CDK5 Inhibitors

CDK1

CDK2

CDK3

CDK4

CDK5

CDK6

CDK7

CDK8

CDK9

CDK11

CDK12

CDK13

CDK14

CDK16

CDK19

CDC

CLK

CDK5 Specific Inhibitors

Product Name	CDK5	CDK1	CDK2	CDK3	CDK4	CDK6	CDK7	CDK8	CDK9	CDK14	CDK16	CDK5 Selectivity	Purity
Abemaciclib methanesulfonate	Cdk5/p25, IC₅₀: 355 nM CDK5/p35, IC₅₀: 287 nM	CDK1/cyclinB1, IC₅₀: 1627 nM	CDK2/cyclinE, IC₅₀: 504 nM		Cdk4/cyclin D1, IC₅₀: 2 nM	CDK6/cyclinD1, IC₅₀: 10 nM	CDK7/Mat1/cyclinH1, IC₅₀: 3910 nM		CDK9/cyclinT1, IC₅₀: 57 nM			Pan Inhibitor	99.95%
Dinaciclib	CDK5, IC₅₀: 1 nM	CDK1, IC₅₀: 3 nM	CDK2, IC₅₀: 1 nM						CDK9, IC₅₀: 4 nM			Pan Inhibitor	99.73%
Abemaciclib	CDK5/p35, IC₅₀: 287 nM Cdk5/p25, IC₅₀: 355 nM	CDK1/cyclinB1, IC₅₀: 1627 nM	CDK2/cyclinE, IC₅₀: 504 nM		Cdk4/cyclin D1, IC₅₀: 2 nM	CDK6/cyclinD1, IC₅₀: 10 nM	CDK7/Mat1/cyclinH1, IC₅₀: 3910 nM		CDK9/cyclinT1, IC₅₀: 57 nM			Pan Inhibitor	99.69%
Seliciclib	CDK5/p35, IC₅₀: 0.16 μM	cdc2/cyclin B, IC₅₀: 0.65 μM	cdk2/cyclin A, IC₅₀: 0.7 μM Cdk2/cyclin E2, IC₅₀: 0.7 μM									Pan Inhibitor	99.94%
AT7519	CDK5/p35, IC₅₀: 13 nM	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			Pan Inhibitor	98.15%
AZD-5438	cdk5-p25, IC₅₀: 14 nM	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			Pan Inhibitor	99.37%
GSK 3 Inhibitor IX	CDK5/p35, IC₅₀: 80 nM	Cdk1/cyclin B, IC₅₀: 320 nM	cdk2/cyclin A, IC₅₀: 300 nM		Cdk4/cyclin D1, IC₅₀: 10 μM							Pan Inhibitor	99.66%
BS-181	CDK5/p35NCK, IC₅₀: 3 μM	CDK1/cycB, IC₅₀: 8.1 μM	CDK2/Cyc E, IC₅₀: 0.88 μM		CDK4/Cyc D1, IC₅₀: 33 μM	CDK6/cycD1, IC₅₀: 47 μM	CDK7/CycH/MAT1, IC₅₀: 0.021 μM		CDK9/cycT, IC₅₀: 4.2 μM			Pan Inhibitor	99.62%
PHA-767491 hydrochloride	CDK5, IC₅₀: 460 nM	CDK1, IC₅₀: 250 nM	CDK2, IC₅₀: 240 nM						CDK9, IC₅₀: 34 nM			Pan Inhibitor	99.91%
THZ2	CDK5, IC₅₀: 134 nM	CDK1, IC₅₀: 96.9 nM	CDK2, IC₅₀: 222 nM				CDK7, IC₅₀: 13.9 nM	CDK8, IC₅₀: 6830 nM	CDK9, IC₅₀: 194 nM			Pan Inhibitor	99.03%
Purvalanol A	cdk5-p35, IC₅₀: 75 nM	cdc2-cyclin B, IC₅₀: 4 nM	cdk2-cyclin E, IC₅₀: 35 nM cdk2-cyclin A, IC₅₀: 70 nM		cdk4-cyclin D1, IC₅₀: 850 nM							Pan Inhibitor	98.66%
Atuveciclib	CDK5/p35(h), IC₅₀: 1600 nM	CDK1/CycB(h), IC₅₀: 1100 nM	CDK2/CycE(h), IC₅₀: 1000 nM	CDK3/CycE(h), IC₅₀: 890 nM					CDK9/CycT1, IC₅₀: 13 nM CDK9/CycT1(h), IC₅₀: 6 nM			Pan Inhibitor	99.42%
R547	CDK5/p35, IC₅₀: 0.1 nM	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	CDK4/cyclin D, Ki: 1 nM	cdk6/cyclin D3, IC₅₀: 4 nM	CDK7/cyclin H, IC₅₀: 171 nM					Pan Inhibitor	99.66%
PHA-793887	Cdk5/p25, IC₅₀: 5 nM	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			Pan Inhibitor	99.95%
AT7519 Hydrochloride	CDK5/p35, IC₅₀: 13 nM	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			Pan Inhibitor	99.99%
MC180295	cdk5-p35, IC₅₀: 159 nM cdk5-p25, IC₅₀: 186 nM	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	cdk6-cyclin D3, IC₅₀: 712 nM	CDK7-CycH/MAT1, IC₅₀: 555 nM		CDK9- Cyclin T1, IC₅₀: 5 nM			Pan Inhibitor	98.47%
Lerociclib dihydrochloride	CDK5/p35, IC₅₀: 832 nM Cdk5/p25, IC₅₀: 1.2 μM	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	cdk6/cyclin D3, IC₅₀: 2 nM	CDK7/Cyclin H/MAT1, IC₅₀: 2.4 μM		CDK9/Cyclin T, IC₅₀: 28 nM			Pan Inhibitor	98.45%
Purvalanol B	CDK5/p35, IC₅₀: 6 nM	cdc2/cyclin B, IC₅₀: 6 nM cyclin dependent kinase 1-cyclinB, IC₅₀: 6 nM	cdk2/cyclin A, IC₅₀: 6 nM CDK2/cyclinE, IC₅₀: 9 nM		Cdk4/cyclin D1, IC₅₀: 10000 nM							Pan Inhibitor	>97.0%
NG 52	Pho85p, IC₅₀: 2 nM	cdc2-cyclin B, IC₅₀: 0.34 μM										Pan Inhibitor	99.93%
JSH-150	Cdk5/p25, IC₅₀: 4.64 μM	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	Pan Inhibitor	98.36%
(R)-CR8	Cdk5/p25, IC₅₀: 0.11 μM	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			Pan Inhibitor	>98.0%
NU6140	cdk5-p25, IC₅₀: 15 μM	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					Pan Inhibitor	>99.0%
Alsterpaullone	CDK5/p35, IC₅₀: 40 nM	Cdk1/cyclin B, IC₅₀: 35 nM	cdk2/cyclin A, IC₅₀: 15 nM CDK2/Cyc E, IC₅₀: 200 nM									Pan Inhibitor	97.30%
5-Iodo-indirubin-3'-monoxime	Cdk5/p25, IC₅₀: 20 nM	Cdk1/cyclin B, IC₅₀: 25 nM										Pan Inhibitor	99.50%
(R)-CR8 trihydrochloride	Cdk5/p25, IC₅₀: 0.11 μM	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			Pan Inhibitor	99.02%
AT7519 trifluoroacetate	CDK5/p35, IC₅₀: 13 nM	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			Pan Inhibitor	98.16%
PHA-767491	CDK5, IC₅₀: 460 nM	CDK1, IC₅₀: 250 nM	CDK2, IC₅₀: 240 nM						CDK9, IC₅₀: 34 nM			Pan Inhibitor
BS-181 hydrochloride	CDK5/p35NCK, IC₅₀: 3 μM	CDK1/cycB, IC₅₀: 8.1 μM	CDK2/Cyc E, IC₅₀: 0.88 μM		CDK4/Cyc D1, IC₅₀: 33 μM	CDK6/cycD1, IC₅₀: 47 μM	CDK7/CycH/MAT1, IC₅₀: 0.021 μM		CDK9/cycT, IC₅₀: 4.2 μM			Pan Inhibitor
NVP-LCQ195	Cdk5/p25, IC₅₀: 1 nM CDK5/p35, IC₅₀: 1 nM	Cdk1/cyclin B, IC₅₀: 2 nM	cdk2/cyclin A, IC₅₀: 2 nM CDK2/cyclinE, IC₅₀: 5 nM	CDK3/Cyclin E, IC₅₀: 42 nM		cdk6/cyclin D3, IC₅₀: 187 nM	CDK7/Cyclin H/MAT1, IC₅₀: 3564 nM		CDK9/cyclinT1, IC₅₀: 15 nM			Pan Inhibitor	98.99%
Lerociclib	CDK5/p35, IC₅₀: 0.832 μM Cdk5/p25, IC₅₀: 1.2 μM	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	cdk6/cyclin D3, IC₅₀: 2 nM	CDK7/Cyclin H/MAT1, IC₅₀: 2.4 μM		CDK9/Cyclin T, IC₅₀: 28 nM			Pan Inhibitor
PNU112455A hydrochloride	CDK5, Km: 3.2 μM		CDK2, Km: 3.6 μM									Pan Inhibitor
Indirubin-3'-monoxime-5-sulphonic acid	CDK5, IC₅₀: 7 nM	CDK1, IC₅₀: 5 nM										Pan Inhibitor
Indirubin-5-sulfonate	CDK5/p35, IC₅₀: 65 nM	Cdk1/cyclin B, IC₅₀: 55 nM	cdk2/cyclin A, IC₅₀: 35 nM CDK2/cyclinE, IC₅₀: 150 nM		Cdk4/cyclin D1, IC₅₀: 300 nM							Pan Inhibitor

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