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Cell Cycle/Checkpoint

Nucleoside Antimetabolite/Analog

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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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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Ribociclib

T61991211441-98-3

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

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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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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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Cdk1/2 Inhibitor III

T14914443798-55-8In house

Cdk1 2 Inhibitor III is a selective inhibitor of Cdk1 2 with an IC50 value of 2.1 μM against CDK1 cyclin B.

$350

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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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Simurosertib

T12642L1330782-76-7

Simurosertib (TAK-931) is a selective and ATP-competitive cell division cycle 7 kinase inhibitor (IC50: <0.3 nM).

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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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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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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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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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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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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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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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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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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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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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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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MBM-55S

T119612083624-07-9In house

MBM-55S is an effective inhibitor of Nek2 with an IC50 of 1 nM. MBM-55S indecus cell cycle arrest and apoptosis thereby inhibiting the proliferation of cancer cells. MBM-55S shows antitumor activities.

$195

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