Search Result

Results for "

CDK7 inhibitor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	CDK (85) Apoptosis (19) Autophagy (2) Bcl-2 Family (1) c-Myc (4) Casein Kinase (2) Caspase (1) DNA/RNA Synthesis (3) Early 2 Factor (E2F) (2) ERK (1) GSK-3 (1) HDAC (1) HIV (2) HSV (2) Isotope-Labeled Compounds (1) JAK (1) Ligands for Target Protein for PROTAC (1) MDM-2/p53 (1) Molecular Glues (2) PKC (1) PROTACs (2) Reactive Oxygen Species (ROS) (1) Reference Standards (3) Ser/Thr Kinase (1) Topoisomerase (2) Wnt (2) β-catenin (1)
By Research Areas:	Cancer (81) Cardiovascular Disease (1) Infection (3) Inflammation/Immunology (2) Metabolic Disease (3) Neurological Disease (2)

By Targets:

CDK (85)

Apoptosis (19)

Autophagy (2)

Bcl-2 Family (1)

c-Myc (4)

Casein Kinase (2)

Caspase (1)

DNA/RNA Synthesis (3)

Early 2 Factor (E2F) (2)

ERK (1)

GSK-3 (1)

HDAC (1)

HIV (2)

HSV (2)

Isotope-Labeled Compounds (1)

JAK (1)

Ligands for Target Protein for PROTAC (1)

MDM-2/p53 (1)

Molecular Glues (2)

PKC (1)

PROTACs (2)

Reactive Oxygen Species (ROS) (1)

Reference Standards (3)

Ser/Thr Kinase (1)

Topoisomerase (2)

Wnt (2)

β-catenin (1)

By Research Areas:

Cancer (81)

Cardiovascular Disease (1)

Infection (3)

Inflammation/Immunology (2)

Metabolic Disease (3)

Neurological Disease (2)

Inhibitors & Agonists

Isotope-Labeled Compounds

Targets Recommended: CDK

Cat. No.	상품명	Target	연구분야	Chemical Structure

HY-138293

SY-5609 5+ Cited Publications 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-10008

SNS-032 10+ Cited Publications BMS-387032	CDK Apoptosis	Cancer
SNS-032 (BMS-387032) is a potent and selective inhibitor of CDK2, *CDK7, and CDK9* with IC₅₀s of 38 nM, 62 nM and 4 nM, respectively. SNS-032 has antitumor effect .

HY-103712A

Samuraciclib hydrochloride 10+ Cited Publications CT7001 hydrochloride; ICEC0942 hydrochloride	CDK Apoptosis	Cancer
Samuraciclib hydrochloride (CT7001 hydrochloride) is a potent, selective, ATP-competitive and orally active *CDK7* inhibitor, with an IC₅₀ of 41 nM. Samuraciclib hydrochloride displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC₅₀ of 578 nM), CDK5 and CDK9, respectively. Samuraciclib hydrochloride inhibits the growth of breast cancer cell lines with GI₅₀ values between 0.2-0.3 µM. Samuraciclib hydrochloride has anti-tumor effects .

HY-101257

YKL-5-124 15+ Cited Publications	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-80013

THZ1 Maximum Cited Publications 93 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-18340

(R)-CR8 1 Publications Verification CR8, (R)-Isomer	Molecular Glues CDK Apoptosis	Neurological Disease Cancer
(R)-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-153278

Q901 CDK7-IN-21	CDK DNA/RNA Synthesis c-Myc Early 2 Factor (E2F) Topoisomerase	Cancer
Q901 (CDK7-IN-21) is a selective and potent *CDK7* inhibitor with an IC₅₀ of 10 nM. Q901 disrupts MYC and E2FTOP1-DPCs and sensitizes tumor to TOP1 inhibitors by suppressing RNAPII transition from initiation to elongation. Q901 can inhibit tumor growth and significantly enhances tumor growth inhibition combined with TOP1 inhibitors. Q901 can be used for the research of cancer, such as colon cancer and lung cancer .

HY-13914

Roniciclib 2 Publications Verification 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-10424

Milciclib 5+ Cited Publications PHA-848125	CDK Autophagy	Cancer
Milciclib (PHA-848125) is a potent, ATP-competitive and dual inhibitor of CDK and Tropomyosin receptor kinase (TRK), with IC₅₀s of 45, 150, 160, 363, 398 nM and 53 nM for cyclin A/CDK2, cyclin H/CDK7, cyclin D1/CDK4, cyclin E/CDK2, cyclin B/CDK1 and TRKA, respectively.

HY-103712

Samuraciclib 10+ Cited Publications CT7001; ICEC0942	CDK Apoptosis	Cancer
Samuraciclib (CT7001) is a potent, selective, ATP-competitive and orally active *CDK7* inhibitor, with an IC₅₀ of 41 nM. Samuraciclib displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC₅₀ of 578 nM), CDK5 and CDK9, respectively. Samuraciclib inhibits the growth of breast cancer cell lines with GI₅₀ values between 0.2-0.3 μM. Samuraciclib has anti-tumor effects .

HY-12280

THZ2 5 Publications Verification	CDK	Cancer
THZ2 is a potent and selective *CDK7* inhibitor with an IC₅₀ of 13.9 nM.

HY-12653

LDC4297 5+ Cited Publications	CDK HIV HSV	Infection
LDC4297 is a selective inhibitor of *CDK7* with an IC₅₀ value of 0.13 nM. LDC4297 inhibits human cytomegalovirus (HCMV) replication with an EC₅₀ value of 24.5 nM. LDC4297 shows broad antiviral activities to Herpesviridae, Adenoviridae, Poxviridae, Retroviridae and Orthomyxoviridae with EC₅₀ value of 0.02-1.21 μM. LDC4297 can be used for the research of infection .

HY-18285

Longdaysin	Wnt Casein Kinase ERK CDK	Cancer
Longdaysin is a inhibitor of the Wnt/β-catenin signaling pathway, which exerts antitumor effect through blocking CK1δ/ε-dependent Wnt signaling. Longdaysin inhibits CK1α, CK1δ, *CDK7, and ERK2* with IC₅₀s of 5.6 µM, 8.8 µM, 29 µM, and 52 µM, respectively .

HY-11009

CGP60474 5+ Cited Publications	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-13266A

BS-181 hydrochloride 5+ Cited Publications	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-12293

LY2857785 4 Publications Verification	CDK Apoptosis	Cancer
LY2857785 is a type I reversible and competitive ATP kinase inhibitor against CDK9 (IC₅₀ 11 nM) and other transcription kinases CDK8 (IC₅₀ 16 nM), and *CDK7* (IC₅₀ 246 nM).

HY-80013A

THZ1 Hydrochloride Maximum Cited Publications 93 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-128587

Mevociclib 5+ Cited Publications SY-1365	CDK	Cancer
Mevociclib (SY-1365) is a potent and first-in-class selective *CDK7* inhibitor, with a K_i of 17.4 nM. Mevociclib exhibits anti-proliferative and apoptotic effects in solid tumor cell lines. Mevociclib possesses anti-tumor activity in hematological and multiple aggressive solid tumors .

HY-128867

bio-THZ1 1 Publications Verification	CDK	Cancer
bio-THZ1 is a biotinylated version of THZ1 and binds irreversibly to CDK7. THZ1 is a selective and potent covalent *CDK7* inhibitor with an IC₅₀ of 3.2 nM .

HY-117203A

CDK12-IN-E9 1 Publications Verification	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-161828

JWZ-5-13	PROTACs CDK	Cancer
JWZ-5-13 is a *CDK7* PROTAC degrader. JWZ-5-13 inhibits the proliferation of cancer cells. JWZ-5-13 is applicable to the research of ovarian cancer, diffuse large B-cell lymphoma, acute T-lymphoblastic leukemia and non-small cell lung cancer .

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-139342

CDK7-IN-4	CDK	Cancer
CDK7-IN-4 (compound I) is a potent *CDK7* (Cyclin-dependent kinase 7) inhibitor. CDK7-IN-4 shows anticancer activity. CDK7-IN-4 inhibits the in vitro growth of cancer cell lines from a variety of histologies including colon , breast , lung , ovary and stomach , in a dose dependent manner .

HY-18340A

(R)-CR8 trihydrochloride 1 Publications Verification 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 .

HY-101257B

YKL-5-124 TFA 15+ Cited Publications	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 .

HY-123955

Casein Kinase inhibitor A86	Casein Kinase CDK Apoptosis	Cancer
Casein Kinase inhibitor A86 is a potent and orally active casein kinase 1α (CK1α) inhibitor. Casein Kinase inhibitor A86 also inhibits of CDK7 (TFIIH) and CDK9 (P-TEFb). Casein Kinase inhibitor A861 induces leukemia cell apoptosis, and has potent anti-leukemic activities .

HY-12653A

LDC4297 hydrochloride 5+ Cited Publications	CDK HIV HSV	Infection
LDC4297 hydrochloride is a selective inhibitor of *CDK7* with an IC₅₀ value of 0.13 nM. LDC4297 hydrochloride inhibits human cytomegalovirus (HCMV) replication with an EC₅₀ value of 24.5 nM. LDC4297 hydrochloride shows broad antiviral activities to Herpesviridae, Adenoviridae, Poxviridae, Retroviridae and Orthomyxoviridae with EC₅₀ values of 0.02-1.21 μM. LDC4297 hydrochloride can be used for the research of infection .

HY-14372

BS-194	CDK	Cancer
BS-194 is an orally active, selective and potent CDK inhibitor. BS-194 inhibits CDK2, CDK1, CDK5, CDK7, CDK9 (IC₅₀s: 3, 30, 30, 250, and 90 nM respectively). BS-194 potently inhibits cancer cells proliferation. BS-194 can be used in the research of cancers like breast cancer, colon cancer .

HY-103712C

Samuraciclib hydrochloride hydrate 10+ Cited Publications CT7001 hydrochloride hydrate; ICEC0942 hydrochloride hydrate	CDK Apoptosis	Cancer
Samuraciclib (CT7001) hydrochloride hydrate is a potent, selective, ATP-competitive and orally active *CDK7* inhibitor, with an IC₅₀ of 41 nM. Samuraciclib hydrochloride hydrate displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC₅₀ of 578 nM), CDK5 and CDK9, respectively. Samuraciclib hydrochloride hydrate inhibits the growth of breast cancer cell lines with GI₅₀ values between 0.2-0.3 μM. Samuraciclib hydrochloride hydrate has anti-tumor effects .

HY-103712B

Samuraciclib hydrochloride dihydrate 10+ Cited Publications CT7001 hydrochloride dihydrate; ICEC0942 hydrochloride dihydrate	CDK Apoptosis	Cancer
Samuraciclib (CT7001) hydrochloride hydrate is a potent, selective, ATP-competitive and orally active *CDK7* inhibitor, with an IC₅₀ of 41 nM. Samuraciclib hydrochloride hydrate displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC₅₀ of 578 nM), CDK5 and CDK9, respectively. Samuraciclib hydrochloride hydrate inhibits the growth of breast cancer cell lines with GI₅₀ values between 0.2-0.3 μM. Samuraciclib hydrochloride hydrate has anti-tumor effects .

HY-147600

CDK7-IN-15	CDK	Cancer
CDK7-IN-15 (Compound 8) is a selective *CDK7* inhibitor with an IC₅₀ greater than 10 nM and less than or equal to 100 nM. CDK7-IN-15 is applicable to the research of cancers associated with transcriptional dysregulation .

HY-155218

TMX-2172	PROTACs CDK	Cancer
TMX-2172 is a selective bivalent cereblon-recruiting PROTAC-based dual CDK2 and CDK5 degrader with IC₅₀ values of 6.5 nM and 6.8 nM, respectively. TMX-2172 shows selectivity for CDK2 and CDK5 over other cell cycle CDKs (CDK1, CDK4, and CDK6) and transcriptional CDKs (CDK7 and CDK9). TMX-2172 inhibits CDK2/CDK5 enzymatic activity, induces their proteasomal degradation, reduces ASCL1 protein levels and half-life, induces cancer cell death, and exerts antiproliferative effects. TMX-2172 can be used for the research of ovarian cancer and small cell lung cancer .

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-155787

SHR5428	CDK	Cancer
SHR5428 is a potent, orally active, selective and noncovalent inhibitor of *CDK7* with highly potent CDK7 enzymatic activity (IC₅₀=2.3 nM). SHR5428 inhibits triple negative breast cancer cellular activity on MDA-MB-468 cell (IC₅₀=6.6 nM) .

HY-151069

TMX-2039	Ligands for Target Protein for PROTAC CDK	Cancer
TMX-2039 is a pan-CDK inhibitor for both cell cycle CDKs (CDK1, CDK2, CDK4, CDK5 and CDK6) and transcriptional CDKs (CDK7 and CDK9), with IC₅₀s of 2.6, 1.0, 52.1, 0.5, 35.0, 32.5 and 25 nM, respectively. TMX-2039 acts as a Ligands for Target Protein for PROTACs .

HY-18969

LDC3140	CDK	Cancer
LDC3140 is a selective CDK7 inhibitor (IC₅₀<5 nM). By inhibiting the activity of CDK7, LDC3140 affects the regulation of the cell cycle, leading to cell cycle arrest and thus inhibiting the proliferation of tumor cells. LDC3140 can be used in the research of cancer treatment .

HY-158170

CDK7-IN-28	CDK	Cancer
CDK7-IN-28 (CDK7-1276) is a potent *CDK7* inhibitor(IC₅₀＜5 nM). CDK7-IN-28 can inhibit proliferation of MDA-MB-468 cell line by blocking cell cycle and inhibiting DNA replication .

HY-147597

CDK7-IN-13	CDK	Cancer
CDK7-IN-13 is a potent inhibitor of *CDK7. CDK7-IN-13* is a pyrimidinyl derivative compound. CDK7-IN-13 has the potential for the research of various cancers, especially the cancer with transcriptional dysregulation (extracted from patent CN114249712A, compound 1) .

HY-163856

CDK7-IN-30	Apoptosis DNA/RNA Synthesis CDK	Cancer
CDK7-IN-30 (Compound 22) is a *CDK7* inhibitor (IC₅₀ = 7.21 nM) that effectively inhibits the phosphorylation of RNA Polymerase II and CDK2. CDK7-IN-30 CDK7-IN-30 can induce cell apoptosis and has anti-cancer activity and can be used in cancer research .

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-13266

BS-181 5+ Cited Publications	CDK Apoptosis	Cancer
BS-181 is a potent and selective *CDK7* inhibitor (IC₅₀=21 nM) than Seliciclib (HY-30237). BS-181 is also against CDK2, CDK5 and CDK9 with IC₅₀ values of 880, 3000 and 4200 nM, respectively (fails to block CDK1, 4 and 6). BS-181 inhibits a panel of cancer cells growth (IC₅₀=11.5 μM-37.3 μM) and induces cell apoptosis. BS-181 has the potential for the research of cancer therapy .

HY-145655

CDK7-IN-11	CDK	Cancer
CDK7-IN-11 is an orally active *CDK7* inhibitor. CDK7-IN-11 exhibits high CDK7 inhibitory activity with IC₅₀ value of 4.2 nM. CDK7-IN-11 can be effectively used for the research of diseases associated with CDK7 .

HY-147598

CDK7-IN-14	CDK	Cancer
CDK7-IN-14 is a potent inhibitor of *CDK7. CDK7-IN-14* is a pyrimidinyl derivative compound. CDK7-IN-14 has the potential for the research of various cancers, especially the cancer with transcriptional dysregulation (extracted from patent CN114249712A, compound 3) .

HY-163721

CDK7-IN-29	CDK	Cancer
CDK7-IN-29 (compound 20) is an inhibitor of CDK7 with an IC₅₀ value of 1.4 nM. CDK7-IN-29 has oral activity and good pharmacokinetic (PK) properties .

HY-172194

JNJ-3738	CDK	Cancer
JNJ-3738 (Compound 148) is the inhibitor for *CDK7* with a K_i of 21.75 nM. JNJ-3738 inhibits the proliferation of CDK7 WT expressing A549 with pIC₅₀ of 7.37 .

HY-80013B

(E/Z)-THZ1 dihydrochloride	CDK	Cancer
(E/Z)-THZ1 dihydrochloride is a selective inhibitor of CDK7 with an IC₅₀ of 3.2 nM. (E/Z)-THZ1 dihydrochloride has antiproliferative effect .

HY-153278A

Q901 TFA CDK7-IN-21 TFA	CDK DNA/RNA Synthesis c-Myc Early 2 Factor (E2F) Topoisomerase	Cancer
Q901 (CDK7-IN-21) TFA is a selective and potent *CDK7* inhibitor with an IC₅₀ of 10 nM. Q901 TFA disrupts MYC and E2FTOP1-DPCs and sensitizes tumor to TOP1 inhibitors by suppressing RNAPII transition from initiation to elongation. Q901 TFA can inhibit tumor growth and significantly enhances tumor growth inhibition combined with TOP1 inhibitors. Q901 TFA can be used for the research of cancer, such as colon cancer and lung cancer .

HY-112450

Olomoucine II	CDK	Cancer
Olomoucine II is a potent CDK inhibitor with IC₅₀ values of 0.06, 0.1, 0.45, 7.6, 19.8 µM for CDK9/cyclin T, CDK2/cyclin E, CDK7/cyclin H, CDK1/cyclin B, CDK4/cyclin D1, respectively. Olomoucine II shows antiproliferative activity .

HY-147409

Ulecaciclib	CDK	Cancer
Ulecaciclib is an orally activitive inhibitor of cyclin-dependent kinase (CDK), with K_i values of 0.62 μM (CDK2/Cyclin A), 0.2 nM (CDK4/Cyclin D1), 3 nM (CDK6/Cyclin D3), and 0.63 μM (CDK7/Cyclin H), respectively. Ulecaciclib can cross blood brain barrier and has good pharmacokinetic characteristics .

HY-153950

CDK7-IN-22	CDK	Cancer
CDK7-IN-22 (compound 101) is an *CDK7* inhibitor with antitumor activity. CDK7-IN-22 shows selectivity on CDK7 .

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