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Search Results for " CDK4 "

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131

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ライブラリー

カタログ番号	製品名	別名	ターゲット
T10736	CDK4/6-IN-2		CDK
	CDK4/6-IN-2 is a potent CDK4 and CDK6 inhibitor (IC50s: 2.7 and 16 nM).		CDK
T39957	CDK4/6-IN-6		CDK
	CDK4/6-IN-6 is a potent CDK4/CDK6 inhibitor with Ki of 0.6 nM and 13.9 nM for CDK4/Cyclin D1 and CDK6/Cyclin D3, respectively.		CDK
T10735	CDK4/6/1 Inhibitor	Crozbaciclib	CDK
	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...		CDK
T39956	CDK4/6-IN-5	CDK4/6-IN-5
	CDK4/6-IN-5 is a highly effective inhibitor of CDK4 and CDK6, with Ki values of 0.2 and 4.4 nM for CDK4/Cyclin D1 and CDK6/Cyclin D3, respectively (WO2019207463A1, example A93).
T21720	GP-82996	Cdk4/6 Inhibitor IV,CINK4	CDK
	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 U...		CDK
T2381	Abemaciclib	CDK4/6 dual inhibitor,LY2835219	CDK
	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.		CDK
T10738	Abemaciclib metabolite M20	CDK4/6-IN-4,LSN3106726	CDK
	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.		CDK
T2082	CDK4-IN-1		CDK
	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.		CDK
T10737	CDK4/6-IN-3		CDK
	CDK4/6-IN-3 is a brain-penetrant CDK4/CDK6 inhibitor (Kis: <0.3 nM and 2.2 nM) used for the treatment of glioblastoma. It inhibits CDK1 with a Ki of 110 nM.		CDK
T79046	CDK4-IN-2		CDK
	CDK4-IN-2 (A17) is a potent inhibitor of CDK4, exhibiting K i and IC 50 values of less than 10 nM and is utilized in cancer research [1].		CDK
T60328	CDK4/6-IN-12
	CDK4/6-IN-12 is a potent cyclin-dependent kinase 4/6 (CDK4/6) inhibitor. CDK4/6-IN-12 has enzymatic inhibitory activity against CDK4 and CDK6 with IC 50 of 592.3 nM and 3090 nM, respectively. CDK4/6-IN-12 can be used in ...
T62605	CDK4/6-IN-13
	Compounds 10B and 10C, functioning as cdk4/6 inhibitors, demonstrated low nanomolar activity, optimal antiproliferative effects, excellent metabolic properties, and acceptable pharmacokinetics targeting cdk4/6.
T72928	CDK4/6-IN-15
	CDK4/6-IN-15, an orally active and selective inhibitor of CDK4/6, effectively halts the growth of cancer cells by arresting the cell cycle at the G1 phase and inhibiting the phosphorylation of the retinoblastoma tumor su...
T72836	SHP2/CDK4-IN-1
	SHP2/CDK4-IN-1 (compound 10) is a dual inhibitor targeting SHP2 and CDK4, exhibiting oral activity and high potency with IC50 values of 4.3 nM for SHP2 and 18.2 nM for CDK4. It effectively induces G0/G1 arrest, inhibitin...
T61892	CDK4/6-IN-8
	CDK4/6-IN-8 (Compound 7p) is a selective inhibitor of CDK4 (IC50=5.01 nM) and CDK6 (IC50=3.97 nM).
T62192	CDK4/6-IN-9
	CDK4/6-IN-9 (compound 10) is a selective inhibitor of CDK4/6, capable of acting on CDK6/cyclin D1 (IC50: 905 nM). CDK4/6-IN-9 has potential research value in multiple myeloma (MM).
T79112	CDK4/6-IN-17		CDK
	CDK4/6-IN-17 (compound 12) is an orally bioavailable inhibitor of CDK4/6, demonstrating potent activity with IC50 values between 10-100 nM in BE(2) cells. It has shown efficacy in inhibiting tumor growth in the COLO205 x...		CDK
T61738	CDK4/6-IN-7
	CDK4/6-IN-7, a highly potent and selective orally active inhibitor of CDK4/6, demonstrates impressive inhibition activity with IC50 values of 1.58 nM and 4.09 nM respectively. This compound is particularly valuable for b...
T74370	CDK4/6-IN-11
	CDK4/6-IN-11 is a potent PROTAC CDK4/6 degrader.
T63135	FLT3/CDK4-IN-1
	FLT3/CDK4-IN-1 is a highly selective, potent, orally active dual inhibitor of FLT3/CDK4, acting on FLT3 (IC50: 7 nM) and CDK4 (IC50: 11 nM).FLT3/CDK4-IN-1 has good anti-tumour effects in vivo, showing anti-proliferative ...
T64244	CDK4/6-IN-10
	CDK4/6-IN-10 is a selective, potent, orally active inhibitor of CDK4 (IC50: 22 nM) and CDK6 (IC50: 10 nM) with antitumour effects. CDK4/6-IN-10 has potential for studies in multiple myeloma (MM).
T72951	CDK4/6-IN-14
	CDK4/6-IN-14 is a potent, highly selective inhibitor of Cyclin-Dependent Kinases 4 and 6 (CDK4/6), demonstrating inhibition concentrations (IC50s) of 10 nM and 16 nM, respectively. It possesses over 60-fold greater selec...
T67780	AM5992	CDK4/6-IN-16	CDK
	AM5992 (example 195) is a potent CDK4 and CDK6 inhibitor (CDK4, IC50= 0.013 μM). AM5992 can be used for the research of CDK4-mediated disorders.		CDK
T75029	HEMTAC CDK4/6 degrader 1
	HEMTAC CDK4/6 degrader 1 is a PROTAC connected by ligands for HSP90 and CDK4/6 with a K d value of 35.7 μM. HEMTAC CDK4/6 degrader 1 induces CDK4/6 degradation in B16F10 melanoma cells. HEMTAC CDK4/6 degrader 1 arrests c...
T9628	10074-A4		c-Myc
	10074-A4 is a c-Myc binding compound that associates with c-Myc370–409 and behaves like a “ligand cloud” around a “protein cloud”, with distinct features from that of a non-binding ligand.		c-Myc
T36694	XY028-140	XY028-140	CDK , Ligand for E3 Ligase
	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.		CDK , Ligand for E3 Ligase
T8762	SW106065	SW-106065	Apoptosis
	SW106065 is a novel pharmacologic inducer of apoptosis in MPNST (malignant peripheral nerve sheath tumors).SW106065 is an apoptosis inducer in malignant peripheral nerve sheath tumors (MPNST). It inhibits ATP consumption...		Apoptosis
T6920	ON123300		FGFR , c-RET , JAK , CDK , PDGFR , Src , AMPK
	ON123300 is a potent and multi-targeted kinase inhibitor for CDK4/Ark5/PDGFRβ/FGFR1/RET/Fyn (IC50: 3.9/5/26/26/9.2/11 nM).		FGFR , c-RET , JAK , CDK , PDGFR , Src , AMPK
T13202	Trilaciclib hydrochloride	G1T28 hydrochloride	CDK
	Trilaciclib hydrochloride (G1T28 hydrochloride) is an inhibitor of CDK4/6 (IC50s: 1 nM and 4 nM for CDK4 and CDK6).		CDK
T3111	Abemaciclib methanesulfonate	abemaciclib mesylate,LY2835219,LY2835219 mesylate,LY2835219 (methanesulfonate)	CDK
	Abemaciclib methanesulfonate (LY2835219) is a specific and effective inhibitor of CDK4(IC50=2 nM) and CDK6(IC50=10 nM).		CDK
T6756	AMG 925		FLT , CDK
	AMG 925 is a potent and orally bioavailable dual FLT3/CDK4 inhibitor with IC50 of 1 nM and 3 nM, respectively.		FLT , CDK
T23284	Ryuvidine		Histone Demethylase , Histone Methyltransferase , CDK
	Ryuvidine is a dual inhibitor of KDM5A and SETD8, an inducer of the DNA damage response with potential anticancer activity, inhibition of H4K20 methylation, and inhibition of CDK4, and can be used to study breast cancer ...		Histone Demethylase , Histone Methyltransferase , CDK
T6924	Riviciclib hydrochloride	P276-00	Apoptosis , CDK
	Riviciclib hydrochloride (P276-00) is a novel CDK1, CDK4 and CDK9 inhibitor with IC50 of 79 nM, 63 nM and 20 nM, respectively. Phase 2/3.		Apoptosis , CDK
T11345L	Lerociclib dihydrochloride	G1T38 dihydrochloride	CDK
	Lerociclib dihydrochloride (G1T38 dihydrochloride) is a potent and selective inhibitor of CDK4/CDK6, with IC50s of 2 nM and 1 nM for CDK6/CyclinD3 and CDK4/CyclinD1, respectively.		CDK
T1785	Palbociclib	PD 0332991	CDK
	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-ne...		CDK
T15732	Ribociclib succinate	LEE011 succinate	CDK
	Ribociclib succinate (LEE011 succinate) is a highly specific CDK4/6 inhibitor (IC50: 10 nM and 39 nM, respectively). It also is over 1,000-fold less potent against the cyclin B/CDK1 complex.		CDK
T6167	SU9516		Apoptosis , p38 MAPK , CDK , PKC , Autophagy
	SU9516 is a potent CDK2 inhibitor, with an IC50 of 22 nM, and also has inhibitory effects on CDK1 and CDK4, with IC50s of 40 nM and 200 nM, respectively.		Apoptosis , p38 MAPK , CDK , PKC , Autophagy
T6240	Palbociclib Isethionate	Palbociclib (PD0332991) Isethionate,PD 0332991 isethionate	CDK
	Palbociclib Isethionate (PD 0332991 isethionate) is a selective inhibitor of CDK4/6 (IC50s: 11/16 nM). It exhibits no inhibition against a panel of 36 additional protein kinases.		CDK
T15335	FN-1501		FLT , CDK
	FN-1501 is a potent FLT3 and CDK inhibitor (IC50s: 2.47, 0.85, 1.96, and 0.28 nM for CDK2/cyclin A, CDK4/cyclin D1, CDK6/cyclin D1 and FLT3, respectively). FN-1501 also has anticancer activity.		FLT , CDK
T6837	Flavopiridol	L868275,Alvocidib,NSC 649890 HCl,HMR-1275	Apoptosis , HIV Protease , CDK , Autophagy
	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 foun...		Apoptosis , HIV Protease , CDK , Autophagy
T6239	Palbociclib monohydrochloride	PD 0332991 hydrochloride,Palbociclib hydrochloride,Palbociclib (PD-0332991) HCl	CDK
	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.		CDK
T2059	Purvalanol A	NG-60	Apoptosis , CDK , Autophagy
	Purvalanol A (NG-60) is an effective and cell-permeable CDK inhibitor with IC50 of 70/4/35/850 nM for cdk2-cyclin A/B/E, and cdk4-cyclin D1, respectively.		Apoptosis , CDK , Autophagy
T13361	XY028-133		CDK
	XY028-133 is a PROTAC-based CDK4/6 degrader for the study of tumors.		CDK
T8463	PF-06873600		CDK
	PF-06873600 is a selective and orally bioavailable cyclin-dependent kinase (CDK) inhibitor(CDK2, CDK4 and CDK6 with Ki of 0.09 nM, 0.13 nM and 0.16 nM, respectively), has potential antineoplastic activity.		CDK
T28218	NU6102	NU-6102,NU 6102	CDK
	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.		CDK
T6199	Ribociclib	LEE011	VEGFR , CDK
	Ribociclib (LEE011) is an orally available, and highly specific CDK4/6 inhibitor (IC50：10/39 nM).		VEGFR , CDK
T9636	Dalpiciclib	SHR-6390	CDK
	Dalpiciclib (SHR-6390) is a highly selective, orally bioavailable, and comparable potency inhibitor of CDK4 and CKD6 with IC50s of 12.4 nM and 9.9 nM, respectively. Dalpiciclib exerts potent antitumor activity in esophag...		CDK
T10745	CDK9-IN-7		CDK
	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).		CDK
T10220	LSN2839567	Abemaciclib metabolite M2	CDK
	LSN2839567 (Abemaciclib metabolite M2) is the active metabolite of Abemaciclib, a potent CDK4 and CDK6 inhibitor (IC50s: 1-3 nM) with anticancer activity.LSN2839567 inhibits CDK9.LSN2839567 inhibits cell growth and cell ...		CDK
T60098	MSC2504877	3-(4-(2-Hydroxypropan-2-yl)phenyl)-6-methylpyrrolo[1,2-a]pyrazin-1(2H)-one	Others
	MSC2504877 is an inhibitor of tankyrase and enhances the effects of clinical CDK4/6 inhibitors. MSC2504877 suppresses the upregulation of Cyclin D2 and Cyclin E2 caused by palbociclib and enhances the suppression of phos...		Others

Compounds

Synonym: Crozbaciclib

Target: CDK

CDK4/6-IN-5

T39956

Synonym: CDK4/6-IN-5

Target:

GP-82996

T21720

Synonym: Cdk4/6 Inhibitor IV,CINK4

Target: CDK

Abemaciclib

T2381

Synonym: CDK4/6 dual inhibitor,LY2835219

Target: CDK

Abemaciclib metabolite M20

T10738

Synonym: CDK4/6-IN-4,LSN3106726

Synonym: CDK4/6-IN-16

Target: CDK

HEMTAC CDK4/6 degrader 1

Target: CDK, Ligand for E3 Ligase

Target: FGFR, c-RET, JAK, CDK, PDGFR, Src, AMPK

Trilaciclib hydrochloride

T13202

Synonym: G1T28 hydrochloride

Target: CDK

Abemaciclib methanesulfonate

T3111

Synonym: abemaciclib mesylate,LY2835219,LY2835219 mesylate,LY2835219 (methanesulfonate)

Target: Histone Demethylase, Histone Methyltransferase, CDK

Riviciclib hydrochloride

T6924

Synonym: P276-00

Target: Apoptosis, CDK

Lerociclib dihydrochloride

T11345L

Synonym: G1T38 dihydrochloride

Synonym: LEE011 succinate

Target: Apoptosis, p38 MAPK, CDK, PKC, Autophagy

Palbociclib Isethionate

T6240

Synonym: Palbociclib (PD0332991) Isethionate,PD 0332991 isethionate

Synonym: L868275,Alvocidib,NSC 649890 HCl,HMR-1275

Target: Apoptosis, HIV Protease, CDK, Autophagy

Palbociclib monohydrochloride

T6239

Synonym: PD 0332991 hydrochloride,Palbociclib hydrochloride,Palbociclib (PD-0332991) HCl

Target: Apoptosis, CDK, Autophagy

Synonym: NU-6102,NU 6102

Synonym: Abemaciclib metabolite M2

Target: CDK

MSC2504877

T60098

Synonym: 3-(4-(2-Hydroxypropan-2-yl)phenyl)-6-methylpyrrolo[1,2-a]pyrazin-1(2H)-one

Target: Others

カタログ番号	製品名	ターゲット
T16324	Nimbolide	Apoptosis , NF-κB , CDK
	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 ...	Apoptosis , NF-κB , CDK
TN1664	Ganoderic acid H	NF-κB , DNA/RNA Synthesis , CDK
	Ganoderic acid H is a potent antitumour agent, it mediates its biological effects through the inhibition of transcription factors AP-1 and NF-kappaB, resulting in the down-regulation of expression of Cdk4.	NF-κB , DNA/RNA Synthesis , CDK

天然物製品

Nimbolide

T16324

Synonym:

Target: Apoptosis, NF-κB, CDK

Ganoderic acid H

TN1664

Synonym:

Target: NF-κB, DNA/RNA Synthesis, CDK

Recombinant Proteins

Species：

Expression System：

Tag：

カタログ番号	製品名	Species	Expression System
TMPY-04548	CDK4 Protein, Human, Recombinant (GST)	Human	Baculovirus Insect Cells
	CDK4 is a member of the Ser/Thr protein kinase family. It is highly similar to the gene products of S. cerevisiae cdc28 and S. pombe cdc2. It is a catalytic subunit of the protein kinase complex that is important for cel...
TMPH-01169	CDK4 Protein, Human, Recombinant (His)	Human	E. coli
	CDK4 Protein, Human, Recombinant (His) is expressed in E. coli.
TMPY-02495	P19 INK4d Protein, Human, Recombinant (GST)	Human	E. coli
	Cyclin-dependent kinase inhibitor 2D(also known as CDKN2D or p19ink4d), a member of the INK4 family of cyclin-dependent kinase (CDK) inhibitors, negatively regulates the cyclin D-CDK4/6 complexes, which promote G1/S tran...
TMPJ-00972	CDKN1B Protein, Human, Recombinant (His)	Human	E. coli
	Cyclin-Dependent Kinase Inhibitor 1B (CDKN1B) is a Kinesin-related motor protein necessary for mitotic spindle assembly and chromosome segregation. CDKN1B is expressed in all tissues with highest levels observed in skele...
TMPJ-00936	CCND2 Protein, Human, Recombinant (His)	Human	E. coli
	CCND2，also known as G1/S-specific cyclin-D2，is a member of the highly conserved cyclin family. Different cyclins exhibit distinct expression and degradation patterns which contribute to the temporal coordination of each ...
TMPJ-00703	Gankyrin Protein, Human, Recombinant	Human	E. coli
	Gankyrin is a multicatalytic proteinase oncoprotein consists of 7 ankyrin repeats. Gankyrin overexpressed in most hepatocellular carcinomas. Gankyrin is involved in theregulation of the phosphorylation of the retinoblast...
TMPJ-00963	CDKN2C Protein, Human, Recombinant (His)	Human	E. coli
	Cyclin-Dependent Kinase 4 Inhibitor C (CDKN2C) is a member of the INK4 family of cyclin dependent kinase inhibitors. CDKN2C contains 4 ANK repeats and interacts with CDK4 or CDK6. Highest levels of CDKN2C can be found in...
TMPY-03599	RPRD1B Protein, Human, Recombinant (His)	Human	HEK293 Cells
	RPRD1B, together with RPRD1A, can accompany RNAP II from promoter regions to 3'-untranslated regions during transcription in vivo, predominantly interact with phosphorylated RNAP II, and can reduce CTD S5- and S7-phospho...
TMPY-04542	CDK2 Protein, Human, Recombinant (His)	Human	Baculovirus Insect Cells
	CDK2 is a member of the Ser/Thr protein kinase family. This protein kinase is highly similar to the gene products of S. cerevisiae cdc28, and S. pombe cdc2. It is a catalytic subunit of the cyclin-dependent protein kinas...
TMPH-02613	ATF-5 Protein, Mouse, Recombinant (His & Myc)	Mouse	E. coli
	Transcription factor that either stimulates or represses gene transcription through binding of different DNA regulatory elements such as cAMP response element (CRE) (consensus: 5'-GTGACGT[AC][AG]-3'), ATF5-specific respo...
TMPH-01552	IRF1 Protein, Human, Recombinant (GST & His)	Human	Baculovirus Insect Cells
	Transcriptional regulator which displays a remarkable functional diversity in the regulation of cellular responses. Regulates transcription of IFN and IFN-inducible genes, host response to viral and bacterial infections,...

CDK4 Protein, Human, Recombinant (GST)

TMPY-04548

Species: Human

Expression System: Baculovirus Insect Cells

CDK4 Protein, Human, Recombinant (His)

TMPH-01169

Species: Human

Expression System: E. coli

p19 INK4d Protein, Human, Recombinant (GST)

TMPY-02495

Species: Human

Expression System: E. coli

CDKN1B Protein, Human, Recombinant (His)

TMPJ-00972

Species: Human

Expression System: E. coli

CCND2 Protein, Human, Recombinant (His)

TMPJ-00936

Species: Human

Expression System: E. coli

Gankyrin Protein, Human, Recombinant

TMPJ-00703

Species: Human

Expression System: E. coli

CDKN2C Protein, Human, Recombinant (His)

TMPJ-00963

Species: Human

Expression System: E. coli

RPRD1B Protein, Human, Recombinant (His)

TMPY-03599

Species: Human

Expression System: HEK293 Cells

CDK2 Protein, Human, Recombinant (His)

TMPY-04542

Species: Human

Expression System: Baculovirus Insect Cells

ATF-5 Protein, Mouse, Recombinant (His & Myc)

TMPH-02613

Species: Mouse

Expression System: E. coli

IRF1 Protein, Human, Recombinant (GST & His)

TMPH-01552

Species: Human

Expression System: Baculovirus Insect Cells

カタログ番号	製品名
L2191	Anti-Breast Cancer Compound Library		1939 compounds
	A unique collection of 1939 compounds with anti-breast cancer therapeutic activity or targeting breast cancer’s major signaling pathways, can be used for anti-breast cancer drug discovery and mechanism study；

ライブラリー

Anti-Breast Cancer Compound Library

L2191

Compounds: 1939