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CDK1-IN-1

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (10) Aryl Hydrocarbon Receptor (1) Casein Kinase (1) Caspase (1) CDK (31) CFTR (1) ERK (1) FGFR (1) GSK-3 (14) Histone Demethylase (1) JNK (1) Lipoxygenase (1) Molecular Glues (2) PKC (1) VEGFR (2)
By Research Areas:	Cancer (30) Inflammation/Immunology (1) Metabolic Disease (1) Neurological Disease (5)

Inhibitors & Agonists

Isotope-Labeled Compounds

Targets Recommended: AIM2 NEKs

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-12529

Ro-3306 30+ Cited Publications	CDK Apoptosis	Cancer
Ro-3306 is a potent and selective inhibitor of *CDK1, with K_is of 20 nM, 35 nM and 340 nM for CDK1, CDK1*/cyclin B1 and CDK2/cyclin E, respectively.

HY-112462

Cdk1/2 Inhibitor III

CDK Cancer

Cdk1/2 Inhibitor III is a selective Cdk1/2 inhibitor, with an IC₅₀ of 2.1 μM for CDK1/cyclin B .

Cdk1/2 Inhibitor III	CDK	Cancer
Cdk1/2 Inhibitor III is a selective *Cdk1/2* inhibitor, with an IC₅₀ of 2.1 μM for CDK1/cyclin B .

HY-115924

*CDK1-IN-1*	CDK	Cancer
CDK1-IN-1 is a potent *CDK1* inhibitor (CDK1/CycB IC₅₀=161.2 nM) with potential antiproliferative activity and selectivity for cancer tissues. CDK1-IN-1 induces apoptosis in p53 dependent manner through the intrinsic apoptotic pathway. CDK1-IN-1 is a potential targeted antitumor agent .

HY-147901

KDM1/CDK1-IN-1	Histone Demethylase CDK Apoptosis Caspase	Cancer
KDM1/CDK1-IN-1 (compound 4) is a potent KDM1 and *CDK1* inhibitor, with IC₅₀ values of 0.096 and 0.078 μM, respectively.KDM1/CDK1-IN-1 induces cell cycle arrest at G2/M phase and apoptosis in HOP-92 cells. KDM1/CDK1-IN-1 exhibits potent cytotoxic activity against the CCRF-CEM, HOP-92 and Hep-G2 cells, with IC₅₀ values of 16.34, 3.45 and 7.79 μM, respectively .

HY-147646

CDK1/Cyc B-IN-1	CDK Apoptosis	Cancer
CDK1/Cyc B-IN-1 (Compound 5) is a selective CDK1/Cyc B complex inhibitor with an IC₅₀ of 97 nM. CDK1/Cyc B-IN-1 triggers apoptosis and G2/M cell cycle arrest. CDK1/Cyc B-IN-1 shows broad-spectrum cytotoxic action against cancer cell lines .

HY-15777

Ribociclib Maximum Cited Publications 51 Publications Verification LEE011	CDK	Cancer
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 .

HY-103221

MeBIO	Aryl Hydrocarbon Receptor GSK-3 CDK	Others
MeBIO is a potent AhR (aryl hydrocarbon receptor) agonist, with IC₅₀ of 44 μM (GSK-3) and 55 μM (CDK1/cyclin B), respectively. MeBIO is inactive on GSK-3β .

HY-11012

TDZD-8 5+ Cited Publications GSK-3β INhibitor I; NP 01139	GSK-3	Cancer
TDZD-8 is an inhibitor of GSK-3β, with an IC₅₀ of 2 μM; TDZD-8 shows less potent activities against Cdk-1/cyclin B, CK-II, PKA, and PKC, with all IC₅₀s of >100 μM.

HY-15777S

Ribociclib-d6 LEE011-d₆	CDK	Cancer
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-15777AS

Ribociclib-d6 hydrochloride LEE011-d₆ hydrochloride	CDK	Cancer
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-117535

CDK2-IN-4 2 Publications Verification	CDK	Cancer
CDK2-IN-4 (compound 73) is a potent and selective CDK2 inhibitor with an IC₅₀ of 44 nM for CDK2/cyclin A, shows 2,000-fold selectivity over CDK1/cyclin B (IC₅₀=86 uM) .

HY-112336

Aloisine RP106	CDK GSK-3	Neurological Disease
Aloisine RP106 (compound 38) is a potent inhibitor of Cdk1/cyclin B, Cdk5/p25, and GSK3 with IC₅₀s of 0.70µM, 1.5µM, 0.92 µM, respectively .

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 .

HY-111930

5-Iodo-indirubin-3'-monoxime	GSK-3 CDK	Cancer
5-Iodo-indirubin-3'-monoxime is a potent GSK-3β, CDK5/P25 and CDK1/cyclin B inhibitor, competing with ATP for binding to the catalytic site of the kinase, with IC₅₀s of 9, 20 and 25 nM, respectively .

HY-103383

(R)-DRF053 dihydrochloride	CDK Casein Kinase	Neurological Disease Cancer
(R)-DRF053 dihydrochloride is a potent casein kinases 1 (CK1), CDK1/cyclin B and CDK5/p25 inhibitor with IC₅₀s of 14 nM, 220 nM and 80 nM, respectively. (R)-DRF053 dihydrochloride prevents the CK1-dependent production of amyloid-beta in a cell model .

HY-16559A

Riviciclib P276-00 free base	CDK	Cancer
Riviciclib (P276-00 free base) is a potent cyclin-dependent kinase (CDK) inhibitor, which inhibits CDK9-cyclinT1, CDK4-cyclin D1, and *CDK1-cyclinB* with IC₅₀s of 20 nM, 63 nM, and 79 nM, respectively . Riviciclib shows antitumor activity on cisplatin-resistant cells .

HY-16559

Riviciclib hydrochloride 2 Publications Verification P276-00	CDK Apoptosis	Cancer
Riviciclib hydrochloride (P276-00) is a potent cyclin-dependent kinase (CDK) inhibitor, which inhibits CDK9-cyclinT1, CDK4-cyclin D1, and *CDK1-cyclinB* with IC₅₀s of 20 nM, 63 nM, and 79 nM, respectively . Riviciclib hydrochloride (P276-00) shows antitumor activity on cisplatin-resistant cells .

HY-10580

GSK 3 Inhibitor IX 5+ Cited Publications 6-BromoINdirubIN-3'-oxime; BIO; MLS 2052	GSK-3 CDK Apoptosis	Cancer
GSK 3 Inhibitor IX (6-Bromoindirubin-3'-oxime; BIO) is a potent, selective, reversible and ATP-competitive inhibitor of GSK-3α/β and *CDK1-cyclinB* complex with IC₅₀s of 5 nM/320 nM/80 nM for (GSK-3α/β)/CDK1/CDK5, respectively.

HY-19807

Indirubin-3'-monoxime 3 Publications Verification INdirubIN-3'-oxime	GSK-3 CDK Lipoxygenase	Cancer
Indirubin-3'-monoxime is a potent GSK-3β inhibitor, and weakly inhibits 5-Lipoxygenase, with IC₅₀s of 22 nM and 7.8-10 µM, respectively; Indirubin-3'-monoxime also shows inhibitory activities against CDK5/p25 and CDK1/cyclin B, with IC₅₀s of 100 and 180 nM.

HY-103647

K00546	CDK VEGFR GSK-3	Cancer
K00546 is a potent *CDK1* and CDK2 inhibitor with IC₅₀s of 0.6 nM and 0.5 nM for CDK1/cyclin B and CDK2/cyclin A, respectively. K00546 is also a potent CDC2-like kinase 1 (CLK1) and CLK3 inhibitor with IC₅₀s of 8.9 nM and 29.2 nM, respectively .

HY-114903

(E/Z)-BIO-acetoxime GSK-3 INhibitor X	GSK-3 CDK	Neurological Disease Metabolic Disease Cancer
(E/Z)-BIO-acetoxime (GSK-3 Inhibitor X) is a potent and selective GSK-3α/β inhibitor, with an IC₅₀ of 10 nM. (E/Z)-BIO-acetoxime shows more than 200-flod selectivity over CDK5/p25, CDK2/cyclin A and CDK1/cyclin B (IC₅₀=2.4, 4.3, 63 μM) .

HY-12214A

NVP-2 20+ Cited Publications	CDK Apoptosis	Cancer
NVP-2 is a potent and selective ATP-competitive cyclin dependent kinase 9 (CDK9) probe, inhibits CDK9/CycT activity with an IC₅₀ of 0.514 nM. NVP-2 displays inhibitory effcts on CDK1/CycB, CDK2/CycA and CDK16/CycY kinases with IC₅₀ values of 0.584 µM, 0.706 µM, and 0.605 µM, respectively. NVP-2 induces cell apoptosis.

HY-111932

Indirubin-5-sulfonate	CDK GSK-3	Cancer
Indirubin-5-sulfonate is a cyclin-dependent kinase (CDK) inhibitor, with IC₅₀ values of 55 nM, 35 nM, 150 nM, 300 nM and 65 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E, CDK4/cyclin D1, and CDK5/p35, respectively . Indirubin-5-sulfonate also shows inhibitory activity against GSK-3β .

HY-15569

NU6102	CDK	Cancer
NU6102 is a potent *CDK1* and CDK2 inhibitor with IC₅₀s of 9.5 nM and 5.4 nM for *CDK1/cyclinB* and CDK2/cyclinA3, respectively. NU6102 shows selectivity for *CDK1/CDK2* over CDK4 (IC₅₀ of 1.6 μM), DYRK1A (IC₅₀ of 0.9 μM), PDK1 (IC₅₀ of 0.8 μM) and ROCKII (IC₅₀ of 0.6 μM) .

HY-12892

SKI-178
SKI-178 is a potent sphingosine kinase-1 (SphK1) and SphK2 inhibitor. SKI-178 is cytotoxic at IC₅₀ concentrations ranging from 1.8 to 0.1 μM in both agent sensitive and multi-agent resistant cancer cell lines (i.e., MTR3, NCI-ADR and HL60/VCR cells). SKI-178 induces apoptosis in a CDK1-dependent manner in human acute myeloid leukemia cell lines .

HY-11009

CGP60474 5 Publications Verification	CDK PKC	Cancer
CGP60474, a highly potent anti-endotoxemic agent, is a potent cyclin-dependent kinase (CDK) inhibitor (IC₅₀ values are 26, 3, 4, 216, 10, 200 and 13 nM for CDK1/B, CDK2/E, CDK2/A, CDK4/D, CDK5/p25, CDK7/H and CDK9/T, respectively). CGP60474 is a selective and ATP-competitive PKC inhibitor .

HY-12302

Kenpaullone 4 Publications Verification 9-Bromopaullone; NSC-664704	CDK GSK-3	Cancer
Kenpaullone is a potent inhibitor of CDK1/cyclin B and GSK-3β, with IC₅₀s of 0.4 μM and 23 nM, and also inhibits CDK2/cyclin A, CDK2/cyclin E, and CDK5/p25 with IC₅₀s of 0.68 μM, 7.5 μM, 0.85 μM, respectively. Kenpaullone, a small molecule inhibitor of KLF4, reduces self-renewal of breast cancer stem cells and cell motility in vitro.

HY-108359

Alsterpaullone 1 Publications Verification 9-Nitropaullone; NSC 705701	CDK GSK-3 Apoptosis	Cancer
Alsterpaullone (9-Nitropaullone) is a potent CDK inhibitor, with IC₅₀s of 35 nM, 15 nM, 200 nM and 40 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E and CDK5/p35, respectively. Alsterpaullone also competes with ATP for binding to GSK-3alpha/GSK-3beta with IC₅₀s of both 4 nM. Alsterpaullone has antitumor activity, and possesses potential for the study in neurodegenerative and proliferative disorders . Alsterpaullone induces apoptosis in leukemia cell line .

HY-112371

(S)-CR8	CDK	Cancer
(S)-CR8 is the S-isomer of CR8. (S)-CR8 is a potent and selective CDK inhibitor with IC₅₀s of 0.060, 0.080, 0.11, 0.12, and 0.15 μM for CDK2/cyclin E, CDK2/cyclin A, CDK9/cyclin T, CDK5/p25, and CDK1/cyclin B, respectively. (S)-CR8 reduces SH-SY5Y cells survival (IC₅₀ 0.40 μM) .

HY-141685

3-Methylthienyl-carbonyl-JNJ-7706621	CDK GSK-3 VEGFR FGFR	Cancer
3-Methylthienyl-carbonyl-JNJ-7706621 is a potent and selective inhibitor of cyclin-dependent kinase (CDK), with IC₅₀s of 6.4 nM and 2 nM for CDK1/cyclin B and CDK2/cyclin A, respectively. 3-Methylthienyl-carbonyl-JNJ-7706621 also shows potent inhibition of GSK-3 (IC₅₀=0.041 μM) and modest potency against CDK4, VEGF-R2, and FGF-R2 (IC₅₀=0.11, 0.13, 0.22 μM, respectively). 3-Methylthienyl-carbonyl-JNJ-7706621 can be used for the research of cancer .

HY-112363

Aloisine A RP107	CDK GSK-3 ERK JNK CFTR	Inflammation/Immunology Cancer
Aloisine A (RP107) is a a potent cyclin-dependent kinase (CDK) inhibitor with IC₅₀s of 0.15 μM, 0.12 μM, 0.4 μM, 0.16 μM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E, CDK5/p35, respectively. Aloisine A ininhibits GSK-3α (IC₅₀=0.5 μM) and GSK-3β (IC₅₀=1.5 μM). Aloisine A stimulates wild-type CFTR and mutated CFTR, with submicromolar affinity by a cAMP-independent mechanism. Aloisine A has the potential for CFTR-related diseases, including cystic fibrosis research .

HY-18340

(R)-CR8 CR8, (R)-Isomer	Molecular Glues CDK Apoptosis	Neurological Disease Cancer
(R)-CR8 (CR8), a second-generation analog of Roscovitine, is a potent *CDK1/2/5/7/9* inhibitor. (R)-CR8 inhibits CDK1/cyclin B (IC₅₀=0.09 μM), CDK2/cyclin A (0.072 μM), CDK2/cyclin E (0.041 μM), CDK5/p25 (0.11 μM), CDK7/cyclin H (1.1 μM), CDK9/cyclin T (0.18 μM) and CK1δ/ε (0.4 μM). (R)-CR8 induces apoptosis and has neuroprotective effect . (R)-CR8 acts as a molecular glue degrader that depletes cyclin K .

HY-18340A

(R)-CR8 trihydrochloride CR8, (R)-Isomer trihydrochloride	Molecular Glues CDK Apoptosis	Neurological Disease Cancer
(R)-CR8 (CR8) trihydrochloride, a second-generation analog of Roscovitine, is a potent *CDK1/2/5/7/9* inhibitor. (R)-CR8 trihydrochloride inhibits CDK1/cyclin B (IC₅₀=0.09 μM), CDK2/cyclin A (0.072 μM), CDK2/cyclin E (0.041 μM), CDK5/p25 (0.11 μM), CDK7/cyclin H (1.1 μM), CDK9/cyclin T (0.18 μM) and CK1δ/ε (0.4 μM). (R)-CR8 trihydrochloride induces apoptosis and has neuroprotective effect . (R)-CR8 trihydrochloride acts as a molecular glue degrader that depletes cyclin K .

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].

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].

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