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CDK

Cyclin-dependent kinases (CDKs) are the families of protein kinases first discovered for their role in regulating the cell cycle. They are also involved in regulating transcription, mRNA processing, and the differentiation of nerve cells.They are present in all known eukaryotes, and their regulatory function in the cell cycle has been evolutionarily conserved.

  • Dinaciclib
    T1912779353-01-4
    Dinaciclib (SCH 727965) is a selective CDK inhibitor targeting CDK1, CDK2, CDK5, and CDK9 (IC50 = 3 1 1 4 nM). It exhibits potential antitumor activity by inhibiting the incorporation of thoracic glycan (dThd) DNA.
    • $47
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  • Nimbolide
    T1632425990-37-8
    Nimbolide suppresses CDK4 CDK6 kinase activity. Nimbolide inhibits the NF-κB, Wnt, PI3K-Akt, MAPK, and JAK-STAT signaling pathways. Nimbolide causes apoptosis through the inactivation of NF-κB. Nimbolide is a triterpene derived from the leaves and flowers
    • $81
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  • Abemaciclib
    T23811231929-97-7
    Abemaciclib (LY2835219) is a dual inhibitor of CDK4/6 (IC50=2/10 nM) with selectivity and specificity. Abemaciclib has antitumor activity and is used to treat advanced or metastatic breast cancer.
    • $48
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  • AS2863619
    T83782241300-51-4
    AS2863619 is an oral inhibitor of cyclin-dependent kinase 8 (CDK8) and CDK19. Inhibition of CDK8 19 can enhance the activation of STAT5, thereby activating the Foxp3 gene. It can convert antigen-specific effector memory T cells into Foxp3+ regulatory T cells to study various immune diseases.
    • $133
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  • Palbociclib
    T1785571190-30-2
    Palbociclib (PD 0332991) is a CDK inhibitor that inhibits CDK4 and CDK6 (IC50=11 16 nM) and is orally active. Palbociclib has anti-tumorigenic activity and has investigational potential for use in ER-positive and HER2-negative breast cancer.
    • $48
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  • Flavopiridol hydrochloride
    T2615131740-09-5
    Flavopiridol hydrochloride (MDL 107826A) is a synthetic N-methylpiperidinyl chlorophenyl flavone compound. As an inhibitor of cyclin-dependent kinase, alvocidib induces cell cycle arrest by preventing phosphorylation of cyclin-dependent kinases (CDKs) and by down-regulating cyclin D1 and D3 expression, resulting in G1 cell cycle arrest and apoptosis. This agent is also a competitive inhibitor of adenosine triphosphate activity.
    • $44
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  • Simurosertib
    T12642L1330782-76-7
    Simurosertib (TAK-931) is a selective and ATP-competitive cell division cycle 7 kinase inhibitor (IC50: <0.3 nM).
    • $68
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  • KB-0742 dihydrochloride
    T94462416874-75-2
    KB-0742 dihydrochloride is a potent, selective, and orally administered inhibitor of CDK9.
    • $97
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  • SY-5609
    T360382417302-07-7In house
    SY-5609 (CDK7-IN-3) is a selective non-covalent CDK7 inhibitor (Kd value is 0.07 nM), with weak inhibitory activity against CDK2, CDK9 and CDK12 with IC50 values ​​of 5.5, 1.9 and 1.7 μM, respectively, and has anti-tumor activity and inhibits cell apoptosis.
    • $142
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  • PF-562271
    T2465717907-75-0
    PF-562271 is an effective ATP-competitive, reversible inhibitor of FAK(IC50=1.5 nM) and Pyk2 kinase(IC50=13 nM).
    • $54
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  • Ribociclib
    T61991211441-98-3
    Ribociclib (LEE011) is an orally available, and highly specific CDK4 6 inhibitor (IC50:10 39 nM).
    • $36
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  • Samuraciclib hydrochloride
    T108981805789-54-1
    Samuraciclib hydrochloride (ICEC0942 hydrochloride) is a potent, selective, ATP competitive and oral active CDK7 inhibitor with IC50 of 41 nM. The selectivity of Samuraciclib hydrochloride is 45-, 15-, 230- and 30-fold higher than CDK1, CDK2 (IC50 is 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.
    • $116
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  • Cdk1/2 Inhibitor III
    T14914443798-55-8In house
    Cdk1 2 Inhibitor III is a selective inhibitor of Cdk1 2 with an IC50 value of 2.1 μM against CDK1 cyclin B.
    • $350
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  • XL413
    T33521169558-38-6In house
    XL-413 is an orally bioavailable cell division cycle 7 homolog (CDC7) kinase inhibitor with potential antineoplastic activity. XL-413 binds to and inhibits the activity of CDC7, which may result in the inhibition of DNA replication and mitosis, the induct
    • $48
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  • Ro-3306
    T2356872573-93-8
    RO-3306 is a selectivity ATP-competitive CDK1 inhibitor (Ki: 20 nM). The selectivity of RO-3306 for CDK1 is >15-fold higher than a diverse panel of human kinases.
    • $32
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  • Sodium Oxamate
    T19831565-73-1
    Sodium Oxamate (Oxamic acid sodium salt) is an LDH inhibitor that specifically inhibits LDHA. Sodium Oxamate has antitumor activity and induces cell cycle arrest and apoptosis.
    • $31
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  • Indisulam
    T4321165668-41-7
    Indisulam (E 7070) is a carbonic anhydrase inhibitor and antitumor CDK inhibitor that targets the G1 phase of the cell cycle by depleting cyclin E, inducing p53 and p21, and inhibiting CDK2, thereby causing a blockade in the G1 S transition.
    • $30
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  • PHA-767491
    T6206845714-00-3
    PHA-767491 (CAY10572) is a potent ATP-competitive dual Cdc7/CDK9 inhibitor with IC50 of 10 nM and 34 nM, respectively.
    • $30
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  • HTH-01-091
    T241522000209-42-5In house
    HTH-01-091 is a potent and selective maternal embryonic leucine zipper kinase (MELK) inhibitor (IC50: 10.5 nM) that also inhibits PIM1 2 3, RIPK2, DYRK3, smMLCK, and CLK2. It can be used to study breast cancer.
    • $296
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  • KenPaullone
    T2247142273-20-9
    KenPaullone (9-Bromopaullone), a potent CDK1, CDK2 and CDK5 inhibitor, as new enhancer for iTreg cell differentiation. Kenpaullone promotes iTreg cell differentiation through increased and prolonged transcription of foxp3 gene by enhancing TGFβ-Smad3 signaling pathway.
    • $32
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  • PF-06873600
    T84632185857-97-8
    PF-06873600, a selective and orally bioavailable cyclin-dependent kinase (CDK) inhibitor (CDK2, CDK4, and CDK6 with Ki values of 0.09 nM, 0.13 nM, and 0.16 nM, respectively), has potential antineoplastic activity.
    • $52
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  • (E/Z)-Zotiraciclib
    T21503937270-47-8
    (E Z)-Zotiraciclib ((E Z)-TG02) effectively inhibits CDK2, JAK2, and FLT3 with IC50s of 13 nM, 73 nM, and 56 nM, respectively.
    • $38
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  • XY028-140
    T366942229974-83-6
    XY028-140 is a selective CDK4/CDK6 degrade and inhibits both CDK4/6 expression and activity in cancer cells. XY028-140 is a PROTAC connected by ligands for Cereblon and CDK.
    • $34
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  • BX795
    T1830702675-74-9
    BX795 is an effective and selective PDK1 inhibitor (IC50: 6 nM), and its selectivity is 140- and 1600-fold for PDK1 over PKA and PKC in cell-free assays, respectively. Meanwhile, the selectivity for PDK1 is 100-fold than GSK3β.
    • $54
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  • JSH-150
    T84842247481-21-4
    JSH-150 is a highly selective CDK9 inhibitor with an IC50 of 1 nM.
    • $30
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  • CDK4/6-IN-2
    T107361800506-48-2
    CDK4 6-IN-2 is a potent inhibitor of CDK4 and CDK6 [IC50s: 2.7 and 16 nM].
    • $97
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  • CDK4/6/1 Inhibitor
    T107352099128-41-1In house
    CDK4/6/1 Inhibitor (Crozbaciclib) is a type of CDK4/6 inhibitor (IC50s: 3 and 1 nM). CDK4/6 inhibitor is a class of compounds used for the treatment of some types of hormone receptor positive, HER2-negative breast cancer, which can block the process of breast cancer cell division and reproduction.
    • $329
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  • THZ531
    T42931702809-17-3
    THZ531 is a covalent inhibitor of both CDK12(IC50=158 nM) and CDK13(IC50=69 nM).
    • $57
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  • P18IN011
    T857677408-67-4
    P18IN011 (P18IN011 - CAS 77408-67-4 - Calbiochem) is a novel inhibitor of p18(INK4C).
    • $133
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  • Flavopiridol
    T6837146426-40-6
    Flavopiridol (Alvocidib) (Alvocidib) competes with ATP to inhibit CDKs including CDK1, CDK2, CDK4 and CDK6 with IC50 of ~ 40 nM. It is 7.5-fold more selective for CDK1, 2, 4, 6 versus CDK7. Flavopiridol is initially found to inhibit EGFR and PKA. Phase 1 2.
    • $34
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  • OTS964 hydrochloride
    T41351338545-07-5
    OTS964 hydrochloride (OTS964) is a potent and selective TOPK inhibitor with potential anticancer activity.
    • $38
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  • T025
    T130582407433-00-3
    T025 is a pan CLK inhibitor with Kds of 4.8, 0.096, 6.5, 0.61, and 0.074 nM for CLK1-4, respectively. T025 displays anti-proliferative activities with IC50s of 30-300 nM in hematological and solid cancer cell lines. T025 can be used in studies about MYC-driven diseases.
    • $146
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  • BSJ-03-123
    T53952361493-16-3
    BSJ-03-123 is a potent, CDK6-selective small-molecule degrader.
    • $84
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  • ML141
    T246371203-35-5
    ML141 (CID-2950007) is an effective, specific and reversible non-competitive inhibitor of Rho family GTPase cdc42 (IC50: 200 nM).
    • $33
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  • R547
    T6312741713-40-6In house
    R547 (Ro 4584820) is a potent ATP-competitive inhibitor of CDK1 2 4 with Ki of 2 nM 3 nM 1 nM. It is less potent to CDK7 and GSK3α β, while inactive to other kinases. Phase 1.
    • $45
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  • URMC-099
    T60571229582-33-5
    URMC-099 is an orally bioavailable, brain penetrant MLK inhibitor (IC50: 19/42/14/150 nM, for MLK1/MLK2/MLK3/DLK), and also inhibits LRRK2 activity (IC50: 11 nM).
    • $52
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  • PF07104091
    T97122460249-19-6
    PF07104091 inhibits CDK2, which may lead to cell cycle arrest, induce apoptosis and inhibit tumor cell proliferation.[1]
    • $372
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  • (S)-Enitociclib
    T703881610408-97-3In house
    (S)-Enitociclib (VIP152) is a selective CDK9 inhibitor that induces complete regression of MYC+ lymphomas by inhibiting RNA polymerase II-mediated transcription of anti-apoptotic and pro-survival proteins.
    • $518
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  • PF 477736
    T6028952021-60-2
    PF 477736 (PF-736,PF-00477736) is a specifc, effective and ATP-competitive Chk1 inhibitor (Ki: 0.49 nM ) and also inhibits FGFR3, Aurora-A, VEGFR2, Flt3, Fms (CSF1R), Ret and Yes.
    • $45
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  • FN-1501
    T153351429515-59-2
    FN-1501 is a potent FLT3 and CDK inhibitor (IC50s: 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 also has anticancer activity.
    • $84
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  • Pinoresinol
    TN2080487-36-5
    Pinoresinol ((+)-Pinoresinol) has antiinflammatory, hepatoprotective, and fungicidal activities, it can protect pial microcirculation from I-reperfusion injury, to increase nitric oxide release and to reduce oxidative stress preserving pial blood flow distribution; it may exert pharmacologically interesting effects via modulation of the insulin-like signalling pathway in C.elegans. Pinoresinol causes an upregulation of the CDK inhibitor p21(WAF1 Cip1) both at mRNA and protein levels, inhibits NF-kappaB and activating protein 1 (AP-1).
    • $52
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  • CDK12-IN-2
    T397522244987-03-7
    CDK12-IN-2 (CDK12 inhibitor 2) is an effective and selective inhibitor of CDK12 with an IC50 of 52 nM, >100 μM, >10 μM and 16 μM for CDK12, CDK2, CDK7, and CDK9. CDK12-IN-2 can be used in studies about the function of CDK12.
    • $93
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  • CCT-251921
    T149011607837-31-9In house
    CCT-251921 is a potent, selective, and orally bioavailable CDK8 inhibitor [IC50: 2.3 nM].
    • $87
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  • Abemaciclib metabolite M20
    T107382138499-06-4In house
    Abemaciclib metabolite M20 (CDK4/6-IN-4) is an active metabolite of Abemaciclib. Abemaciclib metabolite M20 is a selective CDK4/6 inhibitor and can be used for researches on the treatment of cancer.
    • $93
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  • Palbociclib monohydrochloride
    T6239827022-32-2
    Palbociclib monohydrochloride (PD 0332991 hydrochloride) is a selective inhibitor of CDK4 6 (IC50s: 11 16 nM). It exhibits no inhibition against a panel of 36 additional protein kinases.
    • $30
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  • Abemaciclib methanesulfonate
    T31111231930-82-7
    Abemaciclib methanesulfonate (LY2835219) is a specific and effective inhibitor of CDK4(IC50=2 nM) and CDK6(IC50=10 nM).
    • $30
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  • AZD-5597
    T21544924641-59-8
    AZD-5597 ((S)-(4-((5-Fluoro-4-(1-isopropyl-2-methyl-1H-imidazol-5-yl)pyrimidin-2-yl)amino)phenyl)(3-(methylamino)pyrrolidin-1-yl)methanone) is a potent imidazole pyrimidine amide CDK inhibitor.
    • $52
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  • SU9516
    T6167377090-84-1
    SU9516 is a potent CDK2 inhibitor with an IC50 of 22 nM and also inhibits CDK1 and CDK4, with IC50s of 40 nM and 200 nM, respectively.
    • $30
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  • CLK1/2-IN-3
    T238971005784-60-0In house
    CLK1 2-IN-3 (Cpd-3) is a potent and selective CLK1 and CLK2 inhibitor with antiproliferative activity and inhibits the activities of CLK1, CLK2, SRPK1, SRPK2, and SRPK3.CLK1 2-IN-3 induces nuclear speckle enlargement, which induces S6K pre-mRNA-selective splicing and subsequent inhibition of cell growth of multiple cancer cell types. cancer cell types cell growth.
    • $350
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  • 26-Deoxyactein
    TN1222264624-38-6
    23-epi-26-Deoxyactein (27-Deoxyactein) has anti-inflammatory activity, it inhibits nitric oxide production by reducing iNOS expression without affecting activity of the enzyme. It also has anti-cancer activity, it can inhibit growth of the MCF7 human breast cancer cells and induce cell cycle arrest at G1.
    • $98
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