| DC49564 |
PERK-IN-5 |
PERK-IN-5 is a highly potent, selectively and orally bioavailable PERK inhibitor (IC50s of 2 and 9 nM for PERK and p-eIF2α, respectively). PERK-IN-5 can significantly inhibit tumor growth in the 786-O renal cell carcinoma xenograft tumor model. |
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| DC49565 |
AS1892802 |
AS1892802 is a potent, orally active, and highly selective inhibitor of ROCK. The onset of antinociceptive effect of AS1892802 is as fast as those of Tramadol and Diclofenac. AS1892802 did not induce gastric irritation or abnormal behavior. AS1892802 is an attractive analgesic profile for the research of severe osteoarthritis pain. |
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| DC49566 |
Corydamine |
Corydamine, 3-arylisoquinoline alkaloid, is a potent DNA topoisomerase I/II inhibitor. Corydamine has anti-cancer activity. |
|
| DC49567 |
Topoisomerase I/II inhibitor 2 |
Topoisomerase I/II inhibitor 2 (compound 1a) is a potent Topoisomerase inhibitor (IC50= 9.82 μM on Huh7 cells and 6.83 μM on LM9 cells). Topoisomerase I/II inhibitor 2 has dual inhibition on DNA topoisomerase I/II, also can obviously reduce the growth of xenograft tumor in mice model. Topoisomerase I/II inhibitor 2 has the potential value in treating liver cancer. |
|
| DC49568 |
MM41 |
MM41 is a potent stabilizer of human telomeric and gene promoter DNA quadruplexes. MM41 is potently against the MIA PaCa-2 pancreatic cancer cell line with IC50 value of <10 nM. |
|
| DC49569 |
L5-DA |
L5-DA is a G-quadruplex (G4) ligand and selectively stabilized for G4s over ds26. L5-DA exhibits significant cytotoxicity against HeLa cells (IC50=4.3 μM). L5-DA stabilizes G4s in HeLa cells, induces apoptosis, and cell cycle arrest. |
|
| DC50173 |
dCeMM4
Featured
|
dCeMM4 (Compound 5) is a glue degrader. dCeMM4 induces ubiquitination and degradation of cyclin K by prompting an interaction of CDK12-cyclin K with a CRL4B ligase complex. |
|
| DC50174 |
(E/Z)-Zotiraciclib hydrochloride |
(E/Z)-Zotiraciclib ((E/Z)-TG02) hydrochloride is a potent CDK2, JAK2, and FLT3 inhibitor. |
|
| DC50175 |
CDK4/6-IN-11 |
CDK4/6-IN-11 is a potent PROTAC CDK4/6 degrader. |
|
| DC50176 |
(R)-CTX-712 |
(R)-CTX-712 is a potent inhibitor of cdc2-like kinase (CLK). (R)-CTX-712 inhibits CLK kinase activity, and thus inhibits cancer survival and cancer cell growth. (R)-CTX-712 has the potential for the research of cancer disease (extracted from patent JPWO2017188374A1, compound 286). |
|
| DC50177 |
CDK7-IN-2 |
CDK7-IN-2 is a potent inhibitor of CDK7. CDK7 is implicated in both temporal control of the cell cycle and transcriptional activity. CDK7 is implicated in the transcriptional initiation process by phosphorylation of Rbpl subunit of RNA Polymerase II (RNAPII). CDK7 has the potential for the research of cancer disease, in particular aggressive and hard- to-treat cancers (extracted from patent WO2019099298A1, compound 1). |
|
| DC50178 |
CDK5-IN-3 |
CDK5-IN-3 (compound 11) is a potent and selective CDK5 inhibitor, with IC50s of 0.6 nM and 18 nM for CDK5/p25 and CDK2/CycA, respectively. CDK5-IN-3 can be used for the research of autosomal dominant polycystic kidney disease (ADPKD). |
|
| DC50179 |
SZ-015268 |
SZ-015268 is a CDK7 inhibitor with an IC50 of 23.56 nM. SZ-015268 has extremely significant anti-tumor advantages. SZ-015268 inhibits HCC70, OVCAR-3, HCT116 and HCC1806 cells proliferation with IC50s of 33, 80.56, 12.53, and 61.55 nM, respectively. |
|
| DC50180 |
CDK7-IN-12 |
CDK7-IN-12 is a potent inhibitor of CDK7. CDK7-IN-12 plays a key role in transcriptional regulation and cell cycle regulation. CDK7-IN-12 effectively inhibit malignant tumor proliferation in vitro and in vivo. CDK7-IN-12 has the potential for the research of cancer disease (extracted from patent WO2021249417A1, compound 43). |
|
| DC50181 |
CDK1-IN-1 |
CDK1-IN-7 is a potent CDK1 inhibitor (CDK1/CycB IC50=161.2 nM) with potential antiproliferative activity and selectivity for cancer tissues. CDK1-IN-7 induces apoptosis in p53 dependent manner through the intrinsic apoptotic pathway. CDK1-IN-7 is a potential targeted antitumor agent. |
|
| DC50182 |
FLT3/CDK4-IN-1 |
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. |
|
| DC50183 |
dCeMM2 |
dCeMM2 (Compound 2) is a glue degrader. dCeMM2 induces ubiquitination and degradation of cyclin K by prompting an interaction of CDK12-cyclin K with a CRL4B ligase complex. |
|
| DC50184 |
dCeMM3
Featured
|
dCeMM3 (Compound 3) is a glue degrader. dCeMM3 induces ubiquitination and degradation of cyclin K by prompting an interaction of CDK12-cyclin K with a CRL4B ligase complex. |
|
| DC50185 |
NSC693868 |
NSC693868 is a selective inhibitor of CDK1 and CDK5 with IC50s of 600 nM and 400 nM, respectively. NSC693868 less potently inhibits GSK3β with an IC50 of 1 µM) and does not block CDC25 activity. NSC693868 is used to help define the roles of CDK1 and CDK5 in various signaling pathways. |
|
| DC50186 |
5,6-Dichlorobenzimidazole riboside(DBR)
Featured
|
5,6-Dichlorobenzimidazole riboside is a nucleoside analog that inhibits several carboxyl-terminal domain (CTD) kinases including casein kinase II and CDKs. 5,6-Dichlorobenzimidazole riboside trigger p53-dependent apoptosis of human colon adenocarcinoma cells without inducing genotoxic stress to healthy cells. |
|
| DC50188 |
(E/Z)-Zotiraciclib citrate |
(E/Z)-Zotiraciclib citrate is a potent CDK2, JAK2, and FLT3 inhibitor. |
|
| DC50189 |
Anticancer agent 30 |
Anticancer agent 30 (compound 6f-Z), a 3-arylidene-2-oxindole derivative, is a selective CDK2 inhibitor with potent anticancer activity. |
|
| DC50191 |
Anticancer agent 29 |
Anticancer agent 29 (Compd E/Z-6f) is an anticancer agent, with IC50 values of 0.054 μM, 0.127 μM, 0.129 μM, 0.396 μM for CDK2, CDK1, CDK4 and CDK6, respectively. |
|
| DC50192 |
DD-03-156 |
DD-03-156 is a potent and selective degrader of CDK17 and LIMK2. The selectivity and potency of DD-03-156 is exquisite and makes an advanced starting point for the development of a chemical probe for the degradation of CDK17. |
|
| DC70063 |
CFI-402257(luvixasertib)
Featured
|
CFI-402257(luvixasertib) is a potent and selective Mps1/TTK kinase inhibitor with Ki of 0.1 nM and cellular Mps1 EC50 of 6.5 nM. |
|
| DC70071 |
THZ-1 hydrochloride |
THZ-1 hydrochloride is a potent, selective, covalent CDK7 inhibitor with IC50 of 3.2 nM. |
|
| DC70085 |
Nedisertib (Synonyms: Peposertib; M3814)
Featured
|
Nedisertib (M3814, MSC2490484A) is a highly potent, selective, orally bioavailable inhibitor of DNA-PK. |
|
| DC70109 |
(R)-CR8
Featured
|
(R)-CR8 is a potent CDK1/2/5/7/9 inhibitor, inhibits CDK1/cyclin B (IC50, 90 nM), CDK2/cyclin A (72 nM), CDK2/cyclin E (41 nM), CDK5/p25 ( 110 nM), CDK7/cyclin H (1.1 uM), CDK9/cyclin T (0.18 uM) and CK1δ/ε (0.4 uM);
(R)-CR8 induces apoptosis and has neuroprotective effect, CR8 alsp acts as a molecular glue degrader that depletes cyclin K. |
|
| DC70116 |
3-Deazauridine |
3-Deazauridine (DAU, NSC 126849) is a nucleoside analog that competitively inhibits cytidine triphosphate synthetase (CTP).3-Deazauridine inhibits the growth of L1210 leukemia cells when used at a concentration of 6 µM and dose-dependently reduces mortality in a mouse model of leukemia.3-Deazauridine selectively suppresses cell viability in a MYC-dependent manner in ARPE-19 cells.3-Deazauridine causes selective replication stress in MYC-overexpressing cells, which originates from MYC-driven rRNA synthesis.3-Deazauridine combined with ATR inhibitor BAY-1895344 induces synthetic lethality to MYC-overexpressing cells, and suppresses tumor growth in 3D assays and in vivo. |
|
| DC70137 |
Nek2 inhibitor 11 |
A potent, ATP-competitive and relative selective Nek2 inhibitor with IC50 of 0.67 uM; displays >10-fold selectivity over CDK2. |
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