|
T22424 |
1-(4-Chloro-3-(trifluoromethyl)phenyl)-3-(4-(4-cyanophenoxy)phenyl)urea
|
|
Apoptosis
,
STAT
|
|
SC-1 is a a derivative of the multiple tyrosine kinase inhibitor sorafenib. SC-1 potently inhibits the phosphorylation of STAT3 by blocking STAT3 phosphorylation and activation, and induces apoptosis in hepatocellular ca... |
|
T5994 |
KPT-6566
|
|
Others
|
|
KPT-6566 is a novel selective covalent pin1 inhibitor, KPT-6566 shows an IC50 of 640 nM and a Ki of 625.2 nM for PIN1 PPIase domain,and has anti-cancer activity. |
|
T2378 |
RGB-286638 free base
|
|
GSK-3
,
MEK
,
JAK
,
CDK
|
|
RGB-286638 free base is a novel CDK inhibitor with IC50s of 1 nM/2 nM/3 nM/4 nM/5 nM for cyclin T1-CDK9/cyclin B1-CDK1/cyclin E-CDK2/cyclin D1-CDK4/cyclin E-CDK3/p35-CDK5 respectively; less potent against cyclin H-CDK7 a... |
|
T15335 |
FN-1501
|
|
FLT
,
CDK
|
|
FN-1501 is a potent FLT3 and CDK inhibitor (IC50s: 2.47, 0.85, 1.96, and 0.28 nM for CDK2/cyclin A, CDK4/cyclin D1, CDK6/cyclin D1 and FLT3, respectively). FN-1501 also has anticancer activity. |
|
T21720 |
GP-82996
|
Cdk4/6 Inhibitor IV,CINK4 |
CDK
|
|
GP-82996 (CINK4) is a pharmacological inhibitor specifically targeting CDK4/6, exhibiting IC50 values of 1.5 μM for CDK4/cyclin D1, 5.6 μM for CDK6/cyclin D1, and 25 μM for Cdk5/p35. It effectively induces apoptosis in U... |
|
T60485 |
DIF-3
|
|
|
|
DIF-3 is a chemical compound that acts by activating GSK-3β to facilitate the degradation of cyclin D1 and c-Myc, resulting in reduced expression levels of these proteins. In addition, DIF-3 inhibits Wnt/β-catenin signal... |
|
T39957 |
CDK4/6-IN-6
|
|
CDK
|
|
CDK4/6-IN-6 is a potent CDK4/CDK6 inhibitor with Ki of 0.6 nM and 13.9 nM for CDK4/Cyclin D1 and CDK6/Cyclin D3, respectively. |
|
T2059 |
Purvalanol A
|
NG-60 |
Apoptosis
,
CDK
,
Autophagy
|
|
Purvalanol A (NG-60) is an effective and cell-permeable CDK inhibitor with IC50 of 70/4/35/850 nM for cdk2-cyclin A/B/E, and cdk4-cyclin D1, respectively. |
|
T3207 |
Briciclib
|
ON 014185 |
CDK
,
PERK
,
Autophagy
|
|
Briciclib (ON 014185) is a small molecule that suppresses cyclin D1 accumulation in Y cells. |
|
T16391 |
ON-013100
|
|
CDK
|
|
ON-013100 is an antineoplastic drug. ON-013100 also acts as a mitotic inhibitor that could inhibit Cyclin D1 expression. |
|
T15137 |
DK419
|
|
Wnt/beta-catenin
,
AMPK
|
|
DK419 is an orally active inhibitor of Wnt/β-catenin signaling, with an IC50 of 0.19 μM. DK419 decreases protein lelvels of Axin2, β-catenin, c-Myc, Cyclin D1 and Survivin.It also induces production of pAMPK. |
|
T11826 |
LCH-7749944
|
GNF-PF-2356 |
Apoptosis
,
PAK
|
|
LCH-7749944 (GNF-PF-2356) effectively suppresses the proliferation of human gastric cancer cells through downregulation of PAK4/c-Src/EGFR/cyclin D1 pathway and induces apoptosis. LCH-7749944 is a potent PAK4 inhibitor w... |
|
T2615 |
Flavopiridol hydrochloride
|
Alvocidib Hydrochloride,NSC 649890,MDL 107826A,HL 275,FLAVOPIRIDOL HCL,NSC 649890 HCl |
HIV Protease
,
CDK
,
Autophagy
|
|
Flavopiridol hydrochloride (MDL 107826A) is a synthetic N-methylpiperidinyl chlorophenyl flavone compound. As an inhibitor of cyclin-dependent kinase, alvocidib induces cell cycle arrest by preventing phosphorylation of ... |
|
T14665L |
Motixafortide TFA(664334-36-5,Free)
|
TF 14016 TFA,BKT140 TFA,BL-8040 TFA,T140 TFA |
CXCR
|
|
Motixafortide TFA(664334-36-5,Free) (BKT140 TFA) is an antagonist of CXCR4 with IC50 of ～1 nM. It induces the apoptosis of AML blasts by down-regulating ERK, BCL-2, MCL-1 and cyclin-D1 via altered miR-15a/16-1 expression... |
|
T3708 |
BP-1-102
|
|
STAT
|
|
BP-1-102 is an orally active, effective and specific STAT3 inhibitor. BP-1-102 binds Stat3 (Kd: 504 nM), then blocks Stat3-phosphotyrosine (pTyr) peptide interactions and Stat3 activation (4-6.8 μM), and selectively inhi... |
|
T6312 |
R547
|
Ro 4584820 |
Apoptosis
,
GSK-3
,
PKA
,
CDK
|
|
R547 (Ro 4584820) is a potent ATP-competitive inhibitor of CDK1/2/4 with Ki of 2 nM/3 nM/1 nM. It is less potent to CDK7 and GSK3α/β, while inactive to other kinases. Phase 1. |
|
T6924 |
Riviciclib hydrochloride
|
P276-00 |
Apoptosis
,
CDK
|
|
Riviciclib hydrochloride (P276-00) is a novel CDK1, CDK4 and CDK9 inhibitor with IC50 of 79 nM, 63 nM and 20 nM, respectively. Phase 2/3. |
|
T2082 |
CDK4-IN-1
|
|
CDK
|
|
CDK4 inhibitor is a novel and specific CDK4/Cyclin D1 inhibitor with an IC50 of 10 nM; 1500 and 500 fold than CDK1/Cyclin B (IC50>15 uM) and CDK2/Cyclin A (IC50=5.265 uM) respectively. |
|
T27804 |
LCAHA
|
|
|
|
LCAHA is a USP2a inhibitor. LCAHA inhibits growth of cyclin D1-dependent cells. |
|
T28266 |
Org-6906
|
Org6906,Org 6906,Org-6906 free |
|
|
Tylophorine analog Org-6906 is a potential anticancer and immunosuppressive agent. Org-6906 suppresses the translation of cellular regulatory proteins, including cyclin D1, at the elongation step. Org-6906 allosterically... |
|
T63362 |
Ulecaciclib
|
|
|
|
Ulecaciclib is an orally active, blood-brain barrier-transparent, cell cycle protein-dependent kinase (CDK) inhibitor that exhibits favorable pharmacokinetic profiles, with ki of 0.62 μM (CDK2/Cyclin A), 3 nM (CDK6/Cycli... |
|
T30807 |
CG0009
|
CG-0009,CG 0009 |
|
|
CG0009 is a potent and highly selective glycogen synthase kinase 3 (GSK3) inhibitor that inhibitions proliferation, induces apoptosis, and activates the p53-Bax pathway in breast cancer cells through cyclin D1 depletion.... |
|
T27128 |
DCB-3503
|
NSC716802,NSC 716802,NSC-716802,DCB3503,DCB 3503 |
|
|
Tylophorine analog DCB-3503 is a potential anticancer and immunosuppressive agent. DCB-3503 suppresses the translation of cellular regulatory proteins, including cyclin D1, at the elongation step. DCB-3503 allosterically... |
|
T11653 |
Indirubin-5-sulfonate
|
|
Others
|
|
Indirubin-5-sulfonate shows inhibitory activity against GSK-3β. 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/cycli... |
|
T39956 |
CDK4/6-IN-5
|
CDK4/6-IN-5 |
|
|
CDK4/6-IN-5 is a highly effective inhibitor of CDK4 and CDK6, with Ki values of 0.2 and 4.4 nM for CDK4/Cyclin D1 and CDK6/Cyclin D3, respectively (WO2019207463A1, example A93). |
|
T12737 |
Riviciclib
|
P276-00 (free base) |
Others
|
|
Riviciclib is a potent inhibitor of cyclin-dependent kinase (CDK)(CDK9-cyclinT1, CDK4-cyclin D1, and CDK1-cyclinB with IC50s of 20 nM, 63 nM, and 79 nM, respectively),with antitumor activity on cisplatin-resistant cells. |
|
TP2133 |
[Ala92]-p16 (84-103)
|
|
|
|
Peptide derived from the tumor suppressor protein p16; inhibits cyclin-dependent kinase-4 (cdk4)/cyclin D1 (IC50 ~ 1.5 μM) and binds to cdk6. |
|
T38927 |
SR-1277
|
|
|
|
SR-1277 is a highly potent, selective, and ATP competitive inhibitor of CK1δ/ε, with IC50 values of 49 nM and 260 nM, respectively. Additionally, SR-1277 exhibits inhibitory effects on FLT3, CDK4/cyclin D1, CDK6/cyclin D... |
|
T73196 |
RGB-286638
|
|
|
|
RGB-286638 is a multi-target CDK inhibitor that effectively hampers the kinase activity of a range of cyclin-CDK complexes, including cyclin T1-CDK9 (IC50 = 1 nM), cyclin B1-CDK1 (IC50 = 2 nM), cyclin E-CDK2 (IC50 = 3 nM... |
|
T72829 |
β-catenin-IN-4
|
|
|
|
β-Catenin-IN-4 is a β-catenin inhibitor characterized by a K_i value of 0.64 μM. This compound effectively lowers the protein expression levels of cyclin D1 and c-Myc. |
|
T61266 |
CA224
|
|
|
|
CA224 (Compound 1), an orally active and selective Cdk4–cyclin D1 inhibitor, demonstrates an IC50 of 6.2 µM. It induces cell apoptosis and exhibits antitumor activity [1]. |
|
T62192 |
CDK4/6-IN-9
|
|
|
|
CDK4/6-IN-9 (compound 10) is a selective inhibitor of CDK4/6, capable of acting on CDK6/cyclin D1 (IC50: 905 nM). CDK4/6-IN-9 has potential research value in multiple myeloma (MM). |
|
T82762 |
Cdc25A (80-93) (human)
|
|
|
|
Cdc25A (80-93) (human) is a polypeptide implicated in the regulation of cell proliferation and tumorigenesis through modulation of cyclin D1 expression and facilitation of the G1/S phase transition. This compound has app... |
|
T83433 |
1D228
|
|
c-Met/HGFR
|
|
1D228, a c-Met/TRK inhibitor with antitumor properties, suppresses cyclin D1 to precipitate G0/G1 arrest, thereby inhibiting proliferation and migration of cancer cells. This compound is applicable in researching gastric... |
|
T63982 |
Anticancer agent 50
|
|
|
|
Anticancer agent 50 (compound 6) is a potent modulator of the ABCB1 efflux pump with cytotoxic and anti-proliferative activity. anticancer agent 50 reduces the expression of cyclin D1 and induces p53 expression. anticanc... |
|
T70273 |
APTO-253 HCl
|
|
|
|
APTO-253, also known as LOR-253, LT-253, is a small molecule inhibitor of human metal-regulatory transcription factor 1 (MTF-1) with potential antitumor activity. MTF-1 inhibitor LOR-253 inhibits MTF-1 activity and there... |
|
T62514 |
HDAC-IN-46
|
|
|
|
HDAC-IN-46 (compound 12c) is a potent inhibitor of HDAC that acts on HDAC1 (IC50: 0.21 μM) and HDAC6 (IC50: 0.021 μM). HDAC-IN-46 upregulates p-p38 and downregulates Bcl-xL and cyclin D1 in MDA-MB-231 cells. HDAC-IN-46 c... |
|
T41278 |
Obatoclax
|
|
|
|
Obatoclax (GX15-070), a pan-BCL-2 family proteins inhibitor and BH3 mimetic, exhibits a binding affinity (K_i) of 220 nM for BCL-2. It promotes autophagy-dependent cell death and cyclin D1 degradation via the proteasome.... |
|
T72522 |
Aurora kinase-IN-1
|
|
|
|
Aurora kinase-IN-1, a potent aurora kinase inhibitor, modulates cell cycle progression and induces apoptosis by upregulating G1 cell cycle inhibitory proteins (including p21 and p27), elevating G1 progressive cyclin D1, ... |
|
T68980 |
MRK003
|
|
|
|
MRK003 is a γ-secretase inhibitor exhibits promising in vitro pre-clinical activity in multiple myeloma and non-Hodgkin's lymphoma. MRK003 treatment induced caspase-dependent apoptosis and inhibited proliferation of MM a... |
|
T70706 |
APTO-253 isomer
|
|
|
|
APTO-253 isomer is an isomer of APTO-253 with the Fluoro-atom in 6-position. APTO-253 also known as LOR-253, LT-253, is a small molecule inhibitor of human metal-regulatory transcription factor 1 (MTF-1) with potential ... |
|
T29172 |
YD277
|
YD 277,YD-277 |
|
|
YD277 is a small molecule derived from ML264, a KLF5 inhibitor that elicits cytotoxic effects in colon cancer cell lines. YD277 significantly induced G1 cell cycle arrest and apoptosis in MDA-MB-231 and MDA-MB-468 TNBC c... |
|
T69221 |
BMS-554417
|
|
|
|
BMS-554417 is a novel inhibitor of IGF-IR, which inhibits IGF-IR and insulin receptor kinase activity and proliferation in vitro, and reduces tumor xenograft size in vivo. In a series of carcinoma cell lines, the IC50 fo... |
|
T36844 |
Inostamycin A
|
|
|
|
Inostamycin A is a bacterial metabolite that has been found inStreptomycesand has anticancer activity.1It is an inhibitor of CDP-diacylglycerol:inositol 3-phosphatidyltransferase (IC50= 0.02 μg/ml in A431 cell membranes)... |
