CDK

CDK(细胞周期蛋白依赖性激酶)

CDKs (Cyclin-dependent kinases) are serine-threonine 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. CDKs are relatively small proteins, with molecular weights ranging from 34 to 40 kDa, and contain little more than the kinase domain. In fact, yeast cells can proliferate normally when their CDK gene has been replaced with the homologous human gene. By definition, a CDK binds a regulatory protein called a cyclin. Without cyclin, CDK has little kinase activity; only the cyclin-CDK complex is an active kinase.

There are around 20 Cyclin-dependent kinases (CDK1-20) known till date. CDK1, 4 and 5 are involved in cell cycle, and CDK 7, 8, 9 and 11 are associated with transcription.

CDK levels remain relatively constant throughout the cell cycle and most regulation is post-translational. Most knowledge of CDK structure and function is based on CDKs of S. pombe (Cdc2), S. cerevisia (CDC28), and vertebrates (CDC2 and CDK2). The four major mechanisms of CDK regulation are cyclin binding, CAK phosphorylation, regulatory inhibitory phosphorylation, and binding of CDK inhibitory subunits (CKIs).

CDK 相关产品(269)

GC17359 CDK9 inhibitor 2
CAS: 1263369-28-3
纯度: >99.50%
CDK9 inhibitor 2 是一种特殊的细胞周期蛋白依赖性激酶 9 (CDK9) 抑制剂，提取自专利 WO/2012131594A1，化合物 CDKI(8)，在 H929 多发性骨髓瘤 (MM) 细胞系中的 IC50 分别为 5 nM 和 7 nM（72 小时） ) 和 A2058 皮肤细胞系（72 小时）。
GC17400 R547
CAS: 741713-40-6
纯度: >99.50%
A selective Cdk inhibitor
GC17648 Dinaciclib(SCH727965)
CAS: 779353-01-4
纯度: >98.00%
A CDK inhibitor
GC17935 PD 0332991 (Palbociclib) HCl
CAS: 827022-32-2
纯度: >98.00% / >99.00%
PD 0332991 作为 CDK4 和 CDK6 激酶的口服活性强效和高选择性抑制剂，可以在低纳摩尔浓度下阻断 pRb 磷酸化并随后在敏感细胞系中诱导 G1 期停滞。
GC18028 CVT-313
CAS: 199986-75-9
纯度: >99.50%
A Cdk2 inhibitor
GC18117 XL413
CAS: 1169558-38-6
A potent inhibitor of Cdc7
GC18354 Bisindolylmaleimide X (hydrochloride)
CAS: 145317-11-9
纯度: >98.50% / >98.00%
Bisindolylmaleimide X (hydrochloride) 是一种新型的、具有细胞渗透性的蛋白激酶C（PKC）抑制剂。Bisindolylmaleimide X也可抑制细胞周期蛋白依赖性激酶2(CDK2)活性。
GC19067 BGG463
CAS: 890129-26-7
纯度: >98.00%
BGG463 (K03859) 是一种具有口服活性的 II 型 CDK2 抑制剂。
GC19089 CC-671
CAS: 1618658-88-0
纯度: >99.00%
A dual inhibitor of Mps1/TTK and Clk2
GC19096 CDKI-73
CAS: 1421693-22-2
纯度: >99.50%
CDKI-73 (LS-007) 是一种具有口服活性且高效的 CDK9 抑制剂，对 CDK9、CDK1 和 CDK2 的 Ki 值分别为 4 nM、4 nM 和 3 nM。
GC19219 LDC4297
CAS: 1453834-21-3
纯度: >99.00%
A CDK7 inhibitor
GC19233 LY3177833
CAS: 1627696-51-8
纯度: >99.50%
An inhibitor of Cdc7 kinase
GC19267 NU2058
CAS: 161058-83-9
纯度: >99.00%
An inhibitor of Cdk1 and Cdk2
GC19326 Senexin B
CAS: 1449228-40-3
An inhibitor of Cdk8 and Cdk19
GC25593 LY3143921 hydrate
CAS: 1627696-53-0
LY3143921 hydrate is an orally administered ATP-competitive CDC7 inhibitor.
GC25594 LY3405105
CAS: 2326428-25-3
LY3405105 is an orally active CDK7 inhibitor with an IC50 of 92.8 nM. LY3405105 shows potential antineoplastic activity.
GC25996 THZ1 2HCl
CAS: 2095433-94-4
THZ1 is a covalent CDK7 inhibitor which has the unprecedented ability to target a remote cysteine residue located outside of the canonical kinase domain, providing an unanticipated means of achieving selectivity for CDK7.
GC26084 XL413 (BMS-863233)
CAS: 1169562-71-3
XL413 (BMS-863233) is a potent and selective cell division cycle 7 homolog (CDC7) kinase inhibitor with IC50 of 3.4 nM, showing 63-, 12- and 35-fold selectivity over CK2, Pim-1 and pMCM2, respectively. Phase 1/2.
GC30245 CLK1-IN-1
CAS: 2123491-32-5
纯度: >99.00%
CLK1-IN-1是一个有效的、Cdc2-like激酶(CLK1)的选择性抑制剂，其IC50值为2nM。
GC30466 CDK8-IN-3
CAS: 1884500-15-5
CDK8-IN-3是CDK8的抑制剂,来自专利WO2016041618A1，化合物实例1.7。
GC30977 Ca2+ channel agonist 1
CAS: 1402821-24-2
纯度: >99.50%
Ca2+channelagonist1是一种N-型钙离子通道(N-typeCa2+channel)激动剂和Cdk2的抑制剂，EC50分别为14.23μM和3.34μM，对运动神经终端功能障碍有潜在疗效。
GC32429 (-)-BAY-1251152
CAS: 1610358-59-2
纯度: >99.50%
A racemic mixture of (+)-BAY-1251152 and (–)-BAY-1251152
GC32700 CYC065
CAS: 1070790-89-4
纯度: >99.50%
An inhibitor of Cdk2 and Cdk9
GC32717 AZD4573
CAS: 2057509-72-3
纯度: >99.50%
AZD4573 is a potent inhibitor of CDK9 (IC50 of <0.004 μM) with fast-off binding kinetics (t1/2 = 16 min) and high selectivity versus other kinases, including other CDK family kinases.

分类产品列表
货号	产品名称	CAS号	纯度
GC17359	CDK9 inhibitor 2	1263369-28-3	>99.50%
GC17359	CDK9 inhibitor 2 是一种特殊的细胞周期蛋白依赖性激酶 9 (CDK9) 抑制剂，提取自专利 WO/2012131594A1，化合物 CDKI(8)，在 H929 多发性骨髓瘤 (MM) 细胞系中的 IC50 分别为 5 nM 和 7 nM（72 小时） ) 和 A2058 皮肤细胞系（72 小时）。
GC17400	R547	741713-40-6	>99.50%
GC17400	A selective Cdk inhibitor
GC17648	Dinaciclib(SCH727965)	779353-01-4	>98.00%
GC17648	A CDK inhibitor
GC17935	PD 0332991 (Palbociclib) HCl	827022-32-2	>98.00% / >99.00%
GC17935	PD 0332991 作为 CDK4 和 CDK6 激酶的口服活性强效和高选择性抑制剂，可以在低纳摩尔浓度下阻断 pRb 磷酸化并随后在敏感细胞系中诱导 G1 期停滞。
GC18028	CVT-313	199986-75-9	>99.50%
GC18028	A Cdk2 inhibitor
GC18117	XL413	1169558-38-6	-
GC18117	A potent inhibitor of Cdc7
GC18354	Bisindolylmaleimide X (hydrochloride)	145317-11-9	>98.50% / >98.00%
GC18354	Bisindolylmaleimide X (hydrochloride) 是一种新型的、具有细胞渗透性的蛋白激酶C（PKC）抑制剂。Bisindolylmaleimide X也可抑制细胞周期蛋白依赖性激酶2(CDK2)活性。
GC19067	BGG463	890129-26-7	>98.00%
GC19067	BGG463 (K03859) 是一种具有口服活性的 II 型 CDK2 抑制剂。
GC19089	CC-671	1618658-88-0	>99.00%
GC19089	A dual inhibitor of Mps1/TTK and Clk2
GC19096	CDKI-73	1421693-22-2	>99.50%
GC19096	CDKI-73 (LS-007) 是一种具有口服活性且高效的 CDK9 抑制剂，对 CDK9、CDK1 和 CDK2 的 Ki 值分别为 4 nM、4 nM 和 3 nM。
GC19219	LDC4297	1453834-21-3	>99.00%
GC19219	A CDK7 inhibitor
GC19233	LY3177833	1627696-51-8	>99.50%
GC19233	An inhibitor of Cdc7 kinase
GC19267	NU2058	161058-83-9	>99.00%
GC19267	An inhibitor of Cdk1 and Cdk2
GC19326	Senexin B	1449228-40-3	-
GC19326	An inhibitor of Cdk8 and Cdk19
GC25593	LY3143921 hydrate	1627696-53-0	-
GC25593	LY3143921 hydrate is an orally administered ATP-competitive CDC7 inhibitor.
GC25594	LY3405105	2326428-25-3	-
GC25594	LY3405105 is an orally active CDK7 inhibitor with an IC50 of 92.8 nM. LY3405105 shows potential antineoplastic activity.
GC25996	THZ1 2HCl	2095433-94-4	-
GC25996	THZ1 is a covalent CDK7 inhibitor which has the unprecedented ability to target a remote cysteine residue located outside of the canonical kinase domain, providing an unanticipated means of achieving selectivity for CDK7.
GC26084	XL413 (BMS-863233)	1169562-71-3	-
GC26084	XL413 (BMS-863233) is a potent and selective cell division cycle 7 homolog (CDC7) kinase inhibitor with IC50 of 3.4 nM, showing 63-, 12- and 35-fold selectivity over CK2, Pim-1 and pMCM2, respectively. Phase 1/2.
GC30245	CLK1-IN-1	2123491-32-5	>99.00%
GC30245	CLK1-IN-1是一个有效的、Cdc2-like激酶(CLK1)的选择性抑制剂，其IC50值为2nM。
GC30466	CDK8-IN-3	1884500-15-5	-
GC30466	CDK8-IN-3是CDK8的抑制剂,来自专利WO2016041618A1，化合物实例1.7。
GC30977	Ca2+ channel agonist 1	1402821-24-2	>99.50%
GC30977	Ca2+channelagonist1是一种N-型钙离子通道(N-typeCa2+channel)激动剂和Cdk2的抑制剂，EC50分别为14.23μM和3.34μM，对运动神经终端功能障碍有潜在疗效。
GC32429	(-)-BAY-1251152	1610358-59-2	>99.50%
GC32429	A racemic mixture of (+)-BAY-1251152 and (–)-BAY-1251152
GC32700	CYC065	1070790-89-4	>99.50%
GC32700	An inhibitor of Cdk2 and Cdk9
GC32717	AZD4573	2057509-72-3	>99.50%
GC32717	AZD4573 is a potent inhibitor of CDK9 (IC50 of <0.004 μM) with fast-off binding kinetics (t1/2 = 16 min) and high selectivity versus other kinases, including other CDK family kinases.