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CDK4 Inhibitors

" in MedChemExpress (MCE) Product Catalog:

By Targets:	AMPK (1) Apoptosis (17) Autophagy (5) Bcl-2 Family (1) c-Met/HGFR (1) Casein Kinase (1) Caspase (1) CDK (100) COX (1) Drug Metabolite (2) EGFR (1) Epigenetic Reader Domain (1) ERK (1) Estrogen Receptor/ERR (1) FGFR (1) FLT3 (4) Fungal (1) Glutathione Peroxidase (1) GSK-3 (5) HDAC (1) HIV (2) Isotope-Labeled Compounds (1) JAK (2) Ligands for Target Protein for PROTAC (3) MEK (2) NF-κB (1) p38 MAPK (1) PDGFR (1) Phosphatase (1) PI3K (2) Pim (1) PKC (1) PROTACs (1) Raf (1) SHP2 (1) VEGFR (1)
By Research Areas:	Cancer (104) Infection (1) Inflammation/Immunology (2)
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107

Inhibitors & Agonists

Natural
Products

Isotope-Labeled Compounds

Click Chemistry

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-115904

FLT3/CDK4-IN-1	CDK FLT3	Cancer
FLT3/CDK4-IN-1 is a potent, high selective and orally active *FLT3/CDK4* dual inhibitor (IC₅₀=11 and 7 nM for FLT3 and CDK4, respectively). FLT3/CDK4-IN-1 has antiproliferative activities against certain cancer cells. FLT3/CDK4-IN-1 has good antitumor effect in vivo .

HY-153088

CDK4/6-IN-16	CDK	Cancer
CDK4/6-IN-16 (example 195) is a potent *CDK4* and CDK6 inhibitor, with an IC₅₀ of 0.013 μM for *CDK4. CDK4/6-IN-16 can be used for the research of CDK4*-mediated disorders, such as cancer .

HY-126244

CDK4/6-IN-3	CDK	Cancer
CDK4/6-IN-3 is a brain-penetrant *CDK4/CDK6* inhibitor with K_is of <0.3 nM and 2.2 nM, respectively. CDK4/6-IN-3 inhibits CDK1 with a K_i of 110 nM. CDK4/6-IN-3 can be used for the treatment of glioblastoma .

HY-146213

CDK4/6-IN-12	CDK	Cancer
CDK4/6-IN-12 is a potent cyclin-dependent kinase 4/6 (CDK4/6) inhibitor. CDK4/6-IN-12 has enzymatic inhibitory activity for CDK4 and CDK6 with IC₅₀ of 592.3 nM and 3090 nM, respectively. CDK4/6-IN-12 can be used for the research of cancer .

HY-153443

CDK4-IN-2

CDK Cancer

CDK4-IN-2 (A17) is a CDK4 inhibitor, with K_i and IC₅₀ values of <10 nM. Used in cancer research .

CDK4-IN-2	CDK	Cancer
CDK4-IN-2 (A17) is a *CDK4* inhibitor, with K_i and IC₅₀ values of <10 nM. Used in cancer research .

HY-103380

NSC 625987 1 Publications Verification	CDK	Cancer
NSC 625987 is a specific and high-affinity *CDK4* inhibitor with an IC₅₀ of 0.2 μM for CDK4:cyclin D1. NSC 625987 shows >500-fold selectivity for CDK4 over CDK2 .

HY-112418

CDK4/6-IN-18

CDK Cancer

CDK4/6-IN-18 (Example 2BrIC) is a selective CDK4/6 inhibitor. CDK4/6-IN-18 inhibits ionizing radiation (IR)-induced DNA damage in cells .

CDK4/6-IN-18	CDK	Cancer
CDK4/6-IN-18 (Example 2BrIC) is a selective *CDK4/6* inhibitor. CDK4/6-IN-18 inhibits ionizing radiation (IR)-induced DNA damage in cells .

HY-115993

CDK4/6-IN-10	CDK Apoptosis	Cancer
CDK4/6-IN-10 is a potent, selective and orally active *CDK4* and CDK6 inhibitor with IC₅₀s of 22 nM and 10 nM, respectively. CDK4/6-IN-10 shows antitumor activity. CDK4/6-IN-10 has the potential for the research of Multiple myeloma (MM) .

HY-112280

Crozbaciclib

CDK4/6/1 Inhibitor
CDK Cancer

Crozbaciclib (CDK4/6/1 Inhibitor) is a CDK4/6 inhibitor with IC₅₀s of 3 and 1 nM, respectively.

Crozbaciclib CDK4/6/1 Inhibitor	CDK	Cancer
Crozbaciclib (CDK4/6/1 Inhibitor) is a *CDK4/6* inhibitor with IC₅₀s of 3 and 1 nM, respectively.

HY-139450

PF-07220060 CDK4/6-IN-6	CDK	Cancer
PF-07220060 (CDK4/6-IN-6; example A94) is a potent *CDK4/CDK6* inhibitor with a K_i of 0.6 nM and 13.9 nM for CDK4/Cyclin D1 and CDK6/Cyclin D3, respectively .

HY-16297A

Abemaciclib

70+ Cited Publications

LY2835219
CDK Cancer

Abemaciclib (LY2835219) is a selective CDK4/6 inhibitor with IC₅₀ values of 2 nM and 10 nM for CDK4 and CDK6, respectively.

Abemaciclib 70+ Cited Publications LY2835219	CDK	Cancer
Abemaciclib (LY2835219) is a selective *CDK4/6* inhibitor with IC₅₀ values of 2 nM and 10 nM for CDK4 and CDK6, respectively.

HY-114339

CDK4/6-IN-2	CDK	Cancer
CDK4/6-IN-2 is a potent *CDK4* and CDK6 inhibitor extracted from patent US20180000819A1, Compound 1, has IC₅₀s of 2.7 and 16 nM for CDK4 and CDK6, respectively .

HY-153704

CDK4/6-IN-17	CDK	Cancer
CDK4/6-IN-17 (compound 12) is an orally active *CDK4/6* inhibitor with IC₅₀ ranging of 10-100 nM in BE(2) cells. CDK4/6-IN-17 inhibits tumor growth in COLO205 xenograft model .

HY-139449

CDK4/6-IN-5	CDK	Cancer
CDK4/6-IN-5 is a potent *CDK4* and CDK6 inhibitor with K_is of 0.2 and 4.4 nM for CDK4/Cyclin D1 and CDK6/Cyclin D3, respectively . (from patent WO2019207463A1 example A93).

HY-143257

CDK4/6-IN-7	CDK	Cancer
CDK4/6-IN-7 is a potent, selective and orally active *CDK4/6* inhibitor, with IC₅₀s of 1.58 and 4.09 nM, respectively. CDK4/6-IN-7 can be used for the research of breast cancer .

HY-150609

SHP2/CDK4-IN-1	SHP2 Phosphatase CDK	Cancer
SHP2/CDK4-IN-1 (compound 10) is an orally active and potent SHP2 and *CDK4* dual inhibitor, with IC₅₀ values of 4.3 and 18.2 nM, respectively. SHP2/CDK4-IN-1 effectively induces G0/G1 arrest to prevent the proliferation of TNBC cell lines. SHP2/CDK4-IN-1 shows significant antitumor efficacy in the EMT6 syngeneic mouse model. SHP2/CDK4-IN-1 can be used for triple-negative breast cancer (TNBC) research .

HY-115992

CDK4/6-IN-9	CDK	Cancer
CDK4/6-IN-9 (compound 10) is a selective *CDK4/6* inhibitor with an IC₅₀ of 905 nM for CDK6/cyclin D1. CDK4/6-IN-9 has the potential for multiple myeloma (MM) research .

HY-142076

CDK4/6-IN-15	CDK	Cancer
CDK4/6-IN-15 is an orally active and selective *CDK4/6* inhibitor. CDK4/6-IN-15 potently inhibits cancer cells growth. CDK4/6-IN-15 arrests cell cycle at G1 phase and suppresses retinoblastoma tumour suppressor protein (Rb) phosphorylation at S780 and E2 factor (E2F)-regulated gene expression .

HY-143258

CDK4/6-IN-8

CDK Cancer

CDK4/6-IN-8 (Compound 7p) is a selective CDK4 and CDK6 inhibitor with IC₅₀ values of 5.01 nM and 3.97 nM, respectively .

CDK4/6-IN-8	CDK	Cancer
CDK4/6-IN-8 (Compound 7p) is a selective *CDK4* and CDK6 inhibitor with IC₅₀ values of 5.01 nM and 3.97 nM, respectively .

HY-16297

Abemaciclib methanesulfonate 70+ Cited Publications LY2835219 methanesulfonate	CDK	Cancer
Abemaciclib methanesulfonate (LY2835219 methanesulfonate) is a selective *CDK4/6* inhibitor with IC₅₀s of 2 nM and 10 nM for CDK4 and CDK6, respectively .

HY-112272A

Lerociclib dihydrochloride 1 Publications Verification G1T38 dihydrochloride	CDK	Cancer
Lerociclib dihydrochloride (G1T38 dihydrochloride) is a potent and selective inhibitor of *CDK4/CDK6*, with IC₅₀s of 1 nM and 2 nM for *CDK4/CyclinD1* and CDK6/CyclinD3, respectively.

HY-16297AS

Abemaciclib-d8 LY2835219-d₈	CDK	Cancer
Abemaciclib-d₈ is the deuterium labeled Abemaciclib. Abemaciclib (LY2835219) is a selective CDK4/6 inhibitor with IC50 values of 2 nM and 10 nM for CDK4 and CDK6, respectively.

HY-156646

Tibremciclib

CDK Cancer

Tibremciclib is a CDK4 inhibitor with antineoplastic activity .
HY-112272

Lerociclib

G1T38
CDK Cancer

Lerociclib (G1T38) is a potent and selective inhibitor of CDK4/6, with IC₅₀s of 1 nM, 2 nM for CDK4/CyclinD1 and CDK6/CyclinD3, respectively.

Tibremciclib	CDK	Cancer
Tibremciclib is a CDK4 inhibitor with antineoplastic activity .

Lerociclib G1T38	CDK	Cancer
Lerociclib (G1T38) is a potent and selective inhibitor of *CDK4/6, with IC₅₀s* of 1 nM, 2 nM for CDK4/CyclinD1 and CDK6/CyclinD3, respectively.

HY-146214

CDK4/6-IN-13	CDK	Cancer
As a cdk4/6 inhibitor. Compounds 10B and 10C showed low nanomolar activity, ideal antiproliferative activity, excellent metabolic properties and acceptable pharmacokinetics on cdk4/6.

HY-138946

XY028-140

CDK PROTACs Cancer

XY028-140 is a PROTAC connected by ligands for Cereblon and CDK. XY028-140 inhibits both CDK4/6 expression and CDK4/6 activity in cancer cells .

XY028-140	CDK PROTACs	Cancer
XY028-140 is a PROTAC connected by ligands for Cereblon and CDK. XY028-140 inhibits both CDK4/6 expression and CDK4/6 activity in cancer cells .

HY-151898

CDK4/6-IN-14	CDK	Cancer
CDK4/6-IN-14 is a potent and highly selective *CDK4* and CDK6 (CDK) inhibitor with IC₅₀s of 10 nM and 16 nM, respectively. CDK4/6-IN-14 exhibits more than 60-fold selectivity over CDKs 1, 2, 7, and 9, and shows high selectivity among other 205 kinases .

HY-112280A

Crozbaciclib fumarate

CDK Cancer

Crozbaciclib fumarate is a CDK4/6 inhibitor with IC₅₀s of 3 and 1 nM, respectively.
HY-112243

Cimpuciclib

CDK Inflammation/Immunology Cancer

Cimpuciclib is a selective CDK4 inhibitor (IC₅₀: 0.49 nM) that has anti-tumor activity .
HY-112243A

Cimpuciclib tosylate

CDK Inflammation/Immunology Cancer

Cimpuciclib tosylate is a selective CDK4 inhibitor (IC₅₀: 0.49 nM) that has anti-tumor activity .
HY-15889

AMG 925

2 Publications Verification

FLT3 CDK Cancer

AMG 925 is a potent, selective, and orally available FLT3/CDK4 dual inhibitor with IC₅₀s of 2±1 nM and 3±1 nM, respectively.
HY-15889A

AMG 925 HCl

FLT3 CDK Cancer

AMG 925 HCl is a potent, selective, and orally available FLT3/CDK4 dual inhibitor with IC₅₀s of 2±1 nM and 3±1 nM, respectively.

Crozbaciclib fumarate	CDK	Cancer
Crozbaciclib fumarate is a *CDK4/6* inhibitor with IC₅₀s of 3 and 1 nM, respectively.

Cimpuciclib	CDK	Inflammation/Immunology Cancer
Cimpuciclib is a selective *CDK4* inhibitor (IC₅₀: 0.49 nM) that has anti-tumor activity .

Cimpuciclib tosylate	CDK	Inflammation/Immunology Cancer
Cimpuciclib tosylate is a selective *CDK4* inhibitor (IC₅₀: 0.49 nM) that has anti-tumor activity .

AMG 925 2 Publications Verification	FLT3 CDK	Cancer
AMG 925 is a potent, selective, and orally available *FLT3/CDK4* dual inhibitor with IC₅₀s of 2±1 nM and 3±1 nM, respectively.

AMG 925 HCl	FLT3 CDK	Cancer
AMG 925 HCl is a potent, selective, and orally available *FLT3/CDK4* dual inhibitor with IC₅₀s of 2±1 nM and 3±1 nM, respectively.

HY-101467A

Trilaciclib hydrochloride 1 Publications Verification G1T28 hydrochloride	CDK	Cancer
Trilaciclib (G1T28) hydrochloride is an orally active *CDK4/6* inhibitor with IC₅₀ values of 1 nM and 4 nM for CDK4 and CDK6, respectively. Trilaciclib hydrochloride can effectively inhibit tumor cell proliferation and reduce the hematological toxicity caused by chemotherapy. Trilaciclib hydrochloride attenuates apoptosis and myelosuppression induced by 5FU (HY-90006) chemotherapy .

HY-101467

Trilaciclib 1 Publications Verification G1T28	CDK	Cancer
Trilaciclib (G1T28) is an orally active *CDK4/6* inhibitor with IC₅₀ values of 1 nM and 4 nM for CDK4 and CDK6, respectively. . Trilaciclib can effectively inhibit tumor cell proliferation and reduce the hematological toxicity caused by chemotherapy. Trilaciclib attenuates apoptosis and myelosuppression induced by 5FU (HY-90006) chemotherapy .

HY-129336

Abemaciclib metabolite M20 3 Publications Verification LSN3106726	CDK	Cancer
Abemaciclib metabolite M20 (LSN3106726), the active metabolite of Abemaciclib, is a selective *CDK4/6 inhibitor* for the treatment of cancer .

HY-103382

Arcyriaflavin A	Fungal	Infection
Arcyriaflavin A is a fungal metabolite obtained from the fungi, Nocardiopsis. Arcyriaflavin A is an inhibitor of CDK4 (IC₅₀ = 140 nM) and CaMKII (IC₅₀ = 25 nM) .

HY-111207

CA224	CDK Apoptosis	Cancer
CA224 (Compound 1) is a selective and orally active Cdk4–cyclin D1 inhibitor with an IC₅₀ of 6.2 µM. CA224 induces cell apoptosis and shows antitumor activity .

HY-10005

Flavopiridol 30+ Cited Publications HMR-1275; Alvocidib; L86-8275	CDK Autophagy HIV Apoptosis	Cancer
Flavopiridol (Alvocidib) is a broad spectrum and competitive inhibitor of CDKs, inhibiting CDK1, CDK2, CDK4 with IC₅₀s of 30, 170, 100 nM, respectively.

HY-153336

CDK-IN-12

CDK Cancer

CDK-IN-12 (Example 20) is a CDK Inhibitor. CDK-IN-12 Inhibits CDK4/6 with IC₅₀ values less than 20 nM .

CDK-IN-12	CDK	Cancer
CDK-IN-12 (Example 20) is a CDK Inhibitor. CDK-IN-12 Inhibits CDK4/6 with IC₅₀ values less than 20 nM .

HY-10006

Flavopiridol Hydrochloride 30+ Cited Publications Alvocidib Hydrochloride; L86-8275 Hydrochloride; HMR-1275 Hydrochloride	CDK Autophagy HIV	Cancer
Flavopiridol Hydrochloride (Alvocidib Hydrochloride) is a broad inhibitor of CDK, competing with ATP to inhibit CDKs including CDK1, CDK2, CDK4 with IC₅₀s of 30, 170, 100 nM, respectively.

HY-131466

N-Methyl Palbociclib	Drug Metabolite	Others
N-Methyl Palbociclib is an impurity of Palbociclib (HY-50767). Palbociclib (PD 0332991) is an orally active selective CDK4 and CDK6 inhibitor.

HY-136726

CGP-82996 CINK4	CDK	Cancer
GP-82996 (CINK4) is a pharmacological inhibitor of *CDK4/6. GP-82996 has IC₅₀s of 1.5, 5.6 and 25 μM for CDK4/cyclin D1, CDK6/cyclin D1 and Cdk5/p35, respectively. GP-82996 induces the apoptosis* of cancer cells U2OS. GP-82996 can be used in the research of cancer .

HY-18629

SU9516 4 Publications Verification	CDK Autophagy Apoptosis	Cancer
SU9516 is a potent CDK2 inhibitor, with an IC₅₀ of 22 nM, and also shows inhibitory effects on CDK1 and CDK4, with IC₅₀s of 40, 200 nM, respectively.

HY-158106

AZD8421	CDK	Cancer
AZD8421 is a selective CDK2 inhibitor (IC₅₀: 9 nM) with selectivity for CDK1, CDK4 and CDK6. AZD8421 inhibits cancer cell proliferation by inhibiting pRB phosphorylation, inducing cell cycle arrest and senescence. AZD8421 demonstrated promising single efficacy and synergy with CDK4/6 inhibitors such as Palbociclib (HY-50767) in in vivo breast and ovarian models. AZD8421 also has potent single-agent inhibitory activity against drug-resistant breast cancer cells.

HY-50943

AT7519 Hydrochloride 5+ Cited Publications	CDK Apoptosis	Cancer
AT7519 Hydrochloride is a potent inhibitor of CDKs, with IC₅₀s of 210, 47, 100, 13, 170, and <10 nM for CDK1, CDK2, CDK4 to CDK6, and CDK9, respectively.

HY-137449

Rintodestrant G1T48	Estrogen Receptor/ERR CDK	Cancer
Rintodestrant (G1T48) is an orally active, non-steroidal and selective estrogen receptor degrader. Rintodestrant (G1T48) is also a *CDK4/6* inhibitor .

HY-13914

Roniciclib

BAY 1000394
CDK Cancer

Roniciclib is an orally bioavailable pan-cyclin dependent kinase (CDK) inhibitor, with IC₅₀s of 5-25 nM for CDK1, CDK2, CDK3, CDK4, CDK7 and CDK9.

HY-50940

AT7519 5+ Cited Publications AT7519M	CDK Apoptosis	Cancer
AT7519 (AT7519M) as a potent inhibitor of CDKs, with IC₅₀s of 210, 47, 100, 13, 170, and <10 nM for CDK1, CDK2, CDK4 to CDK6, and CDK9, respectively.

HY-128669

Abemaciclib metabolite M2 1 Publications Verification LSN2839567	CDK Drug Metabolite	Cancer
Abemaciclib metabolite M2 (LSN2839567) is a metabolite of Abemaciclib, acts as a potent *CDK4* and CDK6 inhibitor, with IC₅₀s of 1.2 and 1.3 nM, respectively. Anti-cancer activity .

HY-10014

R547 2 Publications Verification	CDK GSK-3 Apoptosis	Cancer
R547 is a potent, selective and orally active ATP-competitive CDK inhibitor, with K_is of 2 nM, 3 nM and 1 nM for CDK1/cyclin B, CDK2/cyclin E and CDK4/cyclin D1, respectively .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-103382

Arcyriaflavin A	Infection Alkaloids Structural Classification Microorganisms Classification of Application Fields Source classification Disease Research Fields Indole Alkaloids	Fungal
Arcyriaflavin A is a fungal metabolite obtained from the fungi, Nocardiopsis. Arcyriaflavin A is an inhibitor of CDK4 (IC₅₀ = 140 nM) and CaMKII (IC₅₀ = 25 nM) .

HY-116035

Nimbolide 1 Publications Verification	Triterpenes Structural Classification Classification of Application Fields Terpenoids Source classification Plants Azadirachta indica A. Juss. Disease Research Fields Meliaceae Cancer	NF-κB CDK Apoptosis
Nimbolide is a triterpene compound that can be isolated from neem (Azadirachta indica), possesses anticancer and antiproliferative activity. Nimbolide induces tumor cell apoptosis by inhibiting NF-κB and *CDK4/CDK6* kinase. Nimbolide suppresses the Wnt, PI3K-Akt, MAPK and JAK-STAT signaling pathways .

HY-N3634

Corylifol C	Structural Classification Leguminosae Source classification Phenols Polyphenols Psoralea corylifolia L. Plants	Others
Corylifol C is a potent protein kinase inhibitor with IC₅₀ valueS of 8.7, 3.0, 2.1, 6.4, 4.5, 6.2, 2.3, 1.2, 5.1 μg/ml for ARK5, Aurora-A, Aurora-B, AXL, B-RAF-VE, CDK4/CycD1, TIE2, EGF-R, EPHB4, respectively .

Cat. No.	Product Name	Chemical Structure

HY-16297AS

Abemaciclib-d8
Abemaciclib-d₈ is the deuterium labeled Abemaciclib. Abemaciclib (LY2835219) is a selective CDK4/6 inhibitor with IC50 values of 2 nM and 10 nM for CDK4 and CDK6, respectively.

HY-129336S

Abemaciclib metabolite M20-d8
Abemaciclib metabolite M20-d₈ is the deuterium labeled Abemaciclib metabolite M20. Abemaciclib metabolite M20 (LSN3106726), the active metabolite of Abemaciclib, is a selective CDK4/6 inhibitor[1].

HY-15777AS

Ribociclib-d6 hydrochloride
Ribociclib-d₆ (hydrochloride) is a deuterium labeled Ribociclib. Ribociclib is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex[1].

HY-50767S

Palbociclib-d8
Palbociclib-d₈ is a deuterium labeled Palbociclib. Palbociclib is a selective and orally active CDK4 and CDK6 inhibitor with IC50s of 11 and 16 nM, respectively. Palbociclib has the potential for ER-positive and HER2-negative breast cancer research[1].

HY-15777S

Ribociclib-d6
Ribociclib-d₆ is a deuterium labeled Ribociclib. Ribociclib is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex[1].

HY-50767S1

Palbociclib-d4 hydrochloride
Palbociclib-d₄ (hydrochloride) is the deuterium labeled Palbociclib hydrochloride. Palbociclib (PD 0332991) is a selective CDK4 and CDK6 inhibitor with IC50s of 11 and 16 nM, respectively. Palbociclib has the potential for ER-positive and HER2-negative breast cancer research[1].

HY-15777S1

Ribociclib-d8
Ribociclib-d₈ is the deuterium labeled Ribociclib[1]. Ribociclib (LEE01) is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex[2].

HY-128669S

Abemaciclib metabolite M2-d6
Abemaciclib metabolite M2-d₆ is the deuterium labeled Abemaciclib metabolite M2. Abemaciclib metabolite M2 (LSN2839567) is a metabolite of Abemaciclib, acts as a potent CDK4 and CDK6 inhibitor, with IC50s in the range of 1-3 nM. Anti-cancer activity[1][2].

HY-126534S

Abemaciclib metabolite M18-d8
Abemaciclib metabolite M18-d₈ is the deuterium labeled Abemaciclib metabolite M18. Abemaciclib metabolite M18 (LSN3106729), the metabolite of Abemaciclib (HY-16297A), is a CDK inhibitor with antitumor activity. Abemaciclib metabolite M18 and a CRBN ligand have been used to design PROTAC CDK4/6 degrader[1][2].

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CDK4 Inhibitors

Inhibitors & Agonists

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Isotope-Labeled Compounds

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