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cdk4 inhibitor

" in TargetMol Product Catalog
  • Inhibitors & Agonists
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Cdk4 Inhibitor
Cyclin-dependent kinase 4 Inhibitor
T84413546102-60-7
PD 0332991, an unsymmetrical indolocarbazole compound, is cell-permeable and exhibits antiproliferative effects by functioning as a potent, selective, reversible, and ATP-competitive inhibitor of Cdk4/D1 (IC 50 = 76 nM). Although it can inhibit other Cdks, such as Cdk2/E and Cdk1/B, effectiveness requires higher concentrations (IC 50 = 520 nM and 2.1 µM, respectively) and demonstrates minimal activity against CaMKII, PKA, or GSK-3β (IC 50 ≥ 12.4 µM). PD 0332991 efficiently inhibits tumor cell growth in HCT-116 and NCI-H460 cell lines with an IC 50 < 3.0 µM, primarily through blocking Rb phosphorylation and inducing G1 cell cycle arrest.
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8-10 weeks
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CDK4/6/1 Inhibitor
Crozbaciclib
T107352099128-41-1In house
CDK4 6 1 Inhibitor (Crozbaciclib) is a type of CDK4 6 inhibitor (IC50s: 3 and 1 nM). CDK4 6 inhibitor is a class of compounds used for the treatment of some types of hormone receptor positive, HER2-negative breast cancer, which can block the process of breast cancer cell division and reproduction.
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6-8weeks
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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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TargetMol | Inhibitor Hot
Salidroside
Rhodioloside
T271710338-51-9
Salidroside is a bioactive phenolic glycoside compound isolated from Rhodiola rosea and is a prolyl endopeptidase inhibitor. Salidroside can alleviate cachexia symptoms in a tumor cachexia mouse model by activating mTOR signaling and protect dopaminergic neurons by enhancing PINK1 Parkin-mediated mitochondrial autophagy. Salidroside can also inhibit the growth of cancer cells by regulating the CDK4-cyclin D1 pathway to block the G1 phase and or regulating the Cdc2-cyclin B1 pathway to block the G2 phase.
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TargetMol | Inhibitor Hot
Flavopiridol
NSC 649890 HCl, L868275, HMR-1275, Alvocidib
T6837146426-40-6
Flavopiridol (Alvocidib) (Alvocidib) competes with ATP to inhibit CDKs including CDK1, CDK2, CDK4 and CDK6 with IC50 of ~ 40 nM. It is 7.5-fold more selective for CDK1, 2, 4, 6 versus CDK7. Flavopiridol is initially found to inhibit EGFR and PKA. Phase 1 2.
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TargetMol | Inhibitor Hot
Abemaciclib metabolite M20
CDK4 6-IN-4, LSN3106726
T107382138499-06-4In house
Abemaciclib metabolite M20 (CDK4 6-IN-4) is an active metabolite of Abemaciclib. Abemaciclib metabolite M20 is a selective CDK4 6 inhibitor and can be used for researches on the treatment of cancer.
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6-8 weeks
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CDK9-IN-7
T107452369981-71-3In house
CDK9-IN-7 is a highly selective and orally active CDK9 cyclin T inhibitor (IC50: 11 nM), which exhibits more potent over other CDKs (CDK4 cyclinD: 148 nM; CDK6 cyclinD: 145 nM).
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6-8 weeks
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CDK4-IN-1
T20821256963-02-6In house
CDK4 inhibitor is a novel and specific CDK4 Cyclin D1 inhibitor with an IC50 of 10 nM; 1500 and 500 fold than CDK1 Cyclin B (IC50>15 uM) and CDK2 Cyclin A (IC50=5.265 uM) respectively.
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GP-82996
CINK4, Cdk4 6 Inhibitor IV
T21720359886-84-3In house
GP-82996 (CINK4) is a pharmacological inhibitor specifically targeting CDK4 6, exhibiting IC50 values of 1.5 μM for CDK4 cyclin D1, 5.6 μM for CDK6 cyclin D1, and 25 μM for Cdk5 p35. It effectively induces apoptosis in U2OS cancer cells, positioning it as a potential investigational tool in cancer research [1] [2].
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7-10 days
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NU6102
NU-6102, NU 6102
T28218444722-95-6In house
NU6102 is a selective and potent ATP-competitive CDK2 inhibitor with antitumor activity against CDK1 cyclinB, CDK2 cyclinA3, CDK1 CDK2, CDK4, DYRK1A , PDK1, and ROCKII, and it can be used to study rectal cancer.
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7-10 days
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zdld20
T617222762279-02-5In house
ZDLD20 is an orally active and selective CDK4 inhibitor, a β-carboline analog with anti-HCT116 and anticancer activity that inhibits colony formation, inhibits invasion and migration, induces apoptosis, and prevents the G1 phase of the cell cycle.
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6-8 weeks
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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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Ribociclib succinate
LEE011 succinate
T157321374639-75-4
Ribociclib succinate (LEE011 succinate) is a highly specific CDK4 6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and exhibits over 1,000-fold reduced potency against the cyclin B CDK1 complex.
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Palbociclib
PD 0332991
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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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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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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Ribociclib
LEE011
T61991211441-98-3
Ribociclib (LEE011) is an orally available, and highly specific CDK4 6 inhibitor (IC50:10 39 nM).
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Palbociclib monohydrochloride
PD 0332991 hydrochloride, Palbociclib hydrochloride, Palbociclib (PD-0332991) HCl
T6239827022-32-2
Palbociclib monohydrochloride (PD 0332991 hydrochloride) is a selective inhibitor of CDK4 6 (IC50s: 11 16 nM). It exhibits no inhibition against a panel of 36 additional protein kinases.
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Rafoxanide
T709322662-39-1
Rafoxanide as a dual CDK4 6 inhibitor for the treatment of skin cancer. Rafoxanide is a salicylanilide used as an anthelmintic. It is used to treat fluke, hookworm and other infestations.
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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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BMS-265246
BMS265246
T2679582315-72-8
BMS-265246 is a potent and selective CDK1 2 inhibitor. Its chemical name is (4-[R-(2,3-Dihydro-benzo[1,4]dioxin-6-yl)-1H-indol-1-yl]-1H-pyrazolo[3,4-d] pyrimidine-6-amine), and it functions by targeting CDK1 and CDK2 to potentially disrupt cell cycle progression.
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CVT-313
NG26, CVT313, CVT 313, Cdk2 Inhibitor III
T3195199986-75-9
CVT-313 (NG-26) is a potent, selective, reversible, and ATP-competitive inhibitor.
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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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