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CDK-IN-2

" in MedChemExpress (MCE) Product Catalog:

By Targets:	CDK (21) Apoptosis (6) Autophagy (1) Bcl-2 Family (1) Caspase (1) Cholinesterase (ChE) (1) E3 Ligase Ligand-Linker Conjugates (1) EGFR (3) IKK (1) Ligands for Target Protein for PROTAC (1) Molecular Glues (2) PROTAC Linkers (1) PROTACs (1) Raf (1)
By Research Areas:	Cancer (21) Inflammation/Immunology (1) Metabolic Disease (1) Neurological Disease (2)
Click Chemistry:	Alkynes (1)

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Click Chemistry

Targets Recommended: CDK AIM2 NEKs

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-13033

CDK-IN-2

1 Publications Verification

CDK INhibitor II
CDK Cancer

CDK-IN-2 is a potent and specific CDK9 inhibitor with IC50 of <8 nM, extracted from reference 1, example 4.
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 .
HY-W010128

6-(Dimethylamino)purine

6-DimethylamINopurINe
CDK Others

6-(Dimethylamino)purine is a dual inhibitor of protein kinase and CDK .

*CDK-IN-2* 1 Publications Verification CDK INhibitor II	CDK	Cancer
CDK-IN-2 is a potent and specific CDK9 inhibitor with IC50 of <8 nM, extracted from reference 1, example 4.

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 .

6-(Dimethylamino)purine 6-DimethylamINopurINe	CDK	Others
6-(Dimethylamino)purine is a dual inhibitor of protein kinase and *CDK* .

HY-146253

CDK1/2/4-IN-1	CDK Apoptosis Bcl-2 Family Caspase	Cancer
CDK1/2/4-IN-1 (compound 3a) is a potent CDK inhibitor with IC₅₀ values of 1.47, 0.78 and 0.87 μM for CDK1, CDK2 and CDK4, respectively. CDK1/2/4-IN-1 arrests cell cycle at G2/M phase and induces apoptosis. CDK1/2/4-IN-1 elevates Bax, caspase-3, P53 levels and decreases Bcl-2 level. CDK1/2/4-IN-1 can be used for cancer research .

HY-130981

FN-1501-propionic acid	CDK Ligands for Target Protein for PROTAC	Cancer
FN-1501-propionic acid is a *CDK2/9* ligand for PROTAC. FN-1501-propionic acid and a CRBN ligand have been used to design PROTAC CDK2/9 degrader (HY-130709) .

HY-130709

PROTAC CDK2/9 Degrader-1	PROTACs CDK	Cancer
PROTAC CDK2/9 Degrader-1 (Compound F3) is a potent dual degrader for *CDK2* (DC₅₀=62 nM) and CDK9 (DC₅₀=33 nM). PROTAC CDK2/9 Degrader-1 suppresses prostate cancer PC-3 cell proliferation (IC₅₀=0.12 µM) by effectively blocking the cell cycle in S and G2/M phases. PROTAC CDK2/9 Degrader-1 is a PROTAC by tethering CDK inhibitor with Cereblon ligand .

HY-103646

CK7

CDK Others

CK7, a Cdk2/9 inhibitor, can be used for the synthesis of Nek1 inhibitor BSc5231 and BSc5367 .

CK7	CDK	Others
CK7, a *Cdk2/9* inhibitor, can be used for the synthesis of Nek1 inhibitor BSc5231 and BSc5367 .

HY-13266A

BS-181 hydrochloride 4 Publications Verification	CDK	Cancer
BS-181 hydrochloride is a highly selective CDK7 inhibitor with IC₅₀ of 21 nM, and > 40-fold selective for CDK7 than CDK1, 2, 4, 5, 6, or 9.

HY-101212

Fadraciclib 5 Publications Verification CYC065	CDK	Cancer
Fadraciclib (CYC065) is a second-generation, orally available ATP-competitive inhibitor of *CDK2/CDK9* kinases with IC₅₀s of 5 and 26 nM, respectively ^[2].

HY-144117

GFB-12811	CDK	Metabolic Disease
GFB-12811 is a high selective and orally active CDK5 inhibitor with an IC₅₀ of 2.3 nM. GFB-12811 is highly selective over the other tested kinases (CDK1/2/6/7/9) .

HY-132914

CDK/HDAC-IN-1

CDK Cancer

CDK/HDAC-IN-1 shows remarkable CDK2/4/6 and HDAC6 inhibitory activity of IC₅₀ = 60.9 ± 2.9, 276 ± 22.3, 27.2 ± 4.2, and 128.6 ± 0.4 nM, respectively.

CDK/HDAC-IN-1	CDK	Cancer
CDK/HDAC-IN-1 shows remarkable *CDK2/4/6* and HDAC6 inhibitory activity of IC₅₀ = 60.9 ± 2.9, 276 ± 22.3, 27.2 ± 4.2, and 128.6 ± 0.4 nM, respectively.

HY-10542

GW 5074 Maximum Cited Publications 7 Publications Verification	Raf Apoptosis	Cancer
GW 5074 is a potent and selective c-Raf inhibitor with IC₅₀ of 9 nM, and has no effect on the activities of JNK1/2/3, MEK1, MKK6/7, CDK1/2, c-Src, p38 MAP, VEGFR2 or c-Fms ^[2].

HY-130713

Thalidomide-C2-amido-C2-COOH	E3 Ligase Ligand-Linker Conjugates Autophagy Apoptosis	Cancer
Thalidomide-C2-amido-C2-COOH incorporates a CRBN ligand for the E3 ubiquitin ligase, and a linker. Thalidomide-C2-amido-C2-COOH can be used to design PROTAC CDK2/9 Degrader-1 (HY-130709) .

HY-130712

NH2-C2-amido-C2-Boc	PROTAC Linkers	Cancer
NH2-C2-amido-C2-Boc is a PROTAC linker, which refers to the alkyl/ether composition. NH2-C5-NH-Boc can be used in the synthesis of a series of PROTACs, such as the PROTAC CDK2/9 Degrader-1 (HY-130709) .

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-149436

CDK2/Bcl2-IN-1	CDK	Cancer
CDK2/Bcl2-IN-1 (compound 1), a saponin and a CDK-2 inhibitor (IC₅₀=117.6 nM) with promising cytotoxicity against cancer cells. CDK2/Bcl2-IN-1 also inhibits Bcl-2, and induces apoptosis in A549 lung cancer cells .

HY-135366

HPN-01	IKK	Inflammation/Immunology
HPN-01 is a potent and selective IKK inhibitor, with pIC₅₀ values of 6.4, 7.0 and <4.8 for IKK-α, IKK-β and IKK-ε, respectively. HPN-01 displays greater 50-fold selectivity over a panel of more than 50 other kinases, including ALK5, CDK-2, EGFR, ErbB2, GSK3β, PLK1, Src, and VEGFR-2 .

HY-156114

EGFR/CDK2-IN-2	EGFR CDK	Cancer
EGFR/CDK2-IN-2 (compound 6a) is a dual inhibitor of EGFR and CDK-2 with IC₅₀s of 19.6 and 87.9 nM, respectively. EGFR/CDK2-IN-2 induces apoptosis in MCF-7 cells and arrests the cell cycle in the S phase. EGFR/CDK2-IN-2 has significant anti-cancer cell toxicity and inhibits MCF-7 with an IC₅₀ of 0.39 μM .

HY-156115

EGFR/CDK2-IN-3	EGFR CDK	Cancer
EGFR/CDK2-IN-3 (compound 4b) is a dual inhibitor of EGFR and CDK-2 with IC₅₀s of 71.7 and 113.7 nM, respectively. EGFR/CDK2-IN-3 induces apoptosis in MCF-7 cells and arrests the cell cycle in the S phase. EGFR/CDK2-IN-3 has significant anti-cancer cell toxicity and inhibits MCF-7 with an IC₅₀ of 3.16 μM .

HY-156116

EGFR/CDK2-IN-4	EGFR CDK	Cancer
EGFR/CDK2-IN-4 (compound 4c) is a dual inhibitor of EGFR and CDK-2 with IC₅₀s of 89.6 and 165.4 nM, respectively. EGFR/CDK2-IN-4 induces apoptosis in MCF-7 cells and arrests the cell cycle in the S phase. EGFR/CDK2-IN-4 has significant anti-cancer cell toxicity and inhibits MCF-7 with an IC₅₀ of 2.74 μM .

HY-148213

CDK2/4/6-IN-1	CDK	Cancer
CDK2/4/6-IN-1(example 29) is a *CDK2/4/6* inhibitor with IC₅₀ values of 2.5, 23.7 and 44.3 nM for CDK2, CDK4 and CDK6, respectively. CDK2/4/6-IN-1 can be used in cancer research . CDK2/4/6-IN-1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-151436

ZLMT-12	CDK Cholinesterase (ChE) Apoptosis	Cancer
ZLMT-12 (compound 35), tacrine derivatives, is a potent, orally active *CDK2/9* inhibitor with IC₅₀ values of 0.002 and 0.011 μM for CDK9 and CDK2, respectively. ZLMT-12 has a weak inhibitory effect on AChE (IC₅₀=19.023 μM) and BChE (IC₅₀=2.768 μM). ZLMT-12 has low toxicity and antiproliferative activity. ZLMT-12 induces apoptosis and arrests the cell cycle in the S phase and G2/M phase .

HY-111388A

SEL120-34A monohydrochloride 5 Publications Verification	CDK	Cancer
SEL120-34A monohydrochloride is an ATP-competitive and selective CDK8 inhibitor, inhibits kinase activities of CDK8/CycC and CDK19/CycC complexes with IC₅₀s of 4.4 nM and 10.4 nM, respectively, with a K_d of 3 nM for CDK8. SEL120-34A monohydrochloride weakly inhibits CDK9 (calculated IC₅₀=1070 nM), but shows no obvious activity against CDK1, 2, 4, 6, 5, 7. SEL120-34A monohydrochloride inhibits phosphorylation of STAT1 S727 and STAT5 S726 . Has anti-tumor activity .

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 ^[2]. (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 ^[2]. (R)-CR8 trihydrochloride acts as a molecular glue degrader that depletes cyclin K .

6-(Dimethylamino)purine 6-DimethylamINopurINe	Classification of Application Fields Other Diseases Disease Research Fields	CDK
6-(Dimethylamino)purine is a dual inhibitor of protein kinase and *CDK* .

CDK2/Bcl2-IN-1	Structural Classification Terpenoids Zygophyllaceae Source classification Diterpenoids Plants Zygophyllum album L.f.	CDK
CDK2/Bcl2-IN-1 (compound 1), a saponin and a CDK-2 inhibitor (IC₅₀=117.6 nM) with promising cytotoxicity against cancer cells. CDK2/Bcl2-IN-1 also inhibits Bcl-2, and induces apoptosis in A549 lung cancer cells .

CDK2/4/6-IN-1		Alkynes
CDK2/4/6-IN-1(example 29) is a *CDK2/4/6* inhibitor with IC₅₀ values of 2.5, 23.7 and 44.3 nM for CDK2, CDK4 and CDK6, respectively. CDK2/4/6-IN-1 can be used in cancer research . CDK2/4/6-IN-1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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CDK-IN-2

Inhibitors & Agonists

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Click Chemistry

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