K CDK Cancer
    hSMG-1 inhibitor 11e is a potent and selective hSMG-1 kinase inhibitor with an IC50 of <0.05 nM. hSMG-1 inhibitor 11e shows >900-fold selectivity over mTOR (IC50 of 45 nM), PI3Kα/γ (IC50s of 61 nM and 92 nM) and CDK1/CDK2 (IC50s of 32 μM and 7.1 μM).
  • HY-15681
    Senexin A

    CDK Cancer
    Senexin A is a CDK8 inhibitor with an IC50 of 280 nM.
  • HY-126675
    AS2863619 free base

    CDK STAT Inflammation/Immunology
    AS2863619 free base enables conversion of antigen-specific effector/memory T cells into Foxp3 + regulatory T (Treg) cells for the treatment of various immunological diseases. AS2863619 free base is a potent, orally active cyclin-dependent kinase 8 (CDK8) and CDK19 inhibitor with IC50s of 0.61 nM and 4.28 nM, respectively. STAT5 activation enhanced by AS2863619 free base inhibition of CDK8/19, which consequently activates the Foxp3 gene.
  • HY-128669
    Abemaciclib metabolite M2

    LSN2839567

    CDK Cancer
    Abemaciclib metabolite M2 (LSN2839567) is a metabolite of Abemaciclib, acts as a potent CDK4 and CDK6 inhibitor, with IC50s in the range of 1-3 nM. Anti-cancer activity.
  • HY-128867
    bio-THZ1

    CDK Cancer
    bio-THZ1 is a biotinylated version of THZ1 and binds irreversibly to CDK7. THZ1 is a selective and potent covalent CDK7 inhibitor with an IC50 of 3.2 nM.
  • HY-19988
    THZ1-R

    CDK Cancer
    THZ1-R is a non-cysteine reactive analog of THZ1 which displays diminished activity for CDK7 inhibition. THZ1-R binds to CDK7 with a Kd of 142 nM.
  • HY-123937
    THAL-SNS-032

    PROTAC and Building Blocks CDK Cancer
    THAL-SNS-032 is a selective CDK9 degrader PROTAC consisting of a CDK-binding SNS-032 ligand linked to a thalidomide derivative that binds the E3 ubiquitin ligase Cereblon (CRBN).
  • HY-15166
    Zotiraciclib

    TG02; SB1317

    CDK JAK FLT3 Cancer
    Zotiraciclib (TG02; SB1317) is a potent inhibitor of CDK2, JAK2, and FLT3 for the treatment of cancer, with IC50s of 13, 73, and 56 nM for CDK2, JAK2 and FLT3, respectively.
  • HY-124719
    hSMG-1 inhibitor 11j

    PI3K mTOR GSK-3 CDK Cancer
    hSMG-1 inhibitor 11j, a pyrimidine derivative, is a potent and selective inhibitor of hSMG-1, with an IC50 of 0.11 nM. hSMG-1 inhibitor 11j exhibits >455-fold selectivity for hSMG-1 over mTOR (IC50=50 nM), PI3Kα/γ (IC50=92/60 nM) and CDK1/CDK2 (IC50=32/7.1 μM). hSMG-1 inhibitor 11j can be used for the research of cancer.
  • HY-50767
    Palbociclib

    PD 0332991

    CDK Cancer
    Palbociclib (PD 0332991) is a selective CDK4 and CDK6 inhibitor with IC50s of 11 and 16 nM, respectively. Palbociclib has the potential for ER-positive and HER2-negative breast cancer research.
  • HY-111931
    Indirubin-3'-monoxime-5-sulphonic acid

    CDK GSK-3 Cancer
    Indirubin-3'-monoxime-5-sulphonic acid is a potent and selective inhibitor of CDK1, CDK5, and GSK-3β with IC50s of 5 nM, 7 nM, and 80 nM, respectively.
  • HY-12483
    SR1664

    PPAR Metabolic Disease
    SR1664 is a PPARγ antagonist. SR1664 binds to PPARγ and potently inhibits Cdk5-mediated PPARγ phosphorylation (IC50=80 nM; Ki= 28.67 nM).
  • HY-12681
    CCT251545

    Wnt Cancer
    CCT251545 is an orally bioavailable and potent inhibitor of WNT signaling with an IC50 of 5 nM in 7dF3 cells. CCT251545 is a selective chemical probe for exploring the role of CDK8 and CDK19 in human disease.
  • HY-50767A
    Palbociclib monohydrochloride

    PD 0332991 monohydrochloride

    CDK Cancer
    Palbociclib (PD 0332991) monohydrochloride is a highly selective CDK4/6 inhibitor with IC50s of 11 nM and 16 nM, respectively. Palbociclib monohydrochloride has the potential for ER-positive and HER2-negative breast cancer research.
  • HY-12280
    THZ2

    CDK Cancer
    THZ2 is a potent and selective CDK7 inhibitor with an IC50 of 13.9 nM.
  • HY-12653
    LDC4297

    CDK HSV Infection
    LDC4297 is a potent and selective CDK7 inhibitor with an IC50 of 0.13 nM.
  • HY-19718
    OTS964

    TOPK CDK Apoptosis Cancer
    OTS964 is an orally active, high affinity and selective TOPK inhibitor with an IC50 of 28 nM. OTS964 is also a potent inhibitor of the cyclin-dependent kinase CDK11, which binds to CDK11B with a Kd of 40 nM.
  • HY-X0150
    JSH-150

    CDK Cancer
    JSH-150 is a highly selective and potent CDK9 inhibitor with an IC50 of 1 nM.
  • HY-11012
    TDZD-8

    GSK-3β Inhibitor I; NP 01139

    GSK-3 Cancer
    TDZD-8 is an inhibitor of GSK-3β, with an IC50 of 2 μM; TDZD-8 shows less potent activities against Cdk-1/cyclin B, CK-II, PKA, and PKC, with all IC50s of >100 μM.
  • HY-15878
    LDC000067

    LDC067

    CDK Apoptosis Cancer
    LDC000067 is a highly specific CDK9 inhibitor with an IC50 value of 44±10 nM in vitro.
  • HY-13816
    NU6027

    CDK ATM/ATR Cancer
    NU6027 is a potent and ATP-competitive inhibitor of both CDK1 and CDK2, with Kis of 2.5 µM and 1.3 µM, respectively. NU6027 is also a potent inhibitor of ATR and enhances hydroxyurea and cisplatin cytotoxicity in an ATR-dependent manner.
  • HY-N5072
    Desmethylglycitein

    4',6,7-Trihydroxyisoflavone

    CDK PI3K PKC Cancer
    Desmethylglycitein (4',6,7-Trihydroxyisoflavone), a metabolite of daidzein, sourced from Glycine max with antioxidant, and anti-cancer activities. Desmethylglycitein binds directly to CDK1 and CDK2 in vivo, resulting in the suppresses CDK1 and CDK2 activity. Desmethylglycitein is a direct inhibitor of protein kinase C (PKC)α, against solar UV (sUV)-induced matrix matrix metalloproteinase 1 (MMP1). Desmethylglycitein binds to PI3K in an ATP competitive manner in the cytosol, where it inhibits the activity of PI3K and downstream signaling cascades, leading to the suppression of adipogenesis in 3T3-L1 preadipocytes.
  • HY-18930
    NU6300

    CDK Cancer
    NU6300 is the first covalent, irreversible and ATP-competitive CDK2 inhibitor.
  • HY-100600
    BGG463

    K03859

    CDK Others
    BGG463 (K03859) is an orally active type II CDK2 inhibitor.
  • HY-19984
    CCT-251921

    CDK Cancer
    CCT-251921 is a potent, selective, and orally bioavailable CDK8 inhibitor with an IC50 of 2.3 nM.
  • HY-12422
    Voruciclib

    CDK Cancer
    Voruciclib is an orally active and selective CDK inhibitor with Ki values of 0.626 nM-9.1 nM. Voruciclib potently blocks CDK9, the transcriptional regulator of MCL-1. Voruciclib represses expression of MCL-1 in multiple models of diffuse large B-cell lymphoma (DLBCL).
  • HY-12422A
    Voruciclib hydrochloride

    CDK Cancer
    Voruciclib hydrochloride is an orally active and selective CDK inhibitor with Ki values of 0.626 nM-9.1 nM. Voruciclib hydrochloride potently blocks CDK9, the transcriptional regulator of MCL-1. Voruciclib hydrochloride represses expression of MCL-1 in multiple models of diffuse large B-cell lymphoma (DLBCL).
  • HY-10542
    GW 5074

    Raf Apoptosis Cancer
    GW 5074 is a potent and selective c-Raf inhibitor with IC50 of 9 nM, and has no effect on the activities of JNK1/2/3, MEK1, MKK6/7, CDK1/2, c-Src, p38 MAP, VEGFR2 or c-Fms.
  • HY-50767S
    Palbociclib D8

    PD 0332991 D8

    CDK Cancer
    Palbociclib D8 (PD 0332991 D8) is a deuterium labeled Palbociclib. Palbociclib is a selective and orally active CDK4 and CDK6 inhibitor with IC50s of 11 and 16 nM, respectively. Palbociclib has the potential for ER-positive and HER2-negative breast cancer research.
  • HY-137894
    PF-07104091

    CDK GSK-3 Cancer
    PF-07104091 is a potent and selective CDK2/cyclin E1 and GSK3β inhibitor, with Kis of 1.16 and 537.81 nM, respectively. PF-07104091 has anti-tumor activity for cyclin E1-amplified cancers. (patent WO2020157652A2).
  • HY-137894A
    PF-07104091 hydrate

    CDK GSK-3 Cancer
    PF-07104091 hydrate is a potent and selective CDK2/cyclin E1 and GSK3β inhibitor, with Kis of 1.16 and 537.81 nM, respectively. PF-07104091 hydrate has anti-tumor activity for cyclin E1-amplified cancers. (patent WO2020157652A2).
  • HY-12467
    OTS964 hydrochloride

    TOPK CDK Apoptosis Cancer
    OTS964 hydrochloride is an orally active, high affinity and selective TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor with an IC50 of 28 nM. OTS964 hydrochloride is also a potent inhibitor of the cyclin-dependent kinase CDK11, which binds to CDK11B with a Kd of 40 nM.
  • HY-130713
    Thalidomide-C2-amido-C2-COOH

    E3 Ligase Ligand-Linker Conjugate Cancer
    Thalidomide-C2-amido-C2-COOH incorporates a CRBN ligand for the E3 ubiquitin ligase, and a linker. Thalidomide-C2-amido-C2-COOH can be used to design PROTAC CDK2/9 Degrader-1 (HY-130709).
  • HY-123955
    Casein Kinase inhibitor A86

    Casein Kinase CDK Apoptosis Cancer
    Casein Kinase inhibitor A86 is a potent and orally active casein kinase 1α (CK1α) inhibitor. Casein Kinase inhibitor A86 also inhibits of CDK7 (TFIIH) and CDK9 (P-TEFb). Casein Kinase inhibitor A861 induces leukemia cell apoptosis, and has potent anti-leukemic activities.
  • HY-N0400
    Wogonin

    CDK Wnt Autophagy Apoptosis Cancer Inflammation/Immunology
    Wogonin is a naturally occurring mono-flavonoid, can inhibit the activity of CDK8 and Wnt, and exhibits anti-inflammatory and anti-tumor effects.
  • HY-130712
    NH2-C2-amido-C2-Boc

    PROTAC Linker Cancer
    NH2-C2-amido-C2-Boc is a PROTAC linker, which refers to the alkyl/ether composition. NH2-C5-NH-Boc can be used in the synthesis of a series of PROTACs, such as the PROTAC CDK2/9 Degrader-1 (HY-130709).
  • HY-112088
    AZD4573

    CDK Cancer
    AZD4573 is a potent and highly selective CDK9 inhibitor (IC50 of <4 nM) that enables transient target engagement for the treatment of hematologic malignancies.
  • HY-15336
    AG 555

    Tyrphostin AG 555

    EGFR Reverse Transcriptase Cancer
    AG 555 (Tyrphostin AG 555), a potent antiretroviral drug, is a potent and selective inhibitor of EGFR and blocks Cdk2 activation.
  • HY-103019A
    (±)-BAY-1251152

    CDK Cancer
    (±)-BAY-1251152 is a racemic mixture of BAY-1251152. BAY-1251152 is a potent and highly selective PTEF/CDK9 inhibitor.
  • HY-103019B
    (-)-BAY-1251152

    CDK Cancer
    (-)-BAY-1251152 is an enanthiomer of BAY-1251152 with rotation (-). BAY-1251152 is a potent and highly selective PTEF/CDK9 inhibitor.
  • HY-114177A
    (S)-PF-06873600

    Others Cancer
    (S)-PF-06873600 it the S enantiomer of PF-06873600. PF-06873600 is a selective and orally bioavailable inhibitor of cyclin-dependent kinase (CDK).
  • HY-137432
    Avotaciclib

    BEY1107

    CDK Cancer
    Avotaciclib (BEY1107) is an orally active cyclin dependent kinase 1 (CDK1) inhibitor. Avotaciclib can be used for the research of cancer.
  • HY-117025A
    Manzamine A hydrochloride

    GSK-3 CDK Parasite HIV Proton Pump Autophagy Cancer Infection Neurological Disease
    Manzamine A hydrochloride, an orally active beta-carboline alkaloid, inhibits specifically GSK-3β and CDK-5 with IC50s of 10.2 and 1.5μM, respectively. Manzamine A hydrochloride targets vacuolar ATPases and inhibits autophagy in pancreatic cancer cells. Manzamine A hydrochloride has antimalarial and anticancer activities. Manzamine A hydrochloride also shows potent activity against HSV-1.
  • HY-A0065
    Palbociclib isethionate

    PD 0332991 isethionate

    CDK Cancer
    Palbociclib isethionate is a highly selective inhibitor of CDK4/6 with IC50s of 11 nM/16 nM, respectively.
  • HY-12422B
    (2S,3R)-Voruciclib hydrochloride

    CDK Cancer
    (2S,3R)-Voruciclib hydrochloride is the enantiomer of Voruciclib hydrochloride. (2S,3R)-Voruciclib is an orally active CDK inhibitor.
  • HY-135366
    HPN-01

    IKK Inflammation/Immunology
    HPN-01 is a potent and selective IKK inhibitor, with pIC50 values of 6.4, 7.0 and <4.8 for IKK-α, IKK-β and IKK-ε, respectively. HPN-01 displays greater 50-fold selectivity over a panel of more than 50 other kinases, including ALK5, CDK-2, EGFR, ErbB2, GSK3β, PLK1, Src, and VEGFR-2.
  • HY-18944
    FIT-039

    CDK HSV CMV DNA/RNA Synthesis Infection
    FIT-039 is a selective, ATP-competitive and orally active CDK9 inhibitor with an IC50 of 5.8 μM for CKD9/cyclin T1. FIT-039 does not inhibit other CDKs and other kinases. FIT-039 inhibits replication of HSV-1 (IC50 of 0.69 μM), HSV-2, human adenovirus, and human CMV. FIT-039 is a promising antiviral agent for inhibiting drug-resistant HSVs and other DNA viruses.
  • HY-141680
    CPS2

    CDK Cancer
    CPS2 is a first-in-class, highly potent, selective and irreversible PROTAC CDK2 degrader (IC50= 24 nM). CPS2 can be used for the research of acute myeloid leukemia.
  • HY-120350
    BI-1347

    CDK Cancer
    BI-1347 is a potent CDK8 inhibitor extracted from patent WO2017202719A1, product I-003, has an IC50 of 1.1 nM.
  • HY-139011
    IV-361

    CDK Cancer
    IV-361 is an orally active and selective CDK7 inhibitor (Ki≤50 nM). IV-361 has anti-cancer activity (US20190256531A1).
  • HY-12892
    SKI-178

    SphK Apoptosis Cancer
    SKI-178 is a potent sphingosine kinase-1 (SphK1) and SphK2 inhibitor. SKI-178 is cytotoxic at IC50 concentrations ranging from 1.8 to 0.1 μM in both drug sensitive and multi-drug resistant cancer cell lines (i.e., MTR3, NCI-ADR and HL60/VCR cells). SKI-178 induces apoptosis in a CDK1-dependent manner in human acute myeloid leukemia cell lines.
  • HY-108136A
    Bisindolylmaleimide X hydrochloride

    BIM-X hydrochloride; Ro31-8425 hydrochloride

    PKC CDK Cardiovascular Disease
    Bisindolylmaleimide X hydrochloride (BIM-X hydrochloride) is a potent and selective protein kinase C (PKC) inhibitor. Bisindolylmaleimide X hydrochloride is a potent cyclin-dependent kinase 2 (CDK2) antagonist with an IC50 of 200 nM.
  • HY-125843
    Pomalidomide-PEG1-C2-N3

    Cereblon Ligand-Linker Conjugates 13; E3 ligase Ligand-Linker Conjugates 50

    E3 Ligase Ligand-Linker Conjugate Cancer
    Pomalidomide-PEG1-C2-N3 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and 1-unit PEG linker used in PROTAC technology. Pomalidomide-PEG1-C2-N3 can be used to design a selective CDK6 PROTAC degrader CP-10. CP-10 induces the degradation of CDK6 with an DC50 of 2.1 nM.
  • HY-103019
    (+)-BAY-1251152

    CDK Cancer
    (+)-BAY-1251152 is an enanthiomer of BAY-1251152 with rotation (+). (+)-BAY-1251152 is a potent and selective CDK9 inhibitor with an IC50 of 3 nM. (+)-BAY-1251152 has anti-tumour activity.
  • HY-114712
    SJ572403

    SJ403

    Others Cancer
    SJ572403 (SJ403) is an inhibitor of disordered protein p27(Kip1). p27(Kip1) is a regulator of the CDKs that control eukaryotic cell division.
  • HY-12624
    ON123300

    CDK AMPK Cancer
    ON123300, a strong and brain-penetrant multi-kinase inhibitor, inhibits CDK4 (IC50=3.9 nM), Ark5 (IC50=5 nM), PDGFRβ (IC50=26 nM), FGFR1 (IC50=26 nM), RET (IC50=9.2 nM), and FYN (IC50=11 nM). Single agent ON123300 causes a dose-dependent suppression of phosphorylation of Akt as well as activation of Erk in brain tumors. ON123300 inhibits CDK6 with an IC50 of 9.82 nM.
  • HY-12422C
    (2S,3R)-Voruciclib

    CDK Cancer
    (2S,3R)-Voruciclib is the (2S,3R)-enantiomer of Voruciclib. (2S,3R)-Voruciclib is an orally active CDK inhibitor.
  • HY-41076
    Ca2+ channel agonist 1

    Calcium Channel CDK Neurological Disease
    Ca 2+ channel agonist 1 is an agonist of N-type Ca 2+ channel and an inhibitor of Cdk2, with EC50s of 14.23 μM and 3.34 μM, respectively, and is used as a potential treatment for motor nerve terminal dysfunction.
  • HY-15532
    SCH900776

    MK-8776

    Checkpoint Kinase (Chk) Cancer
    SCH900776 (MK-8776) is a potent, selective and orally bioavailable inhibitor of checkpoint kinase1 (Chk1) with an IC50 of 3 nM. SCH900776 shows 50- and 500-fold selectivity over CDK2 and Chk2, respectively.
  • HY-12498
    GV-58

    Calcium Channel Neurological Disease
    GV-58 is a potent, selective N- and P/Q-type Ca2+ channels agonist with EC50 of 7.21/8.81 uM for N-type/P-Q-type Ca2+ channel; 20-fold less potent CDK inhibitor activity.
  • HY-129478
    TC11

    Caspase Bcl-2 Family CDK Cancer
    TC11 is a MCL1 degradator and Caspase-9 and CDK1 activator. TC11 structurally relates to immunomodulatory drugs as phenylphthalimide derivative. TC11 induces apoptotic death caused by degradation of MCL1 during prolonged mitotic arrest.
  • HY-P1933A
    [pSer2, pSer5, pSer7]-CTD TFA

    CDK Cancer
    [pSer2, pSer5, pSer7]-CTD (TFA), a substrate for CDK7 (cyclin dependent protein kinase), is a phosphorylated polypeptide at ser2, ser5 and ser7 sites of RNA polymerase II carboxy-terminal domain (CTD).
  • HY-128587
    Mevociclib

    SY-1365

    CDK Cancer
    Mevociclib (SY-1365) is a potent and first-in-class selective CDK7 inhibitor, with a Ki of 17.4 nM. Mevociclib exhibits anti-proliferative and apoptotic effects in solid tumor cell lines. Mevociclib possesses anti-tumor activity in hematological and multiple aggressive solid tumors.
  • HY-N1127
    Tricin

    CMV Cancer Infection
    Tricin is a natural flavonoid present in large amounts in rice bran. Tricin can inhibit human cytomegalovirus (HCMV) replication by inhibiting CDK9. Tricin inhibits the proliferation and invasion of C6 glioma cells via the upregulation of focal-adhesion-finase (FAK)-targeting microRNA-7.
  • HY-N1986
    Cucurbitacin D

    HSP Cancer
    Cucurbitacin D is an active component in Cucurbita texana, disrupts interactions between Hsp90 and two co-chaperones, Cdc37 and p23. Cucurbitacin D prevents Hsp90 client (Her2, Raf, Cdk6, pAkt) maturation without induction of the heat shock response. Anti-cancer activity.
  • HY-N0636
    Eriocitrin

    Apoptosis Cancer
    Eriocitrin is a flavonoid isolated from lemon, which is a strong antioxidant agent. Eriocitrin could inhibit the proliferation of hepatocellular carcinoma cell lines by arresting cell cycle in S phase through up-regulation of p53, cyclin A, cyclin D3 and CDK6. Eriocitrin triggers apoptosis by activating mitochondria-involved intrinsic signaling pathway.
  • HY-114302
    CCB02

    Microtubule/Tubulin Cancer
    CCB02 is a selective CPAP-tubulin interaction inhibitor, binding to tubulin and competing for the CPAP binding site of β-tubulin, with an IC50 of 689 nM, and shows potent anti-tumor activity. CCB02 shows no inhibition on the cell cycle- and centrosome-related kinases, or the phosphorylation status of Aurora A, Plk1, Plk2, CDK2, and CHK1.
  • HY-13941B
    1-Naphthyl PP1 hydrochloride

    1-NA-PP 1 hydrochloride

    Src Cancer
    1-Naphthyl PP1 hydrochloride (1-NA-PP 1 hydrochloride) is a selective inhibitor of src family kinases. 1-Naphthyl PP1 hydrochloride inhibits v-Src and c-Fyn, c-Abl, CDK2 and CAMK II with IC50s of 1.0, 0.6, 0.6, 18 and 22 μM, respectively.
  • HY-116423A
    JH295 hydrate

    Others Cancer
    JH295 hydrate is a potent, irreversible and selective NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 770 nM. JH295 hydrate inhibits cellular Nek2 via alkylation of Cys22. JH295 hydrate is inactive against the mitotic kinases, Cdk1, Aurora B or Plk1, and does not perturb bipolar spindle assembly or the spindle assembly checkpoint.
  • HY-13941
    1-Naphthyl PP1

    1-NA-PP 1

    Src Cancer
    1-Naphthyl PP1 (1-NA-PP 1) is a selective inhibitor of src family kinases. 1-Naphthyl PP1 inhibits v-Src and c-Fyn, c-Abl, CDK2 and CAMK II with IC50s of 1.0, 0.6, 0.6, 18 and 22 μM, respectively.
  • HY-116423
    JH295

    Others Cancer
    JH295 is a potent, irreversible and selective NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 770 nM. JH295 inhibits cellular Nek2 via alkylation of Cys22. JH295 is inactive against the mitotic kinases, Cdk1, Aurora B or Plk1, and does not perturb bipolar spindle assembly or the spindle assembly checkpoint.
  • HY-139039
    BSJ-4-116

    PROTAC and Building Blocks CDK Cancer
    BSJ-4-116 is a highly potent and selective CDK12 degrader (PROTAC) with an IC50 of 6 nM. BSJ-4-116 downregulates DDR genes through a premature termination of transcription, primarily through increasing poly(adenylation). BSJ-4-116 exhibits potent antiproliferative effects, alone and in combination with the poly(ADP-ribose) polymerase inhibitor Olaparib (HY-10162).
  • HY-12072
    Lck Inhibitor

    Src Inflammation/Immunology
    Lck Inhibitor is a potent, orally active Lck (lymphocyte specific kinase) inhibitor with IC50s of 7, 2.1, 4.2 and 200 nM for Lck, Lyn, Src and Syk kinases, respectively. Lck Inhibitor shows >1000-fold selectivity for Lck over MAPK, CDK and RSK family representatives. Lck Inhibitor inhibits T cell proliferation and in vivo models of arthritis.
  • HY-18285
    Longdaysin

    Casein Kinase ERK CDK Cancer
    Longdaysin is a inhibitor of the Wnt/β-catenin signaling pathway, which exerts antitumor effect through blocking CK1δ/ε-dependent Wnt signaling. Longdaysin inhibits CK1α, CK1δ, CDK7, and ERK2 with IC50s of  5.6 µM, 8.8 µM, 29 µM, and 52 µM, respectively.
  • HY-13650
    Indisulam

    E 7070

    Carbonic Anhydrase Cancer
    Indisulam (E 7070) is a carbonic anhydrase inhibitor with anticancer activity. Indisulam (E 7070) is a sulfonamide agent that targets the G1 phase of the cell cycle. Indisulam (E 7070) causes a blockade in the G1/S transition through inhibition of the activation of both CDK2 and cyclin E. Indisulam (E 7070) targets splicing by inducing RBM39 degradation via recruitment to DCAF15.
  • HY-119016A
    SK1-​I hydrochloride

    BML-258 hydrochloride

    SphK Cancer
    SK1-I hydrochloride (BML-258 hydrochloride), an analog of sphingosine, is an isozyme-specific competitive SPHK1 inhibitor with a Ki value of 10 µM. SK1-I hydrochloride shows no activity at SPHK1 PKCα, PKCδ, PKA, AKT1, ERK1, EGFR, CDK2, IKKβ or CamK2β. SK1-I hydrochloride enhances autophagy and has antitumor activity.
  • HY-101042
    AG-494

    Tyrphostin AG 494

    EGFR CDK Cancer
    AG-494 (Tyrphostin AG 494) is a potent and selective EGFR tyrosine kinase inhibitor (IC50=0.7 μM). AG-494 inhibits the autophosphorylation of EGFR, ErbB2, HER1-2 and PDGF-R with IC50s 1.1, 39, 45 and 6 μM, respectively. AG-494 blocks Cdk2 activation and inhibits EGF-dependent DNA synthesis.
  • HY-119016
    SK1-I

    BML-258

    SphK Cancer
    SK1-I (BML-258), an analog of sphingosine, is an isozyme-specific competitive SPHK1 inhibitor with a Ki value of 10 µM. SK1-I shows no activity at SPHK1 PKCα, PKCδ, PKA, AKT1, ERK1, EGFR, CDK2, IKKβ or CamK2β. SK1-I enhances autophagy and has antitumor activity.
  • HY-11010
    AS601245

    JNK Cancer Inflammation/Immunology Neurological Disease
    AS601245 is an orally active, selective, ATP competitive JNK (c-Jun NH2-terminal protein kinase) inhibitor with IC50s of 150, 220, and 70 nM for three JNK human isoforms (hJNK1, hJNK2, and hJNK3), respectively. AS601245 exhibits 10- to 20-fold selectivity over c-src, CDK2, and c-Raf and more than 50- to 100-fold selectivity over a range of Ser/Thr- and Tyr-protein kinases. Neuroprotective properties.
  • HY-112457
    MK2-IN-3 hydrate

    MAPKAPK2 (MK2) Inflammation/Immunology
    MK2-IN-3 hydrate (compound 16) is an orally active, selective, and ATP-competitive MAPKAP-K2 (MK-2) inhibitor with an IC50 of 0.85 nM.MK2-IN-3 hydrate is exceptional selectivity against MK-3 (IC50=0.21 μM), MK-5 (IC50=0.081 μM), ERK2 (IC50=3.44 μM), MNK1(IC50=5.7 μM) as well as CDK2, JNK2, IKK2, MSK1, and MSK2.
  • HY-139254
    Indirubin-3′-oxime

    IDR3O; I3O

    CDK GSK-3 JNK Neurological Disease
    Indirubin-3′-oxime (IDR3O), a synthetic derivative of indirubin, is a potent inhibitor of cyclin-dependent kinases (CDKs) and glycogen synthase kinase 3β (GSK3β). Indirubin-3′-oxime directly inhibits the activity of all three isoforms of JNK (JNK1, JNK2, and JNK3), with IC50s of 0.8 μM, 1.4 μM, and 1.0 μM, respectively. Indirubin-3′-oxime can enhance height growth via activation of Wnt/β-catenin signaling in chondrocytes.
  • HY-N6954
    Garcinone C

    ATM/ATR STAT CDK Cancer
    Garcinone C, a xanthone derivative, is a natural compound extracted from Garcinia oblongifolia Champ that is used as an anti-inflammatory, analgesia, astringency and granulation-promoting medicine, and has potential cytotoxic effects on certain cancers. Garcinone C stimulates the expression levels of ATR and 4E-BP1, while efficiently inhibiting the expression levels of cyclin B1, cyclin D1, cyclin E2, cdc2, Stat3 and CDK7. Garcinone C significantly inhibits cell viability of the human Nasopharyngeal carcinoma (NPC) cell lines CNE1, CNE2, HK1 and HONE1 in a time‑ and dose‑dependent manner.
  • HY-131249
    MK2-IN-3

    MAPKAPK2 (MK2) Inflammation/Immunology
    MK2-IN-3 is a potent and selective inhibitor of MAPKAP-K2 (MK-2), with an IC50 of 8.5 nM. MK2-IN-3 shows selectivity for MK-2 over MK-3, MK-5, ERK2, MNK1, p38a (IC50s=0.21, 0.081, 3.44, 5.7, and >100 μM, respectively) and MSK1, MSK2, CDK2, JNK2, IKK2 (IC50s>200 μM). MK2-IN-3 can reduce TNFα production in both U937 cells and in vivo.