CDK2 选择性抑制剂

目录号 产品名 产品描述 Selective / Pan IC50 / Ki
S6383 1-NM-PP1

1-NM-PP1 (PP1 Analog II, 1NM-PP1, analogue 9) is a potent inhibitor of Src family kinases with IC50 of 4.3 nM and 3.2 nM for v-Src-as1 and c-Fyn-as1, respectively. 1-NM-PP1 also inhibits CDK2-as1, CAMKII-as1 and c-Abl-as2 with IC50 of 5.0 nM, 8.0 nM and 120 nM, respectively.

Selective CDK2-as1, IC50: 5.0 nM
S8100 K03861

K03861是II型 CDK2 抑制剂,作用于CDK2(WT),CDK2(C118L),CDK2(A144C),和 CDK2(C118L/A144C)的 Kd 分别为 50 nM,18.6 nM,15.4 nM,和 9.7 nM。

Selective CDK2(C118L/A144C), Kd: 9.7 nM; CDK2(A144C), Kd: 15.4 nM; CDK2(C118L), Kd: 18.6 nM; CDK2(WT), Kd: 50 nM
S0273 CDK2-IN-73 (CDK2-IN-4)

CDK2-IN-73 (CDK2-IN-4) is a potent and selective inhibitor of CDK2 with IC50 of 44 nM for CDK2/cyclin A, shows 2,000-fold selectivity over CDK1/cyclin B with IC50 of 86 μM.

Selective Cdk2/cyclin A, IC50: 44 nM
S2670 A-674563

A-674563是一种Akt抑制剂,在无细胞试验中Ki为11 nM,对PKA适度有效,作用于Akt1比作用于PKC选择性高30多倍。

Selective CDK2, Ki: 46 nM
S2735 MK-8776 (SCH 900776)

MK-8776 (SCH 900776)是一种选择性Chk1抑制剂,无细胞试验中IC50为3 nM,比作用于Chk2选择性高500倍。Phase 2。

Selective CDK2, IC50: 0.16 μM
S6537 CVT-313

CVT-313 is a potent CDK2 inhibitor with an IC50 of 0.5 microM in vitro. It has no effect on other, nonrelated ATP-dependent serine/threonine kinases.

Selective CDK2, IC50: 0.5 μM
S2642 1-Naphthyl PP1(1-NA-PP1)

1-Naphthyl PP1(1-NA-PP 1) is a highly selective and potent pan-PKD inhibitor with IC50 of 154.6 nM,133.4 nM and 109.4 nM for PKD1, PKD2 and PKD3, respectively. 1-Naphthyl PP1 is a selective inhibitor of Src family kinases (v-Src, c-Fyn) and the tyrosine kinase c-Abl with IC50 of 1.0 μM, 0.6 μM, 0.6 μM, 18 μM and 22 μM for v-Src, c-Fyn, c-Abl, CDK2 and CAMK II, respectively.

Selective CDK2, IC50: 18 μM
S9742 Indisulam

Indisulam (E7070), a sulfonamide anticancer agent, is a potent carbonic anhydrase (CA) inhibitor that inhibits cytosolic isozymes I and II, and transmembrane, tumor-associated isozyme IX. Indisulam suppresses the expression of cyclin E and phosphorylation of CDK2, both of which are essential for the G1 to S transition.

Selective
S2768 Dinaciclib (SCH727965)

Dinaciclib (SCH727965)是一种新型有效的CDK抑制剂,作用于CDK2CDK5CDK1CDK9,无细胞试验中IC50分别为1 nM,1 nM,3 nM和4 nM。它也会阻断胸甘(dThd) DNA整合。Phase 3。

Pan CDK2, IC50: 1 nM
S2688 R547

R547是一种有效的,ATP竞争性CDK1/2/4抑制剂,Ki为2 nM/3 nM/1 nM,对CDK7和GSK3α/β作用效果稍弱,而抑制其他激酶活性。Phase 1。

Pan CDK2/CyclinE, Ki: 3 nM
S1249 JNJ-7706621

JNJ-7706621是一种泛CDK抑制剂,对CDK1/2抑制作用最强,无细胞试验中IC50为9 nM/4 nM,作用于CDK1/2比作用于CDK3/4/6选择性高6倍以上。也能有效抑制Aurora A/B,对Plk1和Wee1没有抑制活性。

Pan CDK2/CyclinE, IC50: 3 nM; CDK2/CyclinA, IC50: 4 nM
S7773 CDKI-73

CDKI-73 (LS-007) is a potent CDK inhibitor in vitro with IC50 of 8.17 nM, 3.27 nM, 8.18 nM, and 5.78 nM for CDK1, CDK2, CDK4, and CDK9, respectively. CDKI-73 induces apoptosis in cancer cells. CDKI-73 is an orally bioavailable and highly efficacious CDK9 inhibitor against acute myeloid leukemia.

Pan CDK2, IC50: 3.27 nM
S7371 Fadraciclib (CYC065)

Fadraciclib (CYC065) is a novel, orally available ATP-competitive inhibitor of CDK2/CDK9 kinases with IC50 of 5 nM and 26 nM, respectively.

Pan CDK2, IC50: 5 nM
S0500 Purvalanol B

Purvalanol B (NG-95) is an inhibitor of cyclin-dependent kinase with IC50 of 6 nM, 6 nM, 9 nM, > 10,000 nM and 6 nM for cdc2/cyclin B, cdk2/cyclin A, cdk2/cyclin E, cdk4/cyclin D1 and cdk5-p35, respectively.

Pan CDK2-Cyclin E, IC50: 9 nM; CDK2-Cyclin A, IC50: 6 nM
S2621 AZD5438

AZD5438是一种有效的CDK1/2/9抑制剂,无细胞试验中IC50为16 nM/6 nM/20 nM。对CDK5/6作用效果稍弱,对GSK3β也有抑制作用。Phase 1。

Pan CDK2, IC50: 6 nM
S1487 PHA-793887

PHA-793887是一种新型有效的CDK2CDK5CDK7抑制剂,IC50分别为8 nM, 5 nM 和10 nM,作用于CDK2, 5,和7比作用于CDK1, 4,和9选择性高6倍以上。Phase 1。

Pan CDK2/CyclinE, IC50: 8 nM; CDK2/CyclinA, IC50: 8 nM
S2014 BMS-265246

BMS-265246是一种有效的选择性CDK1/2抑制剂,无细胞试验中IC50为6 nM/9 nM。作用于CDK1/2 比作用于CDK4选择性高25倍。

Pan CDK2/CyclinE, IC50: 9 nM
S0354 Alsterpaullone

Alsterpaullone is a potent inhibitor of CDK with IC50 of 35 nM, 15 nM, 200 nM and 40 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E and CDK5/p35, respectively. Alsterpaullone competes with ATP for binding to GSK-3alpha/GSK-3beta with IC50 of both 4 nM. Alsterpaullone has antitumor activity and possesses potential for the treatment of neurodegenerative and proliferative disorders.

Pan CDK2/cyclin E, IC50: 200 nM; CDK2/cyclin A, IC50: 15 nM
S7636 SU9516

SU9516是一种3位取代的吲哚酮类CDK抑制剂,对CDK2,CDK1,和CDK4的IC50分别为22 nM,40 nM,和200 nM。

Pan CDK2, IC50: 22 nM
S7357 PF-562271 HCl

PF-562271 HCl是PF-562271的盐酸盐形式,是一种强效的ATP竞争性的可逆的抑制剂,作用于FAKIC50为1.5 nM。相比较FAK,对Pyk2的效果少了大约十倍,除了CDKs类的蛋白酶,PF-562271 HCl的选择性相比其他蛋白酶大大约100倍。

Pan CDK2/CyclinE, IC50: 30 nM
S2890 PF-562271

PF-562271是一种有效的,ATP竞争性的,可逆的FAK抑制剂,无细胞试验中IC50为1.5 nM,作用于FAK比作用于Pyk2选择性高10倍左右,比作用于其他蛋白激酶(除了一些CDKs)选择性高100倍以上。

Pan CDK2/CyclinE, IC50: 30 nM
S2672 PF-00562271 Besylate

PF-00562271是PF-562271的苯磺酸盐,是一种有效的,ATP竞争性,可逆的FAK抑制剂,IC50为1.5 nM,作用于Pyk2比作用于FAK效果低10倍左右,比作用于其他蛋白激酶(除了一些CDKs)选择性高100倍以上。Phase 1。

Pan CDK2/CyclinE, IC50: 30 nM
S7793 Purvalanol A

Purvalanol A 是一种有效的,细胞渗透性 CDK 抑制剂,对cdc2-cyclin B,cdk2-cyclin A,cdk2-cyclin E,和 cdk4-cyclin D1的 IC50 分别为 4 nM,70 nM,35 nM,和 850 nM。

Pan CDK2/CyclinE, IC50: 35 nM; CDK2/CyclinA, IC50: 70 nM
S1145 SNS-032 (BMS-387032)

SNS-032 (BMS-387032)最初被描述为选择性CDK2抑制剂,无细胞试验中IC50为48 nM,比作用于CDK1/CDK4选择性高10和20倍。它也对CDK7/9敏感,IC50为62 nM/4 nM,对CDK6几乎没有抑制效果。 Phase 1。

Pan CDK2/CyclinE, IC50: 48 nM; CDK2/CyclinA, IC50: 38 nM
S1230 Flavopiridol (L86-8275)

Flavopiridol (Alvocidib)与ATP竞争性抑制CDKs,包括CDK1CDK2CDK4CDK6CDK9IC50范围为20-100 nM。作用于CDK1, 2, 4, 6,9比作用于CDK7更具有选择性。Flavopiridol最初被发现能抑制EGFR和PKA。Phase 1/2。

Pan CDK2, IC50: 40 nM
S2679 Flavopiridol (L86-8275) HCl

Flavopiridol HCl与ATP竞争性抑制CDKs,作用于CDK1CDK2CDK4CDK6,无细胞试验中IC50为~40 nM。作用于CDK1/2/4/6比作用于CDK7选择性高7.5倍。Flavopiridol最初被发现可抑制EGFR和PKA。Phase 1/2。

Pan CDK2, IC50: 40 nM
S2751 Milciclib (PHA-848125)

Milciclib (PHA-848125)是一种有效的,ATP竞争性CDK抑制剂,作用于CDK2,IC50为45 nM,作用于CDK2比作用于CDK1, 2, 4, 5和7选择性高3倍以上。Phase 2。

Pan CDK2/CyclinE, IC50: 363 nM; CDK2/CyclinA, IC50: 45 nM
S7808 AT7519 HCl

AT7519 HCl是一种多重CDK抑制剂,作用于CDK1,2,4,6 和 9,无细胞试验中IC50为10-210 nM。它对CDK3作用较弱,而对CDK7几乎没有活性。Phase 2。

Pan CDK2/CyclinA, IC50: 47 nM
S1524 AT7519

AT7519是多种CDK抑制剂,作用于CDK1, 2, 4, 6和9时,IC50为10-210 nM,对CDK3作用效果稍弱,对CDK7几乎没有抑制活性。Phase 2。

Pan CDK2/CyclinA, IC50: 47 nM
S8058 Riviciclib hydrochloride (P276-00)

P276-00是一种新型的CDK1CDK4CDK9抑制剂,IC50分别为79 nM, 63 nM和20 nM。Phase 2/3。

Pan CDK2/CyclinA, IC50: 224 nM; CDK2/CyclinE, IC50: 2.54 μM
S8809 MC180295

MC180295 ((rel)-MC180295) is a novel potent and selective CDK9 inhibitor with an IC50 of 5 nM and is at least 22-fold more selective for CDK9 over other CDKs.

Pan CDK2-Cyclin E, IC50: 367 nM; CDK2-Cyclin A, IC50: 233 nM
S2742 PHA-767491

PHA-767491是一种有效的,ATP竞争性的,双重Cdc7/CDK9抑制剂,无细胞试验中IC50分别为10 nM和34 nM,比作用于CDK1/2和GSK3-β选择性高20倍左右,比作用于MK2和CDK5选择性高50倍,比作用于PLK1和CHK2选择性高100倍。

Pan CDK2, IC50: 240 nM
S2009 Indirubin-3'-monoxime

Indirubin-3'-monoxime (Indirubin-3'-oxime) is a selective CDK inhibitor with IC50 of 0.18 μM, 0.44 μM, 0.25 μM, 3.33 μM, 0.065 μM for CDK1-cyclinB, CDK2-cyclinA, CDK2-cyclinE, CDK4-cyclinD1, CDK5-p35,respectively. Indirubin-3'-monoxime is a direct and selective 5-lipoxygenase inhibitor with IC50 of 7.8-10 µM.

Pan CDK2-cyclinE, IC50: 0.25 μM; CDK2-cyclinA, IC50: 0.44 μM
S7198 BIO

BIO是一种特异性的GSK-3抑制剂,无细胞试验中作用于GSK-3α/β的IC50为5 nM,比作用于CDK5选择性高16倍以上,也是一种泛JAK抑制剂。

Pan CDK2/CyclinA, IC50: 0.30 μM
S8722 Samuraciclib (ICEC0942)

Samuraciclib (ICEC0942, CT7001) is a new, orally bioavailable CDK7 inhibitor with an IC50 of 40nM. The IC50 values for CDK1, CDK2, CDK5 and CDK9 were 45-, 15-, 230- and 30-fold higher. ICEC0942 (CT7001) promotes cell cycle arrest and apoptosis.

Pan CDK2, IC50: 620 nM
S7917 Kenpaullone

Kenpaullone是CDKs的ATP竞争性抑制剂, 它同样也抑制GSK3β,IC50为0.23 μM。

Pan CDK2/CyclinE, IC50: 7.5μM; CDK2/CyclinA, IC50: 0.68μM
S1153 Roscovitine (CYC202)

Roscovitine (Seliciclib,CYC202)是一种有效的,选择性CDK抑制剂,作用于Cdc2CDK2CDK5时,无细胞试验中IC50分别为0.65 μM,0.7 μM和0.16 μM,对CDK4/6几乎没有作用。Phase 2。

Pan CDK2/CyclinE, IC50: 0.7 μM; CDK2/CyclinA, IC50: 0.7 μM
S7114 NU6027

NU6027是一种有效的ATR/CDK抑制剂,抑制CDK1/2ATRDNA-PK时,Ki分别为2.5 μM/1.3 μM, 0.4 μM和 2.2 μM ,进入细胞时比6-氨基嘌呤类抑制剂更容易。

Pan CDK2, Ki: 1.3 μM
S7461 LDC000067

LDC000067 是高度选择性CDK9抑制剂,IC50为44 nM,比作用于CDK2/1/4/6/7的选择性分别高55/125/210/ >227/ >227倍。

Pan CDK2, IC50: 2.441 μM
S6531 Bohemine

Bohemine is a CDK inhibitor with IC50s of 4.6, 83, and 2.7 μM for Cdk2/cyclin E, Cdk2/cyclin A, and Cdk9/cyclin T1, respectively.

Pan Cdk2/cyclin A, IC50: 83 μM; Cdk2/cyclin E, IC50: 4.6 μM
S5316 NU2058

NU2058 (O(6)-Cyclohexylmethylguanine) is an inhibitor of CDK2 with IC50 value of 17 μM in an isolated enzyme assay. It also potentiates melphalan (DMF 2.3), and monohydroxymelphalan (1.7), but not temozolomide or ionising radiation.

Pan CDK2, IC50: 17 μM
S3238 Resibufogenin

Resibufogenin (Bufogenin, Recibufogenin), a component of huachansu with anticancer effect, triggers necroptosis through upregulating receptor-interacting protein kinase 3 (RIP3) and phosphorylating mixed lineage kinase domain-like protein at Ser358. Resibufogenin exerts cytotoxic effect by inducing reactive oxygen species (ROS) accumulation. Resibufogenin induces apoptosis and caspase-3 and caspase-8 activity. Resibufogenin increases Bax/Bcl-2 exp

Pan