| S9665 |
Motixafortide (BL-8040) |
Motixafortide (BL-8040, BKT140, TF 14016, 4-fluorobenzoyl, 4F-benzoyl-TN14003, T140) is an antagonist of CXCR4 with IC50 of ～1 nM. BL-8040 induces the apoptosis of AML blasts by down-regulating ERK, BCL-2, MCL-1 and cyclin-D1 via altered miR-15a/16-1 expression. |
Selective |
|
| S9880 |
MS140 |
MS140 is a specific and highly potent CDK4/6 kinase inhibitor and also a CDK4/6 degrader (PROTAC). |
Pan |
|
| S8389 |
Trilaciclib |
Trilaciclib is a highly potent, selective and reversible cyclin-dependent kinase 4 and 6 (CDK4/6) inhibitor. Trilaciclib inhibits CDK4/cyclin D1 and CDK6/cyclin D3 with IC50 of 1 nM and 4 nM, respectively. |
Pan |
CDK4/cyclin D1, IC50: 1 nM |
| S2688 |
R547 |
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. |
Pan |
CDK4/CyclinD1, Ki: 1 nM |
| S8568 |
G1T38 |
G1T38 (Lerociclib) is a novel, potent, selective, and orally bioavailable CDK4/6 inhibitor with IC50 values of 0.001 μM, 0.002 μM and 0.028 μM for CDK4, CDK6 and CDK9 respectively. |
Pan |
CDK4, IC50: 1 nM |
| S8816 |
PF-06873600 |
PF-06873600 is an inhibitor of cyclin-dependent kinase 2 (CDK2), CDK4, and CDK6 with Ki values of 0.1, 1.2, and 0.1 nM, respectively, blocks the phosphorylation of retinoblastoma protein (RB1), and limits the proliferation of OVCAR-3 ovarian cancer cells with EC50s of 19 and 45 nM, respectively. |
Pan |
CDK4, Ki: 1.2 nM |
| S7158 |
Abemaciclib mesylate |
Abemaciclib mesylate is a potent and selective inhibitor of CDK4 and CDK6 with IC50 of 2 nM and 10 nM in cell-free assays, respectively. Phase 3. |
Pan |
CDK4, IC50: 2 nM |
| S5716 |
Abemaciclib |
Abemaciclib is a cell cycle inhibitor selective for CDK4/6 with IC50 of 2 nM and 10 nM in cell-free assays, respectively. |
Pan |
CDK4, IC50: 2 nM |
| S8161 |
ON123300 |
ON123300 is a potent and multi-targeted kinase inhibitor with IC50 of 3.9 nM, 5 nM, 26 nM, 26 nM, 9.2 nM and 11nM for CDK4, Ark5/NUAK1, PDGFRβ, FGFR1, RET (c-RET), and Fyn, respectively. |
Pan |
CDK4/CyclinD1, IC50: 3.87 nM |
| S7773 |
CDKI-73 |
CDKI-73 (LS-007) is a potent CDK inhibitor in vitro with IC50 of 8.17 nM, 3.27 nM, 8.18 nM, and 5.78 nM for CDK1, CDK2, CDK4, and CDK9, respectively. CDKI-73 induces apoptosis in cancer cells. CDKI-73 is an orally bioavailable and highly efficacious CDK9 inhibitor against acute myeloid leukemia. |
Pan |
CDK4, IC50: 8.18 nM |
| S1579 |
Palbociclib Isethionate |
Palbociclib Isethionate is a highly selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM in cell-free assays. It shows no activity against CDK1/2/5, EGFR, FGFR, PDGFR, InsR, etc. Phase 3. |
Pan |
CDK4/CyclinD1, IC50: 11 nM; CDK4/CyclinD3, IC50: 9 nM |
| S1116 |
Palbociclib (PD-0332991) HCl |
Palbociclib (PD-0332991) HCl is a highly selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM in cell-free assays, respectively. It shows no activity against CDK1/2/5, EGFR, FGFR, PDGFR, InsR, etc. Phase 3. |
Pan |
CDK4/CyclinD1, IC50: 11 nM; CDK4/CyclinD3, IC50: 9 nM |
| S7440 |
Ribociclib |
Ribociclib is an orally available, and highly specific inhibitor of CDK4 and CDK6 with IC50 of 10 nM and 39 nM. Phase 3. |
Pan |
CDK4, IC50: 10 nM |
| S5187 |
Ribociclib hydrochloride |
Ribociclib (LEE011) hydrochloride is a highly specific dual inhibitor of CDK4 and CDK6 with IC50 of 10 nM and 39 nM, respectively. |
Pan |
CDK4, IC50: 10 nM |
| S5188 |
Ribociclib succinate |
Ribociclib (LEE011) succinate (Kisqali) is a highly specific dual inhibitor of CDK4 and CDK6 with IC50 of 10 nM and 39 nM, respectively. |
Pan |
CDK4, IC50: 10 nM |
| S4482 |
Palbociclib |
Palbociclib (PD 0332991) is a highly specific inhibitor of cyclin-dependent kinase 4 (Cdk4) and Cdk6 with IC50 of 11 nM and 16 nM, respectively.This product has poor solubility, animal experiments are available, cell experiments please choose carefully! |
Pan |
Cdk4, IC50: 11 nM |
| S1230 |
Flavopiridol (Alvocidib) |
Flavopiridol (Alvocidib) competes with ATP to inhibit CDKs including CDK1, CDK2, CDK4, CDK6, and CDK9 with IC50 values in the 20-100 nM range. It is more selective for CDK1, 2, 4, 6, 9 versus CDK7. Flavopiridol is initially found to inhibit EGFR and PKA. Flavopiridol induces autophagy and ER stress. Flavopiridol blocks HIV-1 replication. Phase 1/2. |
Pan |
CDK4, IC50: 20-40 nM |
| S2679 |
Flavopiridol (L86-8275) HCl |
Flavopiridol HCl (L86-8275, NSC 649890, Alvocidib, HMR-1275, DSP-2033) competes with ATP to inhibit CDKs including CDK1, CDK2, CDK4 and CDK6 with IC50 of ~ 40 nM in cell-free assays. It is 7.5-fold more selective for CDK1/2/4/6 than CDK7. Flavopiridol is initially found to inhibit EGFR and PKA. Flavopiridol HCl induces autophagy and ER stress. Flavopiridol HCl blocks HIV-1 replication. Phase 1/2. |
Pan |
CDK4, IC50: 40 nM |
| S1487 |
PHA-793887 |
PHA-793887 is a novel and potent inhibitor of CDK2, CDK5 and CDK7 with IC50 of 8 nM, 5 nM and 10 nM. It is greater than 6-fold more selective for CDK2, 5, and 7 than CDK1, 4, and 9. PHA-793887 induces cell-cycle arrest and apoptosis. Phase 1. |
Pan |
CDK4/CyclinD1, IC50: 62 nM |
| S8058 |
Riviciclib hydrochloride (P276-00) |
Riviciclib hydrochloride (P276-00) is a novel CDK1, CDK4 and CDK9 inhibitor with IC50 of 79 nM, 63 nM and 20 nM, respectively. Riviciclib hydrochloride (P276-00) induces apoptosis. Phase 2/3. |
Pan |
CDK4/CyclinD1, IC50: 63 nM |
| S7808 |
AT7519 HCl |
AT7519 HCl is a multi-CDK inhibitor for CDK1, 2, 4, 6 and 9 with IC50 of 10-210 nM in cell-free assays. It is less potent to CDK3 and little active to CDK7. Phase 2.
|
Pan |
CDK4/CyclinD1, IC50: 100 nM |
| S1524 |
AT7519 |
AT7519 is a multi-CDK inhibitor for CDK1, 2, 4, 6 and 9 with IC50 of 10-210 nM. It is less potent to CDK3 and little active to CDK7. AT7519 also decrease GSK3β phosphorylation. AT7519 induces apoptosis. Phase 2. |
Pan |
CDK4/CyclinD1, IC50: 100 nM |
| S8809 |
MC180295 |
MC180295 ((rel)-MC180295) is a novel potent and selective CDK9 inhibitor with an IC50 of 5 nM and is at least 22-fold more selective for CDK9 over other CDKs. |
Pan |
CDK4-Cyclin D, IC50: 112 nM |
| S2751 |
Milciclib |
Milciclib is a potent, ATP-competitive CDK inhibitor for CDK2 with IC50 of 45 nM. It is >3-fold more selective for CDK2 than CDK1, 2, 4, 5, and 7, it's also an inhibitor of TRKA with IC50 of 53nM. Milciclib (PHA-848125) induces cell death through autophagy. Phase 2. |
Pan |
CDK4/CyclinD1, IC50: 160 nM |
| S7636 |
SU9516 |
SU 9516 is a 3-substituted indolinone CDK inhibitor with IC50 of 22 nM, 40 nM, and 200 nM for CDK2, CDK1, and CDK4, respectively.
|
Pan |
CDK4, IC50: 200 nM |
| S2014 |
BMS-265246 |
BMS-265246 is a potent and selective CDK1/2 inhibitor with IC50 of 6 nM/9 nM in a cell-free assay. It is 25-fold more selective for CDK1/2 than CDK4. |
Pan |
CDK4/CyclinD, IC50: 230 nM |
| S1249 |
JNJ-7706621 |
JNJ-7706621 is a pan-CDK inhibitor with the highest potency on CDK1/2 with IC50 of 9 nM/4 nM and showing >6-fold selectivity for CDK1/2 than CDK3/4/6 in cell-free assays. It also potently inhibits Aurora A/B and has no activity on Plk1 and Wee1. |
Pan |
CDK4/CyclinD1, IC50: 253 nM |
| S7793 |
Purvalanol A |
Purvalanol A is a potent, and cell-permeable CDK inhibitor with IC50 of 4 nM, 70 nM, 35 nM, and 850 nM for cdc2-cyclin B, cdk2-cyclin A, cdk2-cyclin E, and cdk4-cyclin D1, respectively. Purvalanol A induces endoplasmic reticulum stress-mediated apoptosis and autophagy. |
Pan |
CDK4/CyclinD1, IC50: 850 nM |
| S2009 |
Indirubin-3'-monoxime |
Indirubin-3'-monoxime (Indirubin-3'-oxime) is a selective CDK inhibitor with IC50 of 0.18 μM, 0.44 μM, 0.25 μM, 3.33 μM, 0.065 μM for CDK1-cyclinB, CDK2-cyclinA, CDK2-cyclinE, CDK4-cyclinD1, CDK5-p35,respectively. Indirubin-3'-monoxime is a direct and selective 5-lipoxygenase inhibitor with IC50 of 7.8-10 µM. |
Pan |
CDK4-cyclinD1, IC50: 3.33 μM |
| S3238 |
Resibufogenin |
Resibufogenin (Bufogenin, Recibufogenin), a component of huachansu with anticancer effect, triggers necroptosis through upregulating receptor-interacting protein kinase 3 (RIP3) and phosphorylating mixed lineage kinase domain-like protein at Ser358. Resibufogenin exerts cytotoxic effect by inducing reactive oxygen species (ROS) accumulation. Resibufogenin induces apoptosis and caspase-3 and caspase-8 activity. Resibufogenin increases Bax/Bcl-2 exp |
Pan |
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