| Product Name |
CDK1 |
CDK2 |
CDK3 |
CDK4 |
CDK5 |
CDK6 |
CDK7 |
CDK8 |
CDK9 |
CDK11 |
CDK12 |
CDK13 |
CDK14 |
CDK16 |
CDK19 |
CDC |
CLK |
Pho85 |
CDK10 |
CDK15 |
CDK17 |
CDK18 |
CDK20 |
PITSLRE |
Purity |
| Palbociclib |
|
|
|
Cdk4/cyclin D3, IC50: 9 nM
Cdk4/cyclin D1, IC50: 11 nM
|
|
Cdk6/cyclin D2, IC50: 16 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.94% |
| Abemaciclib |
CDK1/cyclinB1, IC50: 1627 nM
|
CDK2/cyclinE, IC50: 504 nM
|
|
Cdk4/cyclin D1, IC50: 2 nM
|
CDK5/p35, IC50: 287 nM
Cdk5/p25, IC50: 355 nM
|
CDK6/cyclinD1, IC50: 10 nM
|
CDK7/Mat1/cyclinH1, IC50: 3910 nM
|
|
CDK9/cyclinT1, IC50: 57 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.97% |
| Ro-3306 |
CDK1, Ki: 20 nM
CDK1/cyclinB1, Ki: 35 nM
CDK1/cyclin A, Ki: 110 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.83% |
| Ribociclib |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.94% |
| KI-CDK9d-32 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.99% |
| CGP-74514 |
CDK1/cyclinB1, IC50: 25 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.02% |
| CDK9/EZH2-IN-1 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| Dinaciclib |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.80% |
| Flavopiridol |
|
|
|
CDK4/Cyc D1, IC50: 100 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.73% |
| GSK3326595 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.83% |
| (R)-Roscovitine |
cdc2/cyclin B, IC50: 0.65 μM
|
cdk2/cyclin A, IC50: 0.7 μM
Cdk2/cyclin E2, IC50: 0.7 μM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.53% |
| Palbociclib hydrochloride |
|
|
|
Cdk4/cyclin D3, IC50: 9 nM
Cdk4/cyclin D1, IC50: 11 nM
|
|
Cdk6/cyclin D2, IC50: 16 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.96% |
| THZ1 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.84% |
| Palbociclib monohydrochloride |
|
|
|
Cdk4/cyclin D3, IC50: 9 nM
Cdk4/cyclin D1, IC50: 11 nM
|
|
Cdk6/cyclin D2, IC50: 16 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.98% |
| AZD4573 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.98% |
| Palbociclib isethionate |
|
|
|
Cdk4/cyclin D3, IC50: 9 nM
Cdk4/cyclin D1, IC50: 11 nM
|
|
Cdk6/cyclin D2, IC50: 16 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.95% |
| Abemaciclib methanesulfonate |
CDK1/cyclinB1, IC50: 1627 nM
|
CDK2/cyclinE, IC50: 504 nM
|
|
Cdk4/cyclin D1, IC50: 2 nM
|
Cdk5/p25, IC50: 355 nM
CDK5/p35, IC50: 287 nM
|
CDK6/cyclinD1, IC50: 10 nM
|
CDK7/Mat1/cyclinH1, IC50: 3910 nM
|
|
CDK9/cyclinT1, IC50: 57 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.95% |
| THZ531 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.86% |
| Wogonin |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.92% |
| Kenpaullone |
Cdk1/cyclin B, IC50: 0.4 μM
|
cdk2/cyclin A, IC50: 0.68 μM
CDK2/cyclinE, IC50: 7.5 μM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.20% |
| Tagtociclib hydrate |
|
CDK2/cyclin E1, Ki: 1.16 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.73% |
| SR-4835 |
|
|
|
|
|
|
|
|
|
|
CDK12, IC50: 99 nM
CDK12, Kd: 98 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.73% |
| SNS-032 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.54% |
| SY-5609 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.33% |
| GSK 3 Inhibitor IX |
Cdk1/cyclin B, IC50: 320 nM
|
cdk2/cyclin A, IC50: 300 nM
|
|
Cdk4/cyclin D1, IC50: 10 μM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.73% |
| Toyocamycin |
|
CDK2/cyclinA, IC50: 0.67 μM
|
|
Cdk4/cyclin D3, IC50: 15 μM
|
|
cdk6/cyclin D3, IC50: >10 μM
|
CDK7/Mat1/cyclinH1, IC50: 2.8 μM
|
|
CDK9/cyclinT1, IC50: 79 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.27% |
| hSMG-1 inhibitor 11j |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.82% |
| OTS964 hydrochloride |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.74% |
| NVP-2 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.60% |
| Samuraciclib hydrochloride |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.98% |
| Amantadine |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.90% |
| Simurosertib |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.94% |
| BI-1347 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.84% |
| CPS2 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.33% |
| AT7519 |
Cdk1/cyclin B, IC50: 210 nM
|
cdk2/cyclin A, IC50: 47 nM
|
|
Cdk4/cyclin D1, IC50: 100 nM
|
|
cdk6/cyclin D3, IC50: 170 nM
|
CDK7/Cyclin H/MAT1, IC50: 2400 nM
|
|
CDK9/Cyclin T, IC50: 10 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.69% |
| JNJ-7706621 |
Cdk1/cyclin B, IC50: 9 nM
|
CDK2/cyclinE, IC50: 3 nM
cdk2/cyclin A, IC50: 4 nM
|
CDK3/Cyclin E, IC50: 58 nM
|
Cdk4/cyclin D1, IC50: 253 nM
|
|
CDK6/cyclinD1, IC50: 175 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.39% |
| Enitociclib |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.89% |
| AS2863619 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.94% |
| YKL-5-124 |
|
|
|
|
|
|
CDK7, IC50: 53.5 nM
CDK7/Mat1/CycH, IC50: 9.7 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.53% |
| AZD-5438 |
cdk1-cyclin B1, IC50: 16 nM
|
cdk2-cyclin E, IC50: 6 nM
cdk2-cyclin A, IC50: 45 nM
|
|
cdk4-cyclin D1, IC50: 449 nM
|
|
cdk6-cyclin D3, IC50: 21 nM
|
cdk7-cyclin H, IC50: 821 nM
|
|
cdk9-cyclin T, IC50: 20 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.91% |
| MBQ-167 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.64% |
| Ribociclib hydrochloride |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.95% |
| KB-0742 dihydrochloride |
CDK1/cyclin A, IC50: 2980 nM
|
cdk2/cyclin A, IC50: 397 nM
|
CDK3/Cyclin E, IC50: 1420 nM
|
CDK4/cyclin D, IC50: 3130 nM
|
|
CDK6/cyclinD1, IC50: 3950 nM
|
CDK7/cyclin H, IC50: 1510 nM
|
CDK8/cyclin C, IC50: >10000 nM
|
CDK9/cyclinT1, IC50: 6 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.24% |
| TG003 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
CLK1, IC50: 20 nM
CLK2, IC50: 200 nM
CLK4, IC50: 15 nM
|
|
|
|
|
|
|
|
99.57% |
| BSJ-4-116 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.87% |
| SLK/STK10-IN-1 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.78% |
| CVT-313 |
Cdk1/cyclin B, IC50: 4.2 μM
|
cdk2/cyclin A, IC50: 0.5 μM
|
|
Cdk4/cyclin D1, IC50: 215 μM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.90% |
| Flavopiridol Hydrochloride |
|
|
|
CDK4/Cyc D1, IC50: 100 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.73% |
| hSMG-1 inhibitor 11e |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.94% |
| Fadraciclib |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.78% |
| Ribociclib succinate |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.93% |
| CLK-IN-T3 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
CLK1, IC50: 0.67 nM
CLK2, IC50: 15 nM
CLK3, IC50: 110 nM
|
|
|
|
|
|
|
|
98.63% |
| BTX-A51 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.58% |
| Romaciclib monohydrochloride |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
CDK19/CycC, IC50: 10.4 nM
|
|
|
|
|
|
|
|
|
|
99.29% |
| (R)-CR8 |
Cdk1/cyclin B, IC50: 0.09 μM
|
cdk2/cyclin A, IC50: 0.072 μM
CDK2/cyclinE, IC50: 0.041 μM
|
|
|
|
|
CDK7/cyclin H, IC50: 1.1 μM
|
|
CDK9/Cyclin T, IC50: 0.18 μM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.61% |
| NU6300 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.44% |
| Ebvaciclib |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.98% |
| Nimbolide |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.79% |
| Mevociclib |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.27% |
| NG 52 |
cdc2-cyclin B, IC50: 0.34 μM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.88% |
| CGP60474 |
CDK1-Cyclin B, IC50: 26 nM
|
CDK2/cyclinE, IC50: 3 nM
cdk2/cyclin A, IC50: 4 nM
|
|
CDK4/cyclin D, IC50: 216 nM
|
|
|
CDK7/cyclin H, IC50: 200 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.90% |
| MSC2530818 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.62% |
| PF 477736 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.04% |
| FMF-04-159-2 |
|
CDK2, IC50: 256 nM (in NanoBRET assay)
|
|
|
|
|
|
|
|
|
|
|
CDK14/Cyclin Y, IC50: 39.6 nM (in NanoBRET assay)
|
|
|
|
|
|
|
|
|
|
|
|
99.48% |
| BSJ-04-132 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.07% |
| Tambiciclib |
Cdk1/cyclin B, IC50: 5410 nM
|
cdk2/cyclin A, IC50: 6850 nM
|
CDK3/cyclin E1, IC50: >10000 nM
|
|
|
|
CDK7/Cyclin H/MNAT1, IC50: 3700 nM
|
CDK8/cyclin C, IC50: >10000 nM
|
|
|
|
|
CDK14/Cyclin Y, IC50: 2710 nM
|
CDK16/Cyclin Y, IC50: 195 nM
|
|
|
|
|
|
|
|
|
|
|
99.21% |
| Senexin B |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.09% |
| THZ1 Hydrochloride |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.06% |
| Senexin A |
|
|
|
|
|
|
|
CDK8, Kd: 0.83 μM
CDK8, IC50: 280 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.79% |
| BSJ-03-204 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.76% |
| (E/Z)-Zotiraciclib |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.96% |
| XL413 monohydrochloride |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.65% |
| TL12-186 |
|
cdk2/cyclin A, IC50: 73 nM
|
|
|
|
|
|
|
CDK9/cyclinT1, IC50: 55 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.63% |
| PROTAC CDK2/9 Degrader-1 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.85% |
| T025 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
CLK1, Kd: 4.8 nM
CLK2, Kd: 0.096 nM
CLK3, Kd: 6.5 nM
CLK4, Kd: 0.61 nM
|
|
|
|
|
|
|
|
99.64% |
| AUZ 454 |
|
CDK2(C118L/A144C), Kd: 9.7 nM
CDK2(A144C), Kd: 15.4 nM
CDK2(C118L), Kd: 18.6 nM
CDK2(WT), Kd: 50 nM
CDK2(C118L/A144C-Cyclin B), Kd: 134.1 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.15% |
| XY028-140 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.52% |
| Purvalanol A |
cdc2-cyclin B, IC50: 4 nM
|
cdk2-cyclin E, IC50: 35 nM
cdk2-cyclin A, IC50: 70 nM
|
|
cdk4-cyclin D1, IC50: 850 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.61% |
| BSJ-03-123 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.19% |
| Amantadine hydrochloride |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.0% |
| LDC000067 |
cdk1-cyclin B1, IC50: 5513 nM
|
cdk2-cyclin A, IC50: 2441 nM
|
|
cdk4-cyclin D1, IC50: 9242 nM
|
|
|
|
|
CDK9- Cyclin T1, IC50: 44 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.00% |
| CCT-251921 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.12% |
| BMS-265246 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.59% |
| Rogocekib |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.15% |
| Cucurbitacin E |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.92% |
| SU9516 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.85% |
| Milciclib |
cyclin B/CDK1, IC50: 398 nM
|
cyclin A/CDK2, IC50: 45 nM
cyclin E/CDK2, IC50: 363 nM
|
|
cyclin D1/CDK4, IC50: 160 nM
|
|
|
cyclin H/CDK7, IC50: 150 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.90% |
| R547 |
Cdk1/cyclin B, Ki: 2 nM
Cdk1/cyclin B, IC50: 0.2 nM
|
CDK2/cyclinE, Ki: 3 nM
cdk2/cyclin A, IC50: 0.1 nM
CDK2/cyclinE, IC50: 0.4 nM
|
CDK3/Cyclin E, IC50: 0.8 nM
|
|
|
cdk6/cyclin D3, IC50: 4 nM
|
CDK7/cyclin H, IC50: 171 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.57% |
| Sinigrin |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.97% |
| Atuveciclib |
CDK1/CycB(h), IC50: 1100 nM
|
CDK2/CycE(h), IC50: 1000 nM
|
CDK3/CycE(h), IC50: 890 nM
|
|
CDK5/p35(h), IC50: 1600 nM
|
|
|
|
CDK9/CycT1, IC50: 13 nM
CDK9/CycT1(h), IC50: 6 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.75% |
| Roniciclib |
Cdk1/cyclin B, IC50: 7 nM
|
|
|
CDK4/cyclin D, IC50: 11 nM
|
|
|
CDK7/Cyclin H/MAT1, IC50: 25 nM
|
|
CDK9/cyclinT1, IC50: 5 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.09% |
| PHA-767491 hydrochloride |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.49% |
| Dalpiciclib |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.70% |
| XL413 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.76% |
| XO44 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.38% |
| Thiabendazole |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.94% |
| Narazaciclib |
|
|
|
Cdk4/cyclin D1, IC50: 3.9 nM
|
|
CDK6/cyclinD1, IC50: 9.82 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.66% |
| RGB-286638 |
cyclin B1-CDK1, IC50: 2 nM
|
cyclin E-CDK2, IC50: 3 nM
|
cyclin E-CDK3, IC50: 5 nM
|
cyclin D1-CDK4, IC50: 4 nM
|
|
cyclin D3-CDK6, IC50: 55 nM
|
cyclin H-CDK7, IC50: 44 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.70% |
| Alsterpaullone |
Cdk1/cyclin B, IC50: 35 nM
|
cdk2/cyclin A, IC50: 15 nM
CDK2/Cyc E, IC50: 200 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.85% |
| THZ2 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.03% |
| Trilaciclib hydrochloride |
|
|
|
Cdk4/cyclin D1, IC50: 1 nM
|
|
cdk6/cyclin D3, IC50: 4 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.69% |
| Abemaciclib metabolite M2 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.75% |
| Alisol B 23-acetate |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.65% |
| (R)-CR8 trihydrochloride |
CDK1/cyclinB1, IC50: 0.09 μM
|
cdk2/cyclin A, IC50: 0.072 μM
CDK2/cyclinE, IC50: 0.041 μM
|
|
|
|
|
CDK7/cyclin H, IC50: 1.1 μM
|
|
CDK9/Cyclin T, IC50: 0.18 μM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.37% |
| Asnuciclib |
CDK1, IC50: 8.17 nM
CDK1, Ki: 4 nM
|
CDK2, IC50: 3.27 nM
CDK2, Ki: 3 nM
|
|
|
|
|
CDK7, IC50: 134.26 nM
CDK7, Ki: 91 nM
|
|
CDK9, IC50: 5.78 nM
CDK9, Ki: 4 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.76% |
| Voruciclib |
CDK1/cycB, Ki: 5.4 nM
CDK1/cyc A, Ki: 9.1 nM
|
|
|
|
|
|
|
|
CDK9/cyc T2, Ki: 0.626 nM
CDK9/CycT1, Ki: 1.68 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.77% |
| TC11 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.55% |
| CDK2-IN-4 |
Cdk1/cyclin B, IC50: 86 μM
|
cdk2/cyclin A, IC50: 44 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.85% |
| Romaciclib hydrochloride |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
CDK19/CycC, IC50: 10.4 nM
|
|
|
|
|
|
|
|
|
|
99.98% |
| GFB-12811 |
|
|
|
|
|
|
CDK7/Cyclin H/MAT1, IC50: 718 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.04% |
| Abemaciclib metabolite M18 hydrochloride |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.18% |
| CDK5 inhibitor 20-223 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.62% |
| CLK1-IN-1 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.55% |
| (±)-Enitociclib |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.87% |
| JSH-150 |
Cdk1/cyclin B, IC50: 1.34 μM
|
cdk2/cyclin A, IC50: 2.86 μM
|
|
|
|
|
CDK7/Cyclin H/MNAT1, IC50: 1.72 μM
|
|
CDK9/cyclinT1, IC50: 1 nM
|
|
|
|
CDK14/Cyclin Y, IC50: 1.68 μM
|
CDK16/Cyclin Y, IC50: 292 nM
|
|
|
|
|
|
|
|
|
|
|
98.66% |
| KH-CB19 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
CLK1, IC50: 19.7 nM
CLK3, IC50: 530 nM
|
|
|
|
|
|
|
|
99.31% |
| BS-181 hydrochloride |
|
CDK2/Cyc E, IC50: 0.88 μM
|
|
|
|
|
CDK7/CycH/MAT1, IC50: 0.021 μM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.93% |
| AZ5576 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.86% |
| JH-XI-10-02 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.73% |
| FN-1501 |
|
cdk2/cyclin A, IC50: 2.47 nM
|
|
Cdk4/cyclin D1, IC50: 0.85 nM
|
|
CDK6/cyclinD1, IC50: 1.96 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.72% |
| Lerociclib dihydrochloride |
CDK1/cyclinB1, IC50: 2.4 μM
|
cdk2/cyclin A, IC50: 1.5 μM
CDK2/cyclinE, IC50: 3.6 μM
|
|
Cdk4/cyclin D1, IC50: 1 nM
|
CDK5/p35, IC50: 832 nM
Cdk5/p25, IC50: 1.2 μM
|
cdk6/cyclin D3, IC50: 2 nM
|
CDK7/Cyclin H/MAT1, IC50: 2.4 μM
|
|
CDK9/Cyclin T, IC50: 28 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.51% |
| NU6102 |
Cdk1/cyclin B, IC50: 9.5 nM
|
CDK2/cyclin A3, IC50: 5.4 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.23% |
| KB-0742 |
CDK1/cyclin A, IC50: 2980 nM
|
cdk2/cyclin A, IC50: 397 nM
|
CDK3/Cyclin E, IC50: 1420 nM
|
Cdk4/cyclin D1, IC50: 3130 nM
|
|
CDK6/cyclinD1, IC50: 3950 nM
|
CDK7/cyclin H, IC50: 1510 nM
|
|
CDK9/cyclinT1, IC50: 6 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.38% |
| LY2857785 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.92% |
| PHA-793887 |
Cdk1/cyclin B, IC50: 60 nM
|
cdk2/cyclin A, IC50: 8 nM
CDK2/cyclinE, IC50: 8 nM
|
|
Cdk4/cyclin D1, IC50: 62 nM
|
|
|
CDK7/cyclin H, IC50: 10 nM
|
|
CDK9/cyclinT1, IC50: 138 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.25% |
| MC180295 |
CDK1-Cyclin B, IC50: 138 nM
|
cdk2-cyclin A, IC50: 233 nM
cdk2-cyclin E, IC50: 367 nM
|
CDK3-Cyclin E, IC50: 399 nM
|
CDK4-Cyclin D, IC50: 112 nM
|
cdk5-p35, IC50: 159 nM
cdk5-p25, IC50: 186 nM
|
cdk6-cyclin D3, IC50: 712 nM
|
CDK7-CycH/MAT1, IC50: 555 nM
|
|
CDK9- Cyclin T1, IC50: 5 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.89% |
| CDK12-IN-2 |
|
|
|
|
|
|
CDK7, IC50: >10 μM
CDK7, IC50: >10 μM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.36% |
| Purvalanol B |
cdc2/cyclin B, IC50: 6 nM
|
cdk2/cyclin A, IC50: 6 nM
CDK2/cyclinE, IC50: 9 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CKI-7 free base |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK12-IN-3 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.86% |
| MeBIO |
Cdk1/cyclin B, IC50: 55 μM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.0% |
| Avotaciclib |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.72% |
| PROTAC CDK9 Degrader-1 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.55% |
| Rafutrombopag (tautomerism) |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.33% |
| CP-10 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.41% |
| Bisindolylmaleimide X hydrochloride |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.90% |
| PROTAC CDK12/13 Degrader-1 TFA |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.12% |
| YX-2-107 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.22% |
| CDK2 degrader 1 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.74% |
| Leucettine L41 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
CLK1, IC50: 71 nM
CLK4, IC50: 64 nM
|
|
|
|
|
|
|
|
98.98% |
| XY028-133 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.62% |
| CC-671 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.06% |
| Flavone |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.85% |
| ML167 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
CLK4, IC50: 136 nM
CLK1, IC50: 1522 nM
CLK2, IC50: 1648 nM
|
|
|
|
|
|
|
|
98.62% |
| CDK9-IN-1 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.52% |
| BRD6989 |
|
|
|
|
|
|
|
CDK8, IC50: ~200 nM
recombinant CDK8, IC50: ~0.5 μM
|
|
|
|
|
|
|
recombinant CDK19, IC50: >30 μM
|
|
|
|
|
|
|
|
|
|
99.56% |
| Garcinone C |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.66% |
| CDK5-IN-3 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.49% |
| Samuraciclib hydrochloride dihydrate |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.90% |
| RSS0680 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.03% |
| DS96432529 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.93% |
| CDK12-IN-E9 |
|
cdk2/cyclin A, IC50: 932 nM
|
|
|
|
|
CDK7/Cyclin H/MNAT1, IC50: 1210 nM
|
|
CDK9/cyclinT1, IC50: 23.9 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.71% |
| Riviciclib hydrochloride |
CDK1-Cyclin B, IC50: 0.079 μM
|
cdk2-cyclin A, IC50: 0.224 μM
cdk2-cyclin E, IC50: 2.500 μM
|
|
cdk4-cyclin D1, IC50: 0.063 μM
|
|
cdk6-cyclin D3, IC50: 0.396 μM
|
|
|
CDK9- Cyclin T1, IC50: 0.020 μM
CDK9-cyclin H, IC50: 2.900 μM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.08% |
| Tabersonine |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.14% |
| β-catenin-IN-3 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| Palbociclib-d8 |
|
|
|
Cdk4/cyclin D3, IC50: 9 nM
Cdk4/cyclin D1, IC50: 11 nM
|
|
Cdk6/cyclin D2, IC50: 16 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.84% |
| (-)-Enitociclib |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.85% |
| AMG 925 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.02% |
| LL-K8-22 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.76% |
| GW8510 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.04% |
| CDK9 inhibitor HH1 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.69% |
| Abemaciclib metabolite M20 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| LDC4297 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.14% |
| YJ1206 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| Ipivivint |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.95% |
| K00546 |
Cdk1/cyclin B, IC50: 0.6 nM
|
cdk2/cyclin A, IC50: 0.5 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
CLK1, IC50: 8.9 nM
CLK3, IC50: 29.2 nM
|
|
|
|
|
|
|
|
99.48% |
| (E/Z)-Zotiraciclib hydrochloride |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.90% |
| CDK9-IN-2 |
|
|
|
|
|
|
|
|
CDK9, IC50: 5 nM (H929 multiple myeloma cell line)
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.72% |
| EHT 5372 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
CLK1, IC50: 22.8 nM
CLK2, IC50: 88.8 nM
CLK4, IC50: 59.0 nM
|
|
|
|
|
|
|
|
98.12% |
| Senexin C |
|
|
|
|
|
|
|
CDK8/CycC, IC50: 3.6 nM
CDK8/CycC, Kd: 1.4 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.06% |
| CPD-39 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.06% |
| Olomoucine |
|
cdk2-cyclin A, IC50: 7 μM
cdk2-cyclin E, IC50: 7 μM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.87% |
| CDK-IN-2 |
|
|
|
|
|
|
|
|
CDK9/cyclinT1, IC50: 8 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.27% |
| CDK4/6-IN-15 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.32% |
| CDK2-IN-3 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| LY3177833 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.48% |
| PHA-767491 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.85% |
| YKL-5-124 TFA |
|
|
|
|
|
|
CDK7, IC50: 53.5 nM
CDK7/Mat1/CycH, IC50: 9.7 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.74% |
| BSJ-01-175 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.49% |
| NU6140 |
CDK1-Cyclin B, IC50: 6.6 μM
|
cdk2-cyclin A, IC50: 0.41 μM
|
|
CDK4-Cyclin D, IC50: 5.5 μM
|
|
|
cdk7-cyclin H, IC50: 3.9 μM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.07% |
| Lacto-N-fucopentaose I |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.92% |
| GSK-3 inhibitor 3 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.72% |
| JH-XVI-178 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.87% |
| S6K1-IN-1 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.71% |
| CDK8-IN-13 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.14% |
| CLK1-IN-3 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
CLK1, IC50: 5 nM
CLK2, IC50: 42 nM
CLK4, IC50: 108 nM
|
|
|
|
|
|
|
|
98.54% |
| RGB-286638 free base |
cyclin B1-CDK1, IC50: 2 nM
|
cyclin E-CDK2, IC50: 3 nM
|
cyclin E-CDK3, IC50: 5 nM
|
cyclin D1-CDK4, IC50: 4 nM
|
|
cyclin D3-CDK6, IC50: 55 nM
|
cyclin H-CDK7, IC50: 44 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.87% |
| Longdaysin |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.83% |
| AS2863619 free base |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.87% |
| Dalpiciclib hydrochloride |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.22% |
| CDDD11-8 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.62% |
| CDK7-IN-21 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| AZD5597 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.09% |
| SRX3177 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.59% |
| DB0614 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.80% |
| CDK9-IN-7 |
|
|
|
CDK4/cyclin D, IC50: 148 nM
|
|
CDK6/cyclinD, IC50: 145 nM
|
|
|
CDK9/cyclinT1, IC50: 11 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.05% |
| CDK4/6-IN-2 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.67% |
| CDK2 degrader 3 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.91% |
| BGG463 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.0% |
| Manzamine A hydrochloride |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.66% |
| CDK8-IN-11 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.20% |
| CDK2-IN-30 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.40% |
| Ryuvidine |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.40% |
| Atuveciclib Racemate |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.48% |
| Ribociclib succinate hydrate |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.94% |
| Avotaciclib trihydrochloride |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.60% |
| CDK9-IN-13 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.94% |
| Avotaciclib hydrochloride |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.75% |
| TP-1287 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| DD-03-156 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.90% |
| LDC4297 hydrochloride |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.23% |
| HS-243 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.95% |
| PROTAC CDK12/13 Degrader-1 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.01% |
| TMX-2172 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.38% |
| CDK7-IN-4 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.87% |
| PROTAC CDK4/6 degrader 1 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.88% |
| MU1210 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
CLK1, IC50: 8 nM
CLK2, IC50: 20 nM
CLK4, IC50: 12 nM
|
|
|
|
|
|
|
|
99.50% |
| BSJ-5-63 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.97% |
| Desmethylglycitein |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.98% |
| ZLC491 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.02% |
| NVP-LCQ195 |
Cdk1/cyclin B, IC50: 2 nM
|
cdk2/cyclin A, IC50: 2 nM
CDK2/cyclinE, IC50: 5 nM
|
CDK3/Cyclin E, IC50: 42 nM
|
|
Cdk5/p25, IC50: 1 nM
CDK5/p35, IC50: 1 nM
|
cdk6/cyclin D3, IC50: 187 nM
|
CDK7/Cyclin H/MAT1, IC50: 3564 nM
|
|
CDK9/cyclinT1, IC50: 15 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.81% |
| NU2058 |
|
CDK2, IC50: 17 μM
CDK2, Ki: 12 μM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.66% |
| Butyrolactone I |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.80% |
| CDK9-IN-8 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.65% |
| Samuraciclib hydrochloride hydrate |
|
|
|
|
|
|
CDK7/CycH/MAT1, IC50: 41 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.88% |
| (E/Z)-Zotiraciclib citrate |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.83% |
| CDK1-IN-1 |
CDK1/cycB, IC50: 161.2 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.33% |
| Aristolochic acid D |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.74% |
| FIT-039 |
|
|
|
|
|
|
|
|
CDK9/cyclinT1, IC50: 5.8 μM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.56% |
| CK7 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.72% |
| CDK1-IN-2 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.89% |
| DB1113 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.22% |
| 5-Iodo-indirubin-3'-monoxime |
Cdk1/cyclin B, IC50: 25 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.50% |
| CDK2 degrader 5 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.17% |
| Abemaciclib metabolite M18 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.01% |
| Casein Kinase inhibitor A86 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.26% |
| CPD-10 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| ON-013100 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.66% |
| AT7519 Hydrochloride |
Cdk1/cyclin B, IC50: 210 nM
|
cdk2/cyclin A, IC50: 47 nM
|
|
Cdk4/cyclin D1, IC50: 100 nM
|
|
cdk6/cyclin D3, IC50: 170 nM
|
CDK7/Cyclin H/MAT1, IC50: 2400 nM
|
|
CDK9/Cyclin T, IC50: 10 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.42% |
| Ca2+ channel agonist 1 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.71% |
| NU6027 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.04% |
| HTH-01-091 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.64% |
| CDK8/19-IN-1 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
CDK19/CycC, IC50: 0.99 nM
|
|
|
|
|
|
|
|
|
|
98.03% |
| CDK9-IN-11 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| HEMTAC CDK4/6 degrader 1 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.18% |
| CDK12-IN-5 |
|
CDK2/cyclinE, IC50: 173 μM
|
|
|
|
|
|
|
CDK9/cyclinT1, IC50: 127 μM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.01% |
| THZ1-R |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.06% |
| Isosilybin B |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.32% |
| CDK4 degrader 1 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.50% |
| BS-194 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.36% |
| CGP-82996 |
CDK1/cyclinB, IC50: >100 μM
|
CDK2/cyclinA, IC50: >50 μM
CDK2/cyclin E, IC50: >50 μM
|
|
Cdk4/cyclin D1, IC50: 1.5 μM
CDK4/cyclin D2, IC50: >50 μM
|
|
CDK6/cyclinD1, IC50: 5.6 μM
Cdk6/cyclin D2, IC50: >50 μM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.12% |
| NecroIr1 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.02% |
| CDD-2807 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
CLK4, IC50: 85 nM
CLK2, IC50: 101 nM
CLK1, IC50: 116 nM
|
|
|
|
|
|
|
|
99.52% |
| Cdk5i peptide |
|
|
|
|
Cdk5/p25, Kd: 0.17 μM
CDK5, Kd: 15.72 μM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.83% |
| CDK2-IN-31 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.22% |
| CDK9-IN-12 |
|
|
|
|
|
|
|
|
CDK9/cyclinT1, IC50: 5.41 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.65% |
| (S)-Roscovitine |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.15% |
| Lerociclib |
CDK1/cyclinB1, IC50: 2.4 μM
|
cdk2/cyclin A, IC50: 1.5 μM
CDK2/cyclinE, IC50: 3.6 μM
|
|
Cdk4/cyclin D1, IC50: 1 nM
|
CDK5/p35, IC50: 0.832 μM
Cdk5/p25, IC50: 1.2 μM
|
cdk6/cyclin D3, IC50: 2 nM
|
CDK7/Cyclin H/MAT1, IC50: 2.4 μM
|
|
CDK9/Cyclin T, IC50: 28 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.35% |
| Voruciclib hydrochloride |
CDK1/cycB, Ki: 5.4 nM
CDK1/cyc A, Ki: 9.1 nM
|
|
|
|
|
|
|
|
CDK9/CycT1, Ki: 1.68 nM
CDK9/cyc T2, Ki: 0.626 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.23% |
| Cimpuciclib tosylate |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.65% |
| PROTAC CDK9 degrader-9 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.25% |
| CDK2 degrader 4 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.71% |
| CDK2/4/6-IN-2 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.20% |
| PROTAC CDK9 degrader-2 |
|
|
|
|
|
|
|
|
CDK9, IC50: 17 μM (MCF-7 cells)
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.22% |
| CDK12-IN-6 |
|
CDK2/cyclinE, IC50: >20 μM
|
|
|
|
|
|
|
CDK9/cyclinT1, IC50: >20 μM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.09% |
| Cdk1/2 Inhibitor III |
Cdk1/cyclin B, IC50: 0.6 nM
|
CDK2/cyclinA, IC50: 0.5 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.69% |
| 7BIO |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.20% |
| KH-CB20 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
CLK1, IC50: 16.5 nM
CLK3, IC50: 488 nM
|
|
|
|
|
|
|
|
99.80% |
| ABC1183 |
|
|
|
|
|
|
|
|
CDK9- Cyclin T1, IC50: 321 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.62% |
| PNU-292137 |
CDK1/cyclinB, IC50: 270 nM
|
CDK2/cyclinA, IC50: 37 nM
CDK2/cyclin E, IC50: 92 nM
|
|
CDK4/cyclinD1, IC50: >10000 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.95% |
| CA224 |
|
cdk2-cyclin A, IC50: 521 μM
|
|
cdk4-cyclin D1, IC50: 6.2 μM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.94% |
| CAN508 |
Cdk1/cyclin B, IC50: 44 μM
|
CDK2/cyclinE, IC50: 20 μM
cdk2/cyclin A, IC50: 69 μM
|
|
Cdk4/cyclin D1, IC50: 13.5 μM
|
|
|
CDK7/cyclin H, IC50: 26 μM
|
|
CDK9/cyclinT1, IC50: 0.35 μM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.59% |
| BI-1622 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.97% |
| AT7519 TFA |
Cdk1/cyclin B, IC50: 210 nM
|
cdk2/cyclin A, IC50: 47 nM
|
|
Cdk4/cyclin D1, IC50: 100 nM
|
|
cdk6/cyclin D3, IC50: 170 nM
|
CDK7/Cyclin H/MAT1, IC50: 2400 nM
|
|
CDK9/Cyclin T, IC50: 10 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK8 ligand 1 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.0% |
| CDK1-IN-6 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.96% |
| NSC693868 |
Cdk1/cyclin B, IC50: 600 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.0% |
| NSC 625987 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.01% |
| YKL-1-116 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.67% |
| CLK1/2-IN-1 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
CLK1, IC50: 16 nM
CLK2, IC50: 45 nM
|
|
|
|
|
|
|
|
99.87% |
| CDK4-IN-3 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.07% |
| Vanicoside B |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.82% |
| CDK4/6-IN-9 |
|
|
|
|
|
CDK6/cyclinD1, IC50: 905 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.46% |
| PNU112455A hydrochloride |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.56% |
| CDK9-IN-10 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.09% |
| TMX-2039 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.42% |
| GW297361 |
yeast Cdk1, IC50: 20 nM
human CDK1, IC50: 30 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
yeast Pho85, IC50: 400 nM
|
|
|
|
|
|
|
98.13% |
| (R)-DRF053 dihydrochloride |
CDK1/cyclinB1, IC50: 220 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.30% |
| (R)-(+)-O-Demethylbuchenavianine |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.67% |
| CDK8-IN-1 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.77% |
| CDK2-IN-22 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.64% |
| CDK4/6-IN-12 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.76% |
| CDK1/Cyc B-IN-1 |
CDK1-Cyclin B, IC50: 97 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.47% |
| AG-012986 |
|
|
|
|
|
|
|
|
CDK9/Cyclin T, IC50: 4 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.78% |
| RGB-286147 |
CDK1/cyclinB, IC50: 48 nM
|
|
|
|
|
cdk6/cyclin D3, IC50: 232 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.60% |
| NecroIr2 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.99% |
| CDK2-IN-40 |
|
CDK2/cyclinE, IC50: 10 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.80% |
| GSK-3 inhibitor 4 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.77% |
| Damulin B |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| LA-CB1 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.20% |
| CDK9-IN-14 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.91% |
| CDK6/PIM1-IN-1 hydrochloride |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.38% |
| Samuraciclib |
|
|
|
|
|
|
CDK7/CycH/MAT1, IC50: 41 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK7-IN-1 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.91% |
| (S)-LY3177833 hydrate |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| BS-181 |
|
CDK2/Cyc E, IC50: 0.88 μM
|
|
|
|
|
CDK7/CycH/MAT1, IC50: 0.021 μM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.10% |
| IV-361 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.60% |
| LY3177833 monhydrate |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.76% |
| YJ9069 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| PT-262 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.21% |
| PPA-037 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| HQY1428 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| Bohemine |
|
CDK2/cyclinE, IC50: 4.6 μM
cdk2/cyclin A, IC50: 83 μM
|
|
|
|
|
|
|
CDK9/cyclinT1, IC50: 2.7 μM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.93% |
| (E/Z)-BIO-acetoxime |
CDK1/cyclinB, IC50: 63 μM
|
CDK2/cyclinA, IC50: 4.3 μM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.0% |
| Multi-target kinase inhibitor 2 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.82% |
| Fascaplysin |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK5-IN-1 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.47% |
| Akt1&PKA-IN-1 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK8-IN-12 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.74% |
| ZDLD20 |
|
|
|
CDK4/CycD3, IC50: 6.51 μM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.84% |
| Tambiciclib dimaleate |
CDK1/cyclinB, IC50: 5410 nM
|
CDK2/cyclinA, IC50: 6850 nM
|
CDK3/cyclin E1, IC50: >10,000 nM
|
|
|
|
CDK7/Cyclin H/MNAT1, IC50: 3700 nM
|
CDK8/cyclin C, IC50: >10,000 nM
|
CDK9/cyclinT1, IC50: 1 nM
|
|
|
|
CDK14/Cyclin Y, IC50: 2710 nM
|
CDK16/Cyclin Y, IC50: 195 nM
|
|
|
|
|
|
|
|
|
|
|
|
| CDK6/PIM1-IN-1 |
CDK1/cyclinB, IC50: >10 μM
|
CDK2/cyclinA, IC50: 2.274 μM
|
CDK3/Cyclin E, IC50: >10 μM
|
Cdk4/cyclin D1, IC50: 3.6 nM
|
|
CDK6/cyclinD1, IC50: 39 nM
|
CDK7/Cyclin H/MNAT1, IC50: 393 nM
|
|
CDK9/cyclinT1, IC50: 440 nM
|
|
CDK12/Cyclin K, IC50: >10 μM
|
CDK13/Cyclin K, IC50: >10 μM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| JH-VIII-49 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| DDO-6079 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| AMG 925 (HCl) |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| Akt1&PKA-IN-2 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| Sinigrin hydrate |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.77% |
| Manzamine A |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.2% |
| SEL120-34A |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
CDK19/CycC, IC50: 10.4 nM
|
|
|
|
|
|
|
|
|
|
|
| CDK7-IN-28 |
|
cdk2/cyclin A, IC50: 6224 nM
|
|
|
|
|
CDK7/Cyclin H/MNAT1, IC50: <5 nM
|
|
|
|
|
CDK13/Cyclin K, IC50: 152 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| (R)-CDK2 degrader 6 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.55% |
| Abemaciclib metabolite M20-d8 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
99.26% |
| JA397 |
|
|
|
|
|
|
|
|
|
|
|
|
CDK14/Cyclin Y, EC50: 27.1 nM
|
CDK16/Cyclin Y, EC50: 39.0 nM
|
|
|
|
|
|
|
|
|
|
|
|
| Palbociclib dihydrochloride |
|
|
|
Cdk4/cyclin D3, IC50: 9 nM
Cdk4/cyclin D1, IC50: 11 nM
|
|
Cdk6/cyclin D2, IC50: 16 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| Palbociclib orotate |
|
|
|
Cdk4/cyclin D3, IC50: 9 nM
Cdk4/cyclin D1, IC50: 11 nM
|
|
Cdk6/cyclin D2, IC50: 16 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK1-IN-5 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| Cimpuciclib |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK1-IN-3 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| Rafutrombopag |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| OTS964 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| ZLMT-12 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK7-IN-2 hydrochloride hydrate |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| BS-181 dihydrochloride |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK4/6-IN-3 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| FN-1501-propionic acid |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK9-IN-9 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK7-IN-11 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| HDAC1/2 and CDK2-IN-1 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| Riviciclib |
CDK1-Cyclin B, IC50: 0.079 μM
|
cdk2-cyclin A, IC50: 0.224 μM
cdk2-cyclin E, IC50: 2.540 μM
|
|
cdk4-cyclin D1, IC50: 0.063 μM
|
|
cdk6-cyclin D3, IC50: 0.396 μM
|
|
|
CDK9- Cyclin T1, IC50: 0.020 μM
CDK9-cyclin H, IC50: 2.900 μM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK6/9-IN-1 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| Senexin A hydrochloride |
|
|
|
|
|
|
|
CDK8, IC50: 280 nM
CDK8, Kd: 0.83 μM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| Amantadine sulfate |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK7-IN-30 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK2-IN-41 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK7-IN-6 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK2/4-IN-1 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK7-IN-16 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK8-IN-6 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| Haspin-IN-2 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK4/6-IN-18 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK4/9-IN-1 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| (S)-LY3177833 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK2 degrader 7 |
|
CDK2, DC50: 13 nM (MKN1cells)
CDK2, DC50: 17 nM (TOV21G cells)
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK4/6-IN-23 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CKI-7 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK8-IN-17 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK8/19-IN-3 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK2-IN-12 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| KY19334 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK7-IN-10 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| HDAC1/CDK7-IN-1 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| P-gp/CDK2-IN-1 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK4/6-IN-7 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| Multi-kinase-IN-4 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| Cdc7-IN-15 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| PF-06842874 |
|
|
|
|
|
cdk6/cyclin D3, Ki: 130 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDKI-83 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| Aloisine A |
CDK1/cyclinB, IC50: 0.15 μM
|
CDK2/cyclinA, IC50: 0.12 μM
CDK2/cyclinE, IC50: 0.4 μM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK7-IN-32 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK9-IN-28 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| LZ9 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CLK1/4-IN-1 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
CLK1, IC50: 9.7 nM
CLK4, IC50: 6.6 nM
|
|
|
|
|
|
|
|
|
| M1-20 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CP-07 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| Carbonic anhydrase inhibitor 14 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| PI3Kα-IN-26 |
|
CDK2/CycA2, IC50: 3.96 μM
|
|
|
|
|
|
CDK8/cyclin C, IC50: 137.20 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK4/6-IN-21 maleate |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK4/6-IN-20 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| Palbociclib-C4-Boc |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| Wogonin (Standard) |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK9-IN-37 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| ALK-IN-29 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| G721-0282 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| Multi-target kinase-IN-7 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK2/4/6-IN-1 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| PARP1/CDK12-IN-1 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK5-IN-4 |
|
CDK2, IC50: 6.24 ± 2.8 μM
|
|
|
CDK5, IC50: 9.8 ± 2.29 μM
|
|
|
|
CDK9, IC50: 1.76 ± 0.3 μM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK9 degrader-1 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK9-IN-24 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| TMX-3013 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| XL413 hydrochloride |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| SLM6 |
|
|
|
|
|
|
|
|
CDK9/cyclinT1, IC50: 133 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK2-IN-8 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK9-IN-34 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK9-IN-33 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK9/HDAC1/HDAC3-IN-1 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK5-IN-2 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| GSK3-IN-10 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
CLK1, IC50: 620 nM
CLK4, IC50: 760 nM
CLK2, IC50: 800 nM
|
|
|
|
|
|
|
|
|
| Cdc7-IN-14 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK2-IN-9 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| Cdc7-IN-13 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| TrkA Inhibitor |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK9-IN-19 |
|
|
|
|
|
|
|
|
CDK9/cyclinT1, IC50: 2 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK9-IN-22 |
|
cdk2/cyclin A, IC50: 876.2 nM
|
|
|
|
|
|
|
CDK9/cyclinT1, IC50: 10.4 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| NUAK1-IN-1 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| SHR5428 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK2-IN-20 |
|
CDK2/cyclinE, IC50: 0.219 μM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| USP10-IN-4 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK4/6-IN-14 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK4/6/BRD4-IN-1 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| BLINK11 |
CDK1/Cly Y, IC50: 39.34 nM
|
CDK2/ClyA2, IC50: 83.43 nM
|
|
|
CDK5/p35, IC50: 17.09 nM
Cdk5/p25, IC50: 14.69 nM
|
|
|
|
cdk9-cyclin T, IC50: 83.43 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| IIIM-290 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK4/6/HDAC-IN-1 |
|
|
|
|
|
CDK6, IC50: 13.2 nM
CDK6, IC50: 48.38 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK/HDAC-IN-2 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK8-IN-10 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| ZLHQ-5f |
|
CDK2/CycA2, IC50: 0.145 μM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK9-IN-42 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK9-IN-40 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK4/6-IN-16 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| YY173 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| KDM1/CDK1-IN-1 |
CDK1, IC50: 0.078 ± 2. μM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK2-IN-43 |
|
Cdk2/cyclin E2, IC50: 6 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK2-IN-36 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK12/13-IN-2 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| ARUK2010489 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK2-IN-18 |
|
|
|
Cdk4/cyclin D1, IC50: 46 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK2/9-IN-1 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK7-IN-20 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK9 autophagic degrader 1 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK8-IN-7 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| Carbonic anhydrase inhibitor 33 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK2-IN-47 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK2-IN-7 |
|
CDK2/cyclinE, IC50: 50 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK4/6-IN-21 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| SHP2/CDK4-IN-1 |
|
|
|
CDK4, IC50: 18.2 ± 1.3 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK8-IN-5 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| Anticancer agent 30 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| BMI-1026 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK-IN-14 |
|
CDK2/CycA2, IC50: 0.097 μM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| Cdc7-IN-18 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| P162-0948 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK-TCIP1 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| Cdc7-IN-12 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK11A Human Pre-designed siRNA Set A |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| KB-0742 hydrochloride |
CDK1/cyclin A, IC50: 2980 nM
|
cdk2/cyclin A, IC50: 397 nM
|
CDK3/Cyclin E, IC50: 1420 nM
|
Cdk4/cyclin D1, IC50: 3130 nM
|
|
CDK6/cycD1, IC50: 3950 nM
|
CDK7/cyclin H, IC50: 1510 nM
|
CDK8/cyclin C, IC50: >10000 nM
|
CDK9/cyclinT1, IC50: 6 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| EF-4-177 |
|
CDK2/cyclinE, IC50: 87 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| SZ-015268 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| PROTAC CDK9 degrader-6 |
|
|
|
|
|
|
|
|
CDK942, DC50: 0.03 μM
CDK955, DC50: 0.05 μM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| PROTAC CDK9/CycT1 Degrader-2 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| ARUK2010694 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| VCC972839:01 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CLK1/2-IN-3 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
CLK1, IC50: 1.1 nM
CLK2, IC50: 2.1 nM
|
|
|
|
|
|
|
|
|
| FLT3/ITD-IN-4 |
|
|
|
|
|
|
|
|
|
|
|
|
|
CDK16/Cyclin Y, EC50: 1768 nM
|
|
|
|
|
|
|
|
|
|
|
|
| Multi-kinase-IN-7 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| PSTAIR |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| BLINK15 |
CDK1/Cly Y, IC50: 35.84 nM
|
CDK2/ClyA2, IC50: 44.12 nM
|
|
|
CDK5/p35, IC50: 29.34 nM
Cdk5/p25, IC50: 12.08 nM
|
|
|
|
CDK9/Cyclin T, IC50: 74.63 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK9-IN-41 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
98.84% |
| CDK2-IN-29 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK8-IN-19 |
|
CDK2/CycA2, IC50: 1.13 μM
|
|
|
|
|
|
CDK8/cyclin C, IC50: 25.08 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| Autophagy agonist-1 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| YX0798 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| 3-Methylthienyl-carbonyl-JNJ-7706621 |
CDK1/cyclinB, IC50: 6.4 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK7-IN-8 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| Cdc7-IN-19 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK2/PIM1-IN-1 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| ZLWT-37 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK2-IN-26 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| ZDLD13 |
|
|
|
CDK4/CycD3, IC50: 0.38 μM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK1/2/4-IN-1 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| Antitumor agent-174 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK-IN-12 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CGP-74514 hydrochloride |
CDK1/cyclinB1, IC50: 25 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK8-IN-18 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| Anticancer agent 29 |
CDK1/cyclinB1, IC50: 0.127 μM
|
CDK2/cyclinE, IC50: 0.054 μM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK7/9-IN-1 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK12-IN-7 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK12/13-IN-3 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK19 Probe 1 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK12-IN-4 |
|
CDK2/cyclinE, IC50: >20 μM
|
|
|
|
|
|
|
CDK9/cyclinT1, IC50: >20 μM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| Anticancer agent 264 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| Ulecaciclib |
|
cdk2/cyclin A, Ki: 0.62 μM
|
|
Cdk4/cyclin D1, Ki: 0.2 nM
|
|
|
cdk7-cyclin H, Ki: 0.63 μM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK2-IN-28 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| NUAK1-IN-2 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| PROTAC CDK9 degrader-8 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK7-IN-31 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CGP-74514 dihydrochloride |
CDK1/cyclinB1, IC50: 25 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| PROTAC FLT3/CDKs degrader-1 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK9-IN-32 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK4/6-IN-8 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK12-IN-8 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| Indirubin-3'-monoxime-5-sulphonic acid |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| Multi-kinase-IN-6 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CLZX-205 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK9-IN-23 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| EGFR-IN-45 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK-IN-9 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| LDC3140 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| Aloisine RP106 |
Cdk1/cyclin B, IC50: 0.7 μM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| Indirubin-5-sulfonate |
Cdk1/cyclin B, IC50: 55 nM
|
cdk2/cyclin A, IC50: 35 nM
CDK2/cyclinE, IC50: 150 nM
|
|
Cdk4/cyclin D1, IC50: 300 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| PROTAC CDK9 degrader-5 |
|
|
|
|
|
|
|
|
CDK942, DC50: 0.10 μM
CDK955, DC50: 0.14 μM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| KWZY-11 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK2-IN-42 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK4/6-IN-19 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK-IN-18 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK2-IN-15 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK7-IN-7 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| TMX-2138 |
CDK1/cyclinB, IC50: 8.7 nM
|
CDK2/cyclinA, IC50: 10.9 nM
|
|
CDK4/cyclinD1, IC50: 901 nM
|
|
CDK6/cyclinD1, IC50: 465 nM
|
CDK7/cyclin H, IC50: 286 nM
|
|
CDK9/cyclinT1, IC50: 25.7 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK8-IN-15 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| YJZ5118 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK7-IN-5 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK6/9-IN-2 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK2-IN-45 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| Haspin-IN-1 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK4/6-IN-10 |
|
|
|
|
|
CDK6/cyclinD1, IC50: 10 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK9-IN-36 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK7-IN-29 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK9/PARP-IN-1 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK2-IN-44 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| ARN25499 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK2-IN-14-d3 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK7-IN-27 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| Avotaciclib sulfate |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| FLT3/CDK4-IN-1 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| Isosilybin B (Standard) |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK1-IN-4 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| VEGFR-2-IN-69 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK2-IN-37 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK8/19-IN-2 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
CDK19/CycC, IC50: 2.49 nM
|
|
|
|
|
|
|
|
|
|
|
| Alisol B 23-acetate (Standard) |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| JTK-101 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK2-IN-27 |
CDK1/cyclinB1, IC50: >10-20 nM nM
|
CDK2/cyclin E1, IC50: <10 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| Tabersonine hydrochloride |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| 2-Cyanoethylalsterpaullone |
Cdk1/cyclin B, IC50: 0.23 nM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| Cdk18 Rat Pre-designed siRNA Set A |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| Cdk20 Rat Pre-designed siRNA Set A |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| Cdk15 Rat Pre-designed siRNA Set A |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CCT68127 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| Olomoucine II |
Cdk1/cyclin B, IC50: 7.6 μM
|
CDK2/cyclinE, IC50: 0.1 μM
|
|
CDK4/cyclinD1, IC50: 19.8 μM
|
|
|
CDK7/cyclin H, IC50: 0.45 μM
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| CDK8-IN-16 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
| Cdk10 Mouse Pre-designed siRNA Set A |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|