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Cell Cycle/Checkpoint

Nucleoside Antimetabolite/Analog

Poly(ADP-ribose) Glycohydrolase (PARG)

Serine/threonin kinase

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.

Filter HomeSignaling PathwaysCell Cycle/CheckpointCDK

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

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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.

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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.

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Ribociclib

T61991211441-98-3

Ribociclib (LEE011) is an orally available, and highly specific CDK4 6 inhibitor (IC50:10 39 nM).

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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.

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AZD4573

T104362057509-72-3

AZD4573 is an effective and selective CDK9 inhibitor (IC50: <4 nM). It enables transient target engagement for the treatment of hematologic malignancies.

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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.

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SR-4835

T83252387704-62-1

SR-4835 is a highly selective dual inhibitor of CDK12 and CDK13(CDK12: IC50=99 nM, Kd=98 nM; CDK13: Kd=4.9 nM), which disables triple-negative breast cancer (TNBC) cells

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Palbociclib-d8

T123551628752-83-9

Palbociclib-d8 (PD 0332991 D8) is the 2H-labeled form of Palbociclib. Palbociclib is an orally active CDK inhibitor that inhibits CDK4 and CDK6 (IC50=11 16 nM). Palbociclib has anti-tumor activity and is used in research for estrogen receptor-positive and HER2-negative breast cancer.

$489

35 days

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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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Seliciclib

T2095186692-46-6

Seliciclib (Roscovitine) is a potent inhibitor of Cdk2 cyclin E (IC50=0.1 µM). Seliciclib also inhibits Cdk7 cyclin H, Cdk5 p35 and Cdc2 cyclin B (IC50=0.49 0.16 0.65 µM). Seliciclib has antitumor activity.

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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.

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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.

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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.

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9-Isopropylolomoucine

T23589158982-15-1In house

9-Isopropylolomoucine (N9-Isopropylolomoucine), a cell cycle protein-dependent kinase inhibitor, is a thiopurine.

$350

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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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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.

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XL413 hydrochloride

T67352062200-97-7

XL413 hydrochloride (BMS-863233 Hydrochloride) is a potent, selective and ATP competitive inhibitor of Cdc7, with an IC 50 of 3.4 nM. XL413 hydrochloride also exhibits potent effect with IC 50 s of 215, 42 nM on CK2, PIM1, respectively, and an EC 50 of 118 nM on pMCM.

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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).

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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.

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Roniciclib

T167841223498-69-8

Roniciclib (BAY 1000394) is a potent pan-CDK inhibitor and a novel oral cytotoxic agent. Roniciclib inhibits the activity of cell-cycle CDKs CDK1, CDK2, CDK3, CDK4, and of transcriptional CDKs CDK7 and CDK9 with IC(50) values in the range between 5 and 25 nmol L.

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mc180295

T55332237942-08-2

MC180295 ((rel)-MC180295) is a novel, potent, and highly selective CDK9 inhibitor with an IC50 of 5 nM, demonstrating over 22-fold selectivity compared to other CDKs.

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Cirtuvivint

T396082143917-62-6In house

Cirtuvivint (SM08502) is a potent, orally active CDC-like kinase (CLK) inhibitor useful for the study of arthritis.

$107

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Lerociclib dihydrochloride

T11345L2097938-59-3

Lerociclib dihydrochloride (G1T38 dihydrochloride) is a potent and selective CDK4 CDK6 inhibitor, with IC50 values of 2 nM for CDK6 CyclinD3 and 1 nM for CDK4 CyclinD1.

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