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Results for "

cdk7/cyclinh

" in TargetMol Product Catalog
  • Inhibitors & Agonists
    35
    TargetMol | Inhibitors_Agonists
  • PROTAC Products
    3
    TargetMol | PROTAC
  • Natural Products
    1
    TargetMol | Natural_Products
pha-793887
PHA793887, PHA 793887
T2113718630-59-2
PHA-793887 has been used in trials studying the treatment of Advanced Metastatic Solid Tumors.
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sns-032
SNS032, BMS-387032
T6049345627-80-7
SNS-032 (BMS-387032) is a selective inhibitor of CDK2 (IC50: 48 nM), exhibiting 10- and 20-fold selectivity over CDK1 and CDK4, respectively. It is also sensitive to CDK7 (IC50: 62 nM) and CDK9 (IC50: 4 nM), with no effect on CDK6.
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Milciclib
PHA-848125
T6081802539-81-7
Milciclib (PHA-848125) (PHA-848125) is a potent, ATP-competitive CDK inhibitor for CDK2 with IC50 of 45 nM. It is >3-fold more selective for CDK2 than CDK1, 2, 4, 5, and 7. Phase 2.
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r547
Ro 4584820
T6312741713-40-6In house
R547 (Ro 4584820) is a potent ATP-competitive inhibitor of CDK1 2 4 with Ki of 2 nM 3 nM 1 nM. It is less potent to CDK7 and GSK3α β, while inactive to other kinases. Phase 1.
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NVP-LCQ195
AT9311, LCQ-195
TQ0068902156-99-4In house
NVP-LCQ195 (LCQ-195) (AT9311) is a potent inhibitor of CDK1, CDK2, CDK3 and CDK5 (IC50: 1-42 nM).
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Abemaciclib methanesulfonate
LY2835219 mesylate, LY2835219 (methanesulfonate), LY2835219, abemaciclib mesylate
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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Abemaciclib
LY2835219, CDK4 6 dual inhibitor
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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AT7519
T6205844442-38-2
AT7519 is a CDK1 2 4 6 9 inhibitor (IC50: 10-210 nM). It is less effective to CDK3 and little active to CDK7.
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Samuraciclib hydrochloride
ICEC0942 hydrochloride, CT7001 hydrochloride
T108981805789-54-1
Samuraciclib hydrochloride (ICEC0942 hydrochloride) is a potent, selective, ATP competitive and oral active CDK7 inhibitor with IC50 of 41 nM. The selectivity of Samuraciclib hydrochloride is 45-, 15-, 230- and 30-fold higher than CDK1, CDK2 (IC50 is 578 nM), CDK5 and CDK9 respectively. Samuraciclib hydrochloride inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 μM. Samuraciclib hydrochloride has anti-tumor effects.
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can508
T8796140651-18-9
CAN508 is a potent ATP-competitive CDK9 cyclin T1 inhibitor with an IC50 of 0.35 μM. It also competitively inhibits Cdk2-cyclin E with respect to ATP, with Ki and IC50 values of 13.3 μM and 20 μM, respectively. CAN508 exhibits a 38-fold selectivity for CDK9 cyclin T over other CDK cyclin complexes. [Antitumor activity.]
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NU6140
T16359444723-13-1
NU6140 is a selective inhibitor of CDK2-cyclin A (IC50, 0.41 μM). It shows 10- to 36-fold selectivity over other CDKs. NU6140 also effectively inhibits Aurora A and Aurora B (IC50s: 67 and 35 nM, respectively). It also enhances the apoptotic effect and has anti-cancer activity.
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CGP60474
T14943164658-13-3
CGP60474 is an inhibitor of VEGFR-2 (IC50 = 84 nM) and an inhibitor of ATP-competitive PKC. CGP60474 is also a highly potent anti-endotoxemic agent and inhibits cyclin-dependent kinase (CDK) potently.
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4-6 weeks
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samuraciclib hydrochloride hydrate
T63650
Samuraciclib (CT7001) hydrochloride hydrate is a potent, selective, ATP-competitive, orally active inhibitor of CDK7 (IC50: 41 nM). It inhibits the growth of breast cancer cell lines (GI50: 0.2-0.3 μM) and exhibits potent antitumor effects.
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10-14 weeks
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ykl-5-124 tfa
T736332748220-93-9
YKL-5-124 TFA, a potent and selective irreversible covalent inhibitor of CDK7, demonstrates IC50 values of 53.5 nM for CDK7 and 9.7 nM for the CDK7 Mat1 CycH complex. It exhibits over 100-fold selectivity for CDK7 over CDK9 and CDK2, while showing no activity against CDK12 and CDK13. This compound effectively induces cell-cycle arrest, inhibits E2F-driven gene expression, and has minimal impact on the phosphorylation status of RNA polymerase II.
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mc180295
(rel)-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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AT7519 Hydrochloride
AT7519 HCl, AT 7519 hydrochloride salt
T1778902135-91-5
AT7519 Hydrochloride (AT7519 HCl) is a multi-CDK inhibitor for CDK1, 2, 4, 6 and 9.
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gfb-12811
GFB12811
T626952775311-17-4
GFB-12811 is an orally active, selective, and potent CDK5 inhibitor, used in the study of autosomal dominant polycystic kidney disease.
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10-14 weeks
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YKL-5-124 TFA (1957203-01-8 free base)
YKL-5-124 TFA
T13367
YKL-5-124 TFA is a potent, selective, irreversible and covalent inhibitor of CDK7 (IC50s of 53.5 nM and 9.7 nM for CDK7 and CDK7 Mat1 CycH, respectively).
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8-10 weeks
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RGB-286638
T73196784210-87-3
RGB-286638 is a multi-target CDK inhibitor that effectively hampers the kinase activity of a range of cyclin-CDK complexes, including cyclin T1-CDK9 (IC50 = 1 nM), cyclin B1-CDK1 (IC50 = 2 nM), cyclin E-CDK2 (IC50 = 3 nM), cyclin D1-CDK4 (IC50 = 4 nM), cyclin E-CDK3 (IC50 = 5 nM), and p35-CDK5 (IC50 = 5 nM). Additionally, it inhibits other kinases such as GSK-3β (IC50 = 3 nM), TAK1 (IC50 = 5 nM), Jak2 (IC50 = 50 nM), and MEK1 (IC50 = 54 nM), showcasing its versatile inhibitory potential.
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10-14 weeks
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ykl-5-124
T224611957203-01-8
YKL-5-124, a potent, selective and covalent CDK7 inhibitor with an IC50 of 9.7 nM, 1300 nM and 3020 nM for CDK7 Mat1 CycH, CDK2 and CDK9 respectively, displays biochemical and cellular selectivity for CDK7 over CDK12 13.
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RGB-286638 free base
T2378784210-88-4
RGB-286638 free base is a novel CDK inhibitor with IC50s of 1 nM 2 nM 3 nM 4 nM 5 nM for cyclin T1-CDK9 cyclin B1-CDK1 cyclin E-CDK2 cyclin D1-CDK4 cyclin E-CDK3 p35-CDK5 respectively; less potent against cyclin H-CDK7 and cyclin D3-CDK6.
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(R)​-​CR8
CR8, (R)-Isomer
T12617L294646-77-8
(R)-CR8 ((R)-Isomer) is a potent and selective CDK inhibitor.
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JSH-150
T84842247481-21-4
JSH-150 is a highly selective CDK9 inhibitor with an IC50 of 1 nM.
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TMX-2138
T2043432488892-07-3
TMX-2138 is a CDKs PROTAC degrader, with IC50 values of 8.7 nM for CDK1 cyclinB, 10.9 nM for CDK2 cyclinA, 7.0 nM for CDK5 p25, and 25.7 nM for CDK9 cyclinT1. It enhances the ubiquitination and degradation of CDKs and is utilized for ovarian cancer research.
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