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Results for "

CDK12 inhibitor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (5) CDK (27) DNA/RNA Synthesis (1) GSK-3 (1) HDAC (1) PARP (2) PROTACs (2) Raf (1)
By Research Areas:	Cancer (27) Metabolic Disease (1)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-112626

CDK12-IN-2	CDK	Cancer
CDK12-IN-2 is a potent, selective and nanomolar *CDK12* inhibitor (IC₅₀=52 nM) with good physicochemical properties. CDK12-IN-2 is also a strong CDK13 inhibitor due to CDK13 is the closest homologue of CDK12. CDK12-IN-2 shows excellent kinase selectivity for CDK12 over CDK2, 9, 8, and 7. CDK12-IN-2 inhibits the phosphorylation of Ser2 in the C-terminal domain of RNA polymerase II. CDK12-IN-2 can be used an excellent chemical probe for functional studies of CDK12 .

HY-112261

CDK12-IN-3

CDK Cancer

CDK12-IN-3 is a potent and selective CDK12 inhibitor with an IC₅₀ of 491 nM in enzymatic assay.

CDK12-IN-3	CDK	Cancer
CDK12-IN-3 is a potent and selective *CDK12* inhibitor with an IC₅₀ of 491 nM in enzymatic assay.

HY-157297

CDK-IN-13	CDK	Cancer
CDK-IN-13 (compound 32E) is a potent and selective inhibitor of *CDK12/cyclinK* with an IC₅₀ of 3 nM. CDK-IN-13 inhibits the growth of the HER2-positive breast cancer cell lines .

HY-160284

CDK12/13-IN-1

CDK Cancer

CDK12/13-IN-1 (Compound 4) is a CDK12/13 inhibitor. CDK12/13-IN-1 has antitumor activity .

CDK12/13-IN-1	CDK	Cancer
CDK12/13-IN-1 (Compound 4) is a *CDK12/13* inhibitor. CDK12/13-IN-1 has antitumor activity .

HY-117203A

CDK12-IN-E9	CDK	Cancer
CDK12-IN-E9 is a potent and selective covalent *CDK12* inhibitor and a non-covalent CDK9 inhibitor, while avoiding ABC transporter-mediated efflux. CDK12-IN-E9 has weak binding ability to CDK7/CyclinH complex with an IC₅₀> 1 μM .

HY-139328

CDK12-IN-5	CDK	Cancer
CDK12-IN-5, a pyrazolotriazine, is a potent CDK12 inhibitor with an IC₅₀ of 23.9 nM at high ATP (2 mM). CDK12-IN-5 has no effect on CDK2/Cyclin E (IC₅₀=173 μM) and CDK9/Cyclin T1 (IC₅₀=127 μM) at high ATP (2 mM) (WO2021116178A1) .

HY-144691

PP-C8	PROTACs CDK	Cancer
PP-C8 is a potent and selective *PROTAC CDK12-Cyclin K* degrader. PP-C8 induces CDK12-Cyclin K degradation with DC₅₀s of 416 and 412 nM for CDK12 and Cyclin K, respectively. PP-C8 demonstrates profound synergistic antiproliferative effects with PARP inhibitor in triple-negative breast cancer (TNBC) .

HY-139327

CDK12-IN-4	CDK	Cancer
CDK12-IN-4, a pyrazolotriazine, is a potent CDK12 inhibitor with an IC₅₀ of 0.641 μM at high ATP (2 mM). CDK12-IN-4 has no effect on CDK2/Cyclin E (IC₅₀>20 μM) and CDK9/Cyclin T1 (IC₅₀>20 μM) at high ATP (2 mM) (WO2021116178A1) .

HY-139329

CDK12-IN-6	CDK	Cancer
CDK12-IN-6, a pyrazolotriazine, is a potent CDK12 inhibitor with an IC₅₀ of 1.19 μM at high ATP (2 mM). CDK12-IN-6 has no effect on CDK2/Cyclin E (IC₅₀>20 μM) and CDK9/Cyclin T1 (IC₅₀>20 μM) at high ATP (2 mM) (WO2021116178A1) .

HY-145072

BSJ-01-175	CDK	Cancer
BSJ-01-175 is a potent and selective *CDK12/13* covalent inhibitor. BSJ-01-175 demonstrates exquisite selectivity, potent inhibition of RNA polymerase II phosphorylation, and downregulation of CDK12-targeted genes in cancer cells .

HY-130250

SR-4835 10+ Cited Publications	CDK Apoptosis	Cancer
SR-4835 is a potent, highly selective and ATP competitive dual inhibitor of *CDK12/CDK13* (CDK12: IC₅₀=99 nM, K_d=98 nM; CDK13: K_d=4.9 nM). SR-4835 acts in synergy with DNA-damaging chemotherapy and PARP inhibitors and provokes triple-negative breast cancer (TNBC) cell death .

HY-103618

THZ531

15+ Cited Publications

CDK Cancer

THZ531 is a selective and covalent inhibitor of both CDK12 and CDK13 with IC₅₀s of 158 nM and 69 nM, respectively .

THZ531 15+ Cited Publications	CDK	Cancer
THZ531 is a selective and covalent inhibitor of both *CDK12* and CDK13 with IC₅₀s of 158 nM and 69 nM, respectively .

HY-153244

MFH290	CDK	Cancer
MFH290 is a potent and highly selective cyclin-dependent kinase 12/13 (CDK12/13) covalent inhibitor. MFH290 forms a covalent bond with Cys-1039 of CDK12 and exhibits excellent kinome selectivity and inhibits the phosphorylation of serine-2 in the C-terminal domain (CTD) of RNA-polymerase II (Pol II). MFH290 is used for cancer research .

HY-46568

CDK7/12-IN-1	CDK	Cancer
CDK7/12-IN-1 is a selective CDK7/12 inhibitor with IC₅₀s of 3 and 277 nM for CDK7 and CDK 12, respectively. CDK7 and CDK12 inhibition is an effective strategy to inhibit tumour growth .

HY-80013

THZ1 Maximum Cited Publications 73 Publications Verification	CDK	Cancer
THZ1 is a selective and potent covalent CDK7 inhibitor with an IC₅₀ of 3.2 nM. THZ1 also inhibits the closely related kinases *CDK12* and CDK13 and downregulates MYC expression .

HY-80013A

THZ1 Hydrochloride Maximum Cited Publications 73 Publications Verification	CDK	Cancer
THZ1 Hydrochloride is a selective and potent covalent CDK7 inhibitor with an IC₅₀ of 3.2 nM. THZ1 Hydrochloride also inhibits the closely related kinases *CDK12* and CDK13 and downregulates MYC expression .

HY-155038

Antitumor agent-104	PARP CDK	Cancer
Antitumor agent-104 (Compound 9) is an antitumor agent by inhibiting DNA damage repair in tumors. Antitumor agent-104 inhibits PARP1 enzymatic activity and the PAR protein level. Antitumor agent-104 also inhibits the expression of *CDK12* .

HY-149398

PARP-1/2-IN-2	Apoptosis PARP CDK	Cancer
PARP-1/2-IN-2-IN-1 (Compound 12e) is a *PARP1/2/CDK12* inhibitor (IC₅₀: 34, 30 and 285 nM respectively). PARP-1/2-IN-2 inhibits DNA damage repair, promotes cell cycle arrest and apoptosis. PARP-1/2-IN-2 inhibits the growth of TNBC cells and TNBC xenograft tumor .

HY-10542

GW 5074 5+ Cited Publications	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 .

HY-150641

CDK-IN-9	CDK Apoptosis DNA/RNA Synthesis	Cancer
CDK-IN-9 (compound 24) is a potent CDK inhibitor, also as a molecular glue inducing an interaction between CDK12 and DDB1, with an IC₅₀ values of 4 nM for CDK2/E. CDK-IN-9 leads to polyubiquitination of cyclin K and its subsequent degradation. CDK-IN-9 induce apoptosis through dephosphorylation of retinoblastoma protein and RNA polymerase II .

HY-116871

YKL-1-116	CDK	Cancer
YKL-1-116 is a selective and covalent inhibitor of Cdk7. YKL-1-116 does not target Cdk9, Cdk12, or Cdk13. YKL-1-116 is more potent than THZ1 (HY-80013) toward both Cdk7 ^WT and Cdk7 ^as, although Cdk7 ^as is relatively resistant to this compound as well .

HY-138293

SY-5609 1 Publications Verification CDK7-IN-3	CDK Apoptosis	Cancer
SY-5609 (CDK7-IN-3) is an orally active, highly selective, noncovalent CDK7 inhibitor with a K_D of 0.065 nM. SY-5609 shows poor inhibition on CDK2 (K_i=2600 nM), CDK9 (K_i=960 nM), CDK12 (K_i=870 nM). SY-5609 induces apoptosis in tumor cells and has antitumor activity .

HY-149819

CDK/HDAC-IN-3	HDAC CDK	Cancer
CDK/HDAC-IN-3 is an orally active HDACs/CDKs dual inhibitor. CDK/HDAC-IN-3 has potent and selective inhibition of CDK9, CDK12, CDK13, HDAC1, HDAC2 and HDAC3 with IC₅₀ values of 98.32 nM, 98.85 nM, 100 nM, 62.12 nM, 93.28nM and 82.87 nM. CDK/HDAC-IN-3 can be used for the acute myeloid leukemia (AML) .

HY-139039

BSJ-4-116	PROTACs CDK	Cancer
BSJ-4-116 is a PROTAC connected by ligands for Cereblon and CDK. BSJ-4-116 is a highly potent and selective *CDK12* degrader (PROTAC) with an IC₅₀ of 6 nM. BSJ-4-116 downregulates DDR genes through a premature termination of transcription, primarily through increasing poly(adenylation). BSJ-4-116 exhibits potent antiproliferative effects, alone and in combination with the poly(ADP-ribose) polymerase inhibitor Olaparib (HY-10162) .

HY-151878

CDK7-IN-20	CDK GSK-3	Metabolic Disease
CDK7-IN-20 is a potent, selective and irreversible CDK7 (CDK) inhibitor with an IC₅₀ value of 4 nM. CDK7-IN-20 displays >206-fold selectivity for CDK7 over CDK1, CDK2, CDK3, CDK5, CDK6, CDK9 and CDK12 . CDK7-IN-20 has the potential for autosomal dominant polycystic kidney disease (ADPKD) research .

HY-101257

YKL-5-124 5 Publications Verification	CDK	Cancer
YKL-5-124 is a potent, selective, irreversible and covalent CDK7 inhibitor with IC₅₀s of 53.5 nM and 9.7 nM for CDK7 and CDK7/Mat1/CycH, respectively. YKL-5-124 is >100-fold greater selective for CDK7 than CDK9 and CDK2, and inactive against CDK12 and CDK13. YKL-5-124 induces a strong cell-cycle arrest, inhibits E2F-driven gene expression, and exhibits little effect on RNA polymerase II phosphorylation status .

HY-101257B

YKL-5-124 TFA 5 Publications Verification	CDK	Cancer
YKL-5-124 TFA is a potent, selective, irreversible and covalent CDK7 inhibitor with IC₅₀s of 53.5 nM and 9.7 nM for CDK7 and CDK7/Mat1/CycH, respectively. YKL-5-124 TFA is >100-fold greater selective for CDK7 than CDK9 and CDK2, and inactive against CDK12 and CDK13. YKL-5-124 TFA induces a strong cell-cycle arrest, inhibits E2F-driven gene expression, and exhibits little effect on RNA polymerase II phosphorylation status .

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CDK12 inhibitor

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