|
T40047 |
CDK6/9-IN-1
|
CDK6/9-IN-1 |
|
|
CDK6/9-IN-1 (compound 66) is a potent dual inhibitor of CDK 6 and CDK 9 that can be administered orally. It exhibits inhibitory activity with IC 50 values of 40.5 nM and 39.5 nM against CDK6 and CDK9, respectively. |
|
T63071 |
CDK6/PIM1-IN-1
|
|
|
|
CDK6/PIM1-IN-1 is a balanced, potent, dual CDK6 (IC50: 39 nM) and PIM1 (IC50: 88 nM) inhibitor. CDK6/PIM1-IN-1 showed inhibitory effect on CDK4 with IC50 value of 3.6 nM. CDK6/PIM1-IN-1 can significantly inhibit the prol... |
|
T18515 |
Palbociclib-propargyl
|
PROTAC CDK6 ligand 1 |
Others
|
|
Palbociclib-propargyl, a PROTAC ligand targeting the protein CDK6, connects to the CRBN ligand through a PEG linker to form PROTAC CP-10. CP-10 exhibits a potent DC50 value of 2.1 nM against CDK6[1]. |
|
T36694 |
XY028-140
|
XY028-140 |
CDK
,
Ligand for E3 Ligase
|
|
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. |
|
T8762 |
SW106065
|
SW-106065 |
Apoptosis
|
|
SW106065 is a novel pharmacologic inducer of apoptosis in MPNST (malignant peripheral nerve sheath tumors).SW106065 is an apoptosis inducer in malignant peripheral nerve sheath tumors (MPNST). It inhibits ATP consumption... |
|
T6920 |
ON123300
|
|
FGFR
,
c-RET
,
JAK
,
CDK
,
PDGFR
,
Src
,
AMPK
|
|
ON123300 is a potent and multi-targeted kinase inhibitor for CDK4/Ark5/PDGFRβ/FGFR1/RET/Fyn (IC50: 3.9/5/26/26/9.2/11 nM). |
|
T10736 |
CDK4/6-IN-2
|
|
CDK
|
|
CDK4/6-IN-2 is a potent CDK4 and CDK6 inhibitor (IC50s: 2.7 and 16 nM). |
|
T39957 |
CDK4/6-IN-6
|
|
CDK
|
|
CDK4/6-IN-6 is a potent CDK4/CDK6 inhibitor with Ki of 0.6 nM and 13.9 nM for CDK4/Cyclin D1 and CDK6/Cyclin D3, respectively. |
|
T3111 |
Abemaciclib methanesulfonate
|
abemaciclib mesylate,LY2835219,LY2835219 mesylate,LY2835219 (methanesulfonate) |
CDK
|
|
Abemaciclib methanesulfonate (LY2835219) is a specific and effective inhibitor of CDK4(IC50=2 nM) and CDK6(IC50=10 nM). |
|
T13202 |
Trilaciclib hydrochloride
|
G1T28 hydrochloride |
CDK
|
|
Trilaciclib hydrochloride (G1T28 hydrochloride) is an inhibitor of CDK4/6 (IC50s: 1 nM and 4 nM for CDK4 and CDK6). |
|
T11345L |
Lerociclib dihydrochloride
|
G1T38 dihydrochloride |
CDK
|
|
Lerociclib dihydrochloride (G1T38 dihydrochloride) is a potent and selective inhibitor of CDK4/CDK6, with IC50s of 2 nM and 1 nM for CDK6/CyclinD3 and CDK4/CyclinD1, respectively. |
|
T1785 |
Palbociclib
|
PD 0332991 |
CDK
|
|
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-ne... |
|
T8463 |
PF-06873600
|
|
CDK
|
|
PF-06873600 is a selective and orally bioavailable cyclin-dependent kinase (CDK) inhibitor(CDK2, CDK4 and CDK6 with Ki of 0.09 nM, 0.13 nM and 0.16 nM, respectively), has potential antineoplastic activity. |
|
T15335 |
FN-1501
|
|
FLT
,
CDK
|
|
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. |
|
T5395 |
BSJ-03-123
|
|
CDK
|
|
BSJ-03-123 is a potent, CDK6-selective small-molecule degrader. |
|
T6837 |
Flavopiridol
|
L868275,Alvocidib,NSC 649890 HCl,HMR-1275 |
Apoptosis
,
HIV Protease
,
CDK
,
Autophagy
|
|
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 foun... |
|
T10220 |
LSN2839567
|
Abemaciclib metabolite M2 |
CDK
|
|
LSN2839567 (Abemaciclib metabolite M2) is the active metabolite of Abemaciclib, a potent CDK4 and CDK6 inhibitor (IC50s: 1-3 nM) with anticancer activity.LSN2839567 inhibits CDK9.LSN2839567 inhibits cell growth and cell ... |
|
T10745 |
CDK9-IN-7
|
|
CDK
|
|
CDK9-IN-7 is a highly selective 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). |
|
T74710 |
YX-2-107
|
|
CDK
|
|
YX-2-107 is a selective and potent CDK6-degrading PROTAC with an IC50 value of 4.4 nM.YX-2-107 inhibits RB phosphorylation and FOXM1 expression in vitro, and inhibits the development of Ph+ ALL in rats.YX-2-107 can be us... |
|
T21720 |
GP-82996
|
Cdk4/6 Inhibitor IV,CINK4 |
CDK
|
|
GP-82996 (CINK4) is a pharmacological inhibitor specifically targeting CDK4/6, exhibiting IC50 values of 1.5 μM for CDK4/cyclin D1, 5.6 μM for CDK6/cyclin D1, and 25 μM for Cdk5/p35. It effectively induces apoptosis in U... |
|
T6049 |
SNS-032
|
SNS032,BMS-387032 |
Apoptosis
,
GSK-3
,
CDK
|
|
SNS-032 (BMS-387032) 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. |
|
T6205 |
AT7519
|
|
Apoptosis
,
GSK-3
,
CDK
|
|
AT7519 is a CDK1/2/4/6/9 inhibitor (IC50: 10-210 nM). It is less effective to CDK3 and little active to CDK7. |
|
T2378 |
RGB-286638 free base
|
|
GSK-3
,
MEK
,
JAK
,
CDK
|
|
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 a... |
|
T1778 |
AT7519 Hydrochloride
|
AT7519 HCl,AT 7519 hydrochloride salt |
Apoptosis
,
GSK-3
,
CDK
|
|
AT7519 Hydrochloride (AT7519 HCl) is a multi-CDK inhibitor for CDK1, 2, 4, 6 and 9. |
|
T2506 |
AZD-5438
|
AZD5438 |
CDK
|
|
AZD-5438 is an effective inhibitor of CDK, for CDK1(IC50=16 nM), CDK2(IC50=6 nM), CDK9(IC50=20 nM). |
|
T6239 |
Palbociclib monohydrochloride
|
PD 0332991 hydrochloride,Palbociclib hydrochloride,Palbociclib (PD-0332991) HCl |
CDK
|
|
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. |
|
T10735 |
CDK4/6/1 Inhibitor
|
Crozbaciclib |
CDK
|
|
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... |
|
T13202L |
Trilaciclib
|
G1T28 |
CDK
|
|
Trilaciclib is an inhibitor of CDK4/6 (IC50s: 1 nM and 4 nM for CDK4 and CDK6, respectively). |
|
T13627 |
CP-10
|
|
CDK
|
|
CP-10 is a PROTAC with highly selective and remarkable CDK6 degradation (DC50: 2.1 nM). It inhibits the proliferation of several hematopoietic cancer cells including multiple myeloma and can degrade mutated and overexpre... |
|
T10737 |
CDK4/6-IN-3
|
|
CDK
|
|
CDK4/6-IN-3 is a brain-penetrant CDK4/CDK6 inhibitor (Kis: <0.3 nM and 2.2 nM) used for the treatment of glioblastoma. It inhibits CDK1 with a Ki of 110 nM. |
|
T12355 |
Palbociclib-d8
|
PD 0332991 D8,Palbociclib D8 |
CDK
|
|
Palbociclib D8 is a deuterium labeled Palbociclib. Palbociclib is a selective and orally active inhibitor of CDK4 and CDK6 (IC50s of 11 and 16 nM, respectively). |
|
T9636 |
Dalpiciclib
|
SHR-6390 |
CDK
|
|
Dalpiciclib (SHR-6390) is a highly selective, orally bioavailable, and comparable potency inhibitor of CDK4 and CKD6 with IC50s of 12.4 nM and 9.9 nM, respectively. Dalpiciclib exerts potent antitumor activity in esophag... |
|
T15732 |
Ribociclib succinate
|
LEE011 succinate |
CDK
|
|
Ribociclib succinate (LEE011 succinate) is a highly specific CDK4/6 inhibitor (IC50: 10 nM and 39 nM, respectively). It also is over 1,000-fold less potent against the cyclin B/CDK1 complex. |
|
T2381 |
Abemaciclib
|
CDK4/6 dual inhibitor,LY2835219 |
CDK
|
|
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. |
|
T39956 |
CDK4/6-IN-5
|
CDK4/6-IN-5 |
|
|
CDK4/6-IN-5 is a highly effective inhibitor of CDK4 and CDK6, with Ki values of 0.2 and 4.4 nM for CDK4/Cyclin D1 and CDK6/Cyclin D3, respectively (WO2019207463A1, example A93). |
|
T22590 |
AT7519 TFA
|
AT7519 trifluoroacetate |
Others
|
|
AT7519 is a kinase inhibitor (IC50: 0.19, 0.044, 0.51, 0.067, 0.66 and 0.018 μM for CDK1/cyclinB, CDK2/CyclinA, CDK2/Cyclin E, CDk4/CyclinD1, CDK6/Cyclin D3, CDk5/p35). |
|
T35477 |
BSJ-Bump
|
|
|
|
Negative control for BSJ-03-123 . Displays binding and no degradation of Cdk6 in vitro.
Brand et al (2019) Homolog-selective degradation as a strategy to probe the function of CDK6 in AML. Cell Chem.Biol. 26 300 PMID:305... |
|
T11345 |
Lerociclib
|
G1T38 |
CDK
|
|
Lerociclib (G1T38) is a potent and selective inhibitor of CDK4/6, with IC50s of 2nM, 1 nM for CDK6/CyclinD3 and CDK4/CyclinD1, respectively. |
|
T35476 |
BSJ-04-132
|
|
|
|
Selective Cdk4 degrader. Degrades Cdk4 in Molt-4 cells, with no effect on Cdk6 levels. Displays cereblon-dependent degradation.
Jiang et al (2019) Development of dual and selective degraders of cyclin-dependent kinases 4... |
|
T67780 |
AM5992
|
CDK4/6-IN-16 |
CDK
|
|
AM5992 (example 195) is a potent CDK4 and CDK6 inhibitor (CDK4, IC50= 0.013 μM). AM5992 can be used for the research of CDK4-mediated disorders. |
|
T78130 |
N-Methyl Palbociclib
|
|
Drug Metabolite
|
|
N-Methyl Palbociclib is an impurity of the orally active selective CDK4 and CDK6 inhibitor Palbociclib (PD 0332991). |
|
T61892 |
CDK4/6-IN-8
|
|
|
|
CDK4/6-IN-8 (Compound 7p) is a selective inhibitor of CDK4 (IC50=5.01 nM) and CDK6 (IC50=3.97 nM). |
|
T17904 |
Pomalidomide-PEG1-C2-N3
|
E3 ligase Ligand-Linker Conjugates 50,Cereblon Ligand-Linker Conjugates 13 |
Others
|
|
Pomalidomide-PEG1-C2-N3 is a compound that has been synthesized as a conjugate of an E3 ligase ligand-linker. This compound incorporates the cereblon ligand based on Pomalidomide and a 1-unit PEG linker, which are common... |
|
T61378 |
Anticancer agent 29
|
|
|
|
Anticancer agent 29 (Compd E/Z-6f) exhibits potent anticancer activity, as indicated by IC50 values of 0.054 μM, 0.127 μM, 0.129 μM, and 0.396 μM for CDK2, CDK1, CDK4, and CDK6, respectively [1]. |
|
TP2133 |
[Ala92]-p16 (84-103)
|
|
|
|
Peptide derived from the tumor suppressor protein p16; inhibits cyclin-dependent kinase-4 (cdk4)/cyclin D1 (IC50 ~ 1.5 μM) and binds to cdk6. |
|
T72507 |
Palbociclib orotate
|
PD 0332991 orotate |
CDK
|
|
Palbociclib (PD 0332991) orotate, an orally active selective inhibitor of CDK4 and CDK6, exhibits IC50 values of 11 and 16 nM, respectively. This compound demonstrates potent anti-proliferative effects and induces cell c... |
|
T64244 |
CDK4/6-IN-10
|
|
|
|
CDK4/6-IN-10 is a selective, potent, orally active inhibitor of CDK4 (IC50: 22 nM) and CDK6 (IC50: 10 nM) with antitumour effects. CDK4/6-IN-10 has potential for studies in multiple myeloma (MM). |
|
T62192 |
CDK4/6-IN-9
|
|
|
|
CDK4/6-IN-9 (compound 10) is a selective inhibitor of CDK4/6, capable of acting on CDK6/cyclin D1 (IC50: 905 nM). CDK4/6-IN-9 has potential research value in multiple myeloma (MM). |
|
T63634 |
Palbociclib dihydrochloride
|
|
|
|
Palbociclib (PD 0332991) dihydrochloride is an orally active, selective inhibitor of CDK4 (IC50: 11 nM) and CDK6 (IC50: 16 nM). Palbociclib dihydrochloride has anti-proliferative activity and cell cycle arrest in HR-posi... |
|
T60328 |
CDK4/6-IN-12
|
|
|
|
CDK4/6-IN-12 is a potent cyclin-dependent kinase 4/6 (CDK4/6) inhibitor. CDK4/6-IN-12 has enzymatic inhibitory activity against CDK4 and CDK6 with IC 50 of 592.3 nM and 3090 nM, respectively. CDK4/6-IN-12 can be used in ... |
