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CDK
T1778 AT 7519 hydrochloride salt AT7519 hydrochloride is a multi-CDK inhibitor for CDK1, 2, 4, 6 and 9.
T1785 Palbociclib Palbociclib is an orally available cyclin-dependent kinase (CDK) inhibitor with potential antineoplastic activity. Palbociclib selectively inhibits cyclin-dependent kinase 4 (CDK4) and 6 (CDK6), thereby inhibiting retinoblastoma (Rb) protein phosphorylation early in the G1 phase leading to cell cycl
T1830 BX795 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.
T1837 BX-912 BX-912 is a specific inhibitor of 3-Phosphoinositide-dependent Kinase-1 (PDK1, IC50: 12 nM). The selectivity of BX-912 is more 10 fold than C-Kit, EGFR, PKA, PKC etc.
T1855 ZCL 278 ZCL278 is a selective Cdc42 GTPase inhibitor.
T1912 Dinaciclib Dinaciclib, a new-type and effective CDK inhibitor, for CDK2( IC50=1 nM), CDK5(IC50=1 nM), CDK1( IC50=3 nM) and CDK9(IC50=4 nM), has potential antineoplastic activity.
T1917 BIO BIO is a specific inhibitor of GSK-3.
T1947 BS-181 BS-181 is a highly selective CDK7 inhibitor (IC50: 21 nM); >40-fold selective for CDK7 than CDK1/2/4/5/6/9.
T2028 NG-52 NG 52 is a cell-permeable, reversible, and ATP-compatible inhibitor of the cell cycle-regulating kinase Cdc28p and the related Pho85p kinase.
T2029 Bohemine Bohemine is a cyclin-dependent kinase inhibitor.
T2032 WHI-P180 WHI-P180 is a potent EGFR and Cdk2 inhibitors with IC50 of 4.0 and 1.0 uM, respectively.
T2059 Purvalanol A Purvalanol A is an effective and cell-permeable CDK inhibitor with IC50 of 70/4/35/850 nM for cdk2-cyclin A/B/E, and cdk4-cyclin D1, respectively.
T2082 CDK4-IN-1 CDK4 inhibitor is a novel and specific CDK4/Cyclin D1 inhibitor with an IC50 of 10 nM; 1500 and 500 fold than CDK1/Cyclin B (IC50>15 uM) and CDK2/Cyclin A (IC50=5.265 uM) respectively.
T2095 Roscovitine Seliciclib is an orally available small molecule and cyclin-dependent kinase (CDK) inhibitor with potential apoptotic and antineoplastic activity.
T2113 PHA-793887 PHA-793887 has been used in trials studying the treatment of Advanced/Metastatic Solid Tumors.
T2118 SC-514 SC-514 is a selective, orally active, ATP-competitive IKK-2 inhibitor (IC50=11.2±4.7 μM), obstructs NF-κB-dependent gene expression.
T2153 1-NM-PP1 1NM-PP1 is a cell-permeable PP1 analog that acts as a potent and selective inhibitor of mutant kinases over their wild-type progenitors.
T2193 2-Chloropyrazine 2-Chloropyrazine is used in chemical industry.
T2246 LRRK2-IN-1 LRRK2-IN-1 is an effective and selective LRRK2 inhibitor.
T2247 KenPaullone Kenpaullone, 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.
T2356 Ro 3306 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.
T2378 RGB-286638 free base RGB-286638 free base is a novel CDK inhibitor with IC50s of 1 nM/2 nM/3 nM/4 nM/5 nM for cyclin T1-CDK9/cyclin B1-CDK1/cyclin E-CDK2/cyclin D1-CDK4/cyclin E-CDK3/p35-CDK5 respectively; less potent against cyclin H-CDK7 and cyclin D3-CDK6.
T2381 LY2835219 free base LY2835219 is an effective and specific CDK4/6 inhibitor (IC50: 2/10 nM).
T2440 IC261 IC261 is a novel inhibitor of CK1, triggers the mitotic checkpoint control. The IC50 of IC261 for CK1 was 16 μM and for Cdk5 is 4.5 mM.
T2463 ML141 ML141 is an effective, specific and reversible non-competitive inhibitor of Rho family GTPase cdc42 (IC50: 200 nM).
T2465 PF-562271 PF-562271 is an effective ATP-competitive, reversible inhibitor of FAK(IC50=1.5 nM) and Pyk2 kinase(IC50=13 nM).
T2506 AZD-5438 AZD5438 is an effective inhibitor of CDK, for CDK1(IC50=16 nM),CDK2(IC50=6 nM),CDK9(IC50=20 nM).
T2517 SCH900776 CHK1 Inhibitor MK-8776 is an agent targeting cell cycle checkpoint kinase 1 (Chk1) with potential radiosensitization and chemosensitization activities.
T2615 Flavopiridol Hydrochloride Alvocidib Hydrochloride 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
T2653 SB1317 SB1317 is a potent inhibitor of cyclin dependant kinases (CDKs), Janus kinase 2 (JAK2), and Fms-like tyrosine kinase-3 (FLT3)。
T2670 ML167 ML167 is a highly selective Cdc2-like kinase 4 (Clk4) inhibitor.
T2679 BMS-265246 BMS-265246 is a potent and selective CDK1/2 inhibitor.
T2695 TBB TBB(NSC 231634) is a highly selective, ATP/GTP-competitive inhibitor of casein kinase-2 (CK2).
T2709 TAK901 TAK-901 has been used in trials studying the treatment of Lymphoma, Myelofibrosis, Multiple Myeloma, Myeloid Metaplasia, and Advanced Solid Tumors, among others.
T3111 LY2835219 LY2835219 is a specific and effective inhibitor of CDK4(IC50=2 nM) and CDK6(IC50=10 nM).
T3166 VX-11e VX-11e is a potent, selective, and orally bioavailable ERK(Extracellular Signal-Regulated Kinase) inhibitor; antitumor agent.
T3186 NU2058 NU2058 is a guanine-based CDK inhibitor, also inhibits DNA topoisomerase II ATPase activity.
T3195 CVT-313 CVT-313(NG-26) is a potent, selective, reversible, and ATP-competitive inhibitor.
T3207 Briciclib Briciclib is a small molecule that suppresses cyclin D1 accumulation in Y cells.
T3352 XL413 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 induction of tumor cell apoptosis, and the inhibiti
T3589 NSC23005 Sodium NSC23005 sodium is a novel and effective p18 inhibitor (ED50=5.21 nM) in promoting Hematopoietic stem cells (HSCs) expansion in both murine and human models.
T3590 NSC23005 NSC23005 sodium is a p18INK inhibitor with potently promoted hematopoietic stem cell (HSC) expansion (ED50: 5.21 nM).
T3664 THZ1 THZ1 is a novel selective and potent covalent CDK7 inhibitor.
T3700 SCH900776 S-isomer SCH900776 (S-isomer) is an effective, specific and orally bioavailable inhibitor of checkpoint kinase Chk1 (IC50: 3 nM). It also inhibitors Chk2 (IC50: 1500 nM) and cyclin-dependent kinase CDK2 (IC50: 160 nM).
T4051 LDC4297 LDC4297 is a potent and selective CDK7 inhibitor.
T4227 SB1317(TG-02) hydrochloride (937270-47-8(free base)) SB1317 is an effective inhibitor of CDK2/JAK2/FLT3 (IC50: 13/73/56 nM).
T6049 SNS-032 (BMS-387032) SNS-032 is a selective inhibitor of CDK2 (IC50: 48 nM ) and is 10- and 20-fold selective over CDK1/CDK4. It is also sensitive to CDK7/9 (IC50: 62 nM/4 nM), and no effect on CDK6.
T6052 GW441756 GW 441756 is a specific Tropomyosin-related kinase A (TrkA) inhibitor with an IC50 value of 2 nM.
T6057 URMC-099 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).
T6081 Milciclib (PHA-848125) Milciclib (PHA-848125) is a potent, ATP-competitive CDK inhibitor for CDK2 with IC50 of 45 nM. It is >3-fold more selective for CDK2 than CDK1, 2, 4, 5, and 7. Phase 2.
T6126 JNJ-7706621 JNJ-7706621 is a potent aurora kinase inhibitor, and also inhibits CDK1 and CDK2.
T6139 A-674563 A-674563 is an Akt1 inhibitor with Ki of 11 nM, modest potent to PKA and >30-fold selective for Akt1 over PKC.
T6154 SU11274 SU11274(IC50=10 nM) is a specific Met inhibitor. It shows no significant effects on PGDFRβ, EGFR or Tie2.
T6162 BS-181 hydrochloride BS-181 HCl is a highly selective CDK7 inhibitor with IC50 of 21 nM. It is more than 40-fold selective for CDK7 than CDK1, 2, 4, 5, 6, or 9.
T6167 SU9516 SU9516 is a potent CDK2 inhibitor, with an IC50 of 22 nM, and also has inhibitory effects on CDK1 and CDK4, with IC50s of 40 nM and 200 nM, respectively.
T6169 Indirubin Indirubin is a potent cyclin-dependent kinases and GSK-3β inhibitor with IC50 of about 5 uM and 0.6 uM.
T6177 PF-00562271 PF-562271 (besylate) is a potent, ATP-competitive, reversible inhibitor of FAK with IC50 of 1.5 nM, ~10-fold less potent for Pyk2 than FAK and >100-fold selectivity against other protein kinases, except for some CDKs.
T6199 LEE011 LEE011 is an orally available, and highly specific CDK4/6 inhibitor (IC50:10/39 nM).
T6205 AT7519 AT7519 is a CDK1/2/4/6/9 inhibitor (IC50: 10-210 nM). It is less effective to CDK3 and little active to CDK7.
T6206 PHA-767491 PHA-767491 is a potent ATP-competitive dual Cdc7/CDK9 inhibitor with IC50 of 10 nM and 34 nM, respectively.
T6223 U0126-EtOH U0126-EtOH, a non-ATP competitive specific inhibitor of MEK1/2, with the IC50 for MEK1/2 is 0.07 μM/0.06 μM. The affinity of U0126-EtOH for ΔN3-S218E/S222D MEK is100-fold higher over PD98059.
T6239 Palbociclib (PD-0332991) hydrochloride Palbociclib (PD-0332991) HCl, a greatly selective inhibitor of CDK4/6, with IC50 for CDK4/6 is 11 nM,16 nM, respectively. Palbociclib exhibits no inhibition against CDK1/2/5, EGFR, FGFR, PDGFR, InsR, etc.
T6240 Palbociclib (PD0332991) Isethionate Palbociclib (PD0332991) Isethionate is a highly specific CDK4/6 inhibitor ( IC50: 11/16 nM). It shows no activity against CDK1/2/5, FGFR, EGFR, InsR, PDGFR, etc.
T6255 Bromosporine Bromosporine is a broad spectrum inhibitor for bromodomains for BRD2/4/9 and CECR2 (IC50: 0.41/0.29/0.122/0.017 μM), respectively.
T6312 R547 R547 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.
T6458 CYC116 CYC116 is a potent inhibitor of Aurora A/B with Ki of 8.0 nM/9.2 nM, is less potent to VEGFR2 (Ki of 44 nM), with 50-fold greater potency than CDKs, not active against PKA, Akt/PKB, PKC, no effect on GSK-3α/β, CK2, Plk1 and SAPK2A. Phase 1.
T6563 LDC000067 LDC000067 is a highly specific and selective CDK9 inhibitor with an IC50 value of 44±10 nM.
T6612 NU6027 NU6027 is a potent ATR/CDK inhibitor, inhibits CDK1/2, ATR and DNA-PK with Ki of 2.5 μM/1.3 μM, 0.4 μM and 2.2 μM, enter cells more readily than the 6-aminopurine-based inhibitors.
T6735 XL413-hydrochloride XL-413 is an orally bioavailable cell division cycle 7 homolog (CDC7) kinase inhibitor with potential antineoplastic activity. CDC7 kinase inhibitor BMS-863233 binds to and inhibits the activity of CDC7, which may result in the inhibition of DNA replication and mitosis, the induction of tumor cell a
T6756 AMG 925 AMG 925 is a potent and orally bioavailable dual FLT3/CDK4 inhibitor with IC50 of 1 nM and 3 nM, respectively.
T6786 BI-9564 BI-9564, a specific cell-permeable BRD9 BD inhibitor. The Kd for BRD9 is 5.9 nM, and IC50 for BET family is > 100 μM.
T6837 Flavopiridol (Alvocidib) Flavopiridol (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.
T6866 K03861 K03861 is a type II CDK2 inhibitor with Kd of 50 nM, 18.6 nM, 15.4 nM, and 9.7 nM for CDK2(WT), CDK2(C118L), CDK2(A144C), and CDK2(C118L/A144C), respectlvely.
T6920 ON123300 ON123300 is a potent and multi-targeted kinase inhibitor for CDK4/Ark5/PDGFRβ/FGFR1/RET/Fyn (IC50: 3.9/5/26/26/9.2/11nM).
T6924 P276-00 P276-00 is a novel CDK1, CDK4 and CDK9 inhibitor with IC50 of 79 nM, 63 nM and 20 nM, respectively. Phase 2/3.
T6940 PHA767491 HCl PHA-767491 is an effective ATP-competitive dual Cdc7/CDK9 inhibitor (IC50: 10/34 nM). It has ~20-fold selectivity against GSK3-β and CDK1/2, 50-fold selectivity against CDK5 and MK2, 100-fold selectivity against CHK2 and PLK1.
T4293 THZ531 THZ531 is a covalent inhibitor of both CDK12(IC50=158 nM) and CDK13(IC50=69 nM).
T4417 LDC-4297 HCl (1453834-21-3(free base)) LDC4297 is a potent and selective CDK7 inhibitor with an IC50 of 0.13 nM.
T4321 Indisulam Indisulam is a carbonic anhydrase inibitor and Antitumor CDK inhibitor. Indisulam targets the G1 phase of the cell cycle by depleting cyclin E. inducing p53 and p21, and inhibiting CDK2, causing a blockade in the G1/S transition.
T4444 A-674563 HCl (552325-73-2(free base)) A-674563 is an orally available, ATP-competitive, and reversible inhibitor of Akt (Ki: 11 nM for Akt1) [1]. It exhibits inhibitory activity against PKA and Cdk2 (IC50: 16/46 nM) but is 10- to >1,800-fold selective for Akt1 versus additional kinases in the CMGC, CAMK, and TK families [1].
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