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Cat. No.: HY-152263

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HEMTAC CDK4/6 degrader 1

Name: HEMTAC CDK4/6 degrader 1
Brand: MedChemExpress
SKU: HY-152263
Price: 750.00 USD
Availability: InStock
Rating: 5 (1 reviews)

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HEMTAC CDK4/6 degrader 1 is a PROTAC connected by ligands for HSP90 and CDK4/6 with a K_d value of 35.7 μM. HEMTAC CDK4/6 degrader 1 induces CDK4/6 degradation in B16F10 melanoma cells. HEMTAC CDK4/6 degrader 1 arrests cell cycle at G0/G1 phase and induces apoptosis. HEMTAC CDK4/6 degrader 1 can be used in research of cancer. HEMTAC CDK4/6 degrader 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

For research use only. We do not sell to patients.

Purity: 98.18%
CAS No.: 2821803-61-4
Formula: C₄₈H₅₃ClN₁₆O₄
Molecular Weight:953.49

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

HEMTAC CDK4/6 degrader 1 Chemical Structure

CAS No.: 2821803-61-4

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

HEMTAC CDK4/6 degrader 1 is a PROTAC connected by ligands for HSP90 and CDK4/6 with a K_d value of 35.7 μM. HEMTAC CDK4/6 degrader 1 induces CDK4/6 degradation in B16F10 melanoma cells. HEMTAC CDK4/6 degrader 1 arrests cell cycle at G0/G1 phase and induces apoptosis. HEMTAC CDK4/6 degrader 1 can be used in research of cancer^[1]. HEMTAC CDK4/6 degrader 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

IC₅₀ & Target^[1]

CDK4

CDK6

Hsp90TACs

All Hsp-targeting Chimeras Isoforms :

All CDK Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A-375	IC₅₀	0.126 μM Compound: 26	Cytotoxicity against human A-375 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Cytotoxicity against human A-375 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 36574496]
A549	IC₅₀	0.86 μM Compound: 26	Cytotoxicity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Cytotoxicity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 36574496]
B16-F10	IC₅₀	0.112 μM Compound: 26	Cytotoxicity against mouse B16-F10 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Cytotoxicity against mouse B16-F10 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 36574496]
HepG2	IC₅₀	0.499 μM Compound: 26	Cytotoxicity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Cytotoxicity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 36574496]
MDA-MB-231	IC₅₀	0.313 μM Compound: 26	Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 36574496]

In Vitro

HEMTAC CDK4/6 degrader 1 (compound 26; 0.01-1 μM; 24 h) induces CDK4 and CDK6 degradation in the treated B16F10 cells with a DC₅₀ value (the drug concentration that results in 50% protein degradation) of approximately 26 and 19 nM and a D_max (maximal percent degradation) of 88 and 92%, respectively^[1].
HEMTAC CDK4/6 degrader 1 (0.01-100 μM; 72 h) has anti-proliferative activity against a broad range of human cancer cell lines^[1].
HEMTAC CDK4/6 degrader 1 (250 nM; 24 or 48 h) induces B16F10 cells to undergo apoptosis in a dose-dependent manner and arrests cell cycle at G0/G1 phase^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[1]

Cell Line:

B16F10, A375, HepG2, MDA-MB-231, and A549 cells
Concentration:

0.01-100 μM
Incubation Time:

72 hours
Result:

Inhibited cell growth in a dose-dependent manner.

Apoptosis Analysis^[1]

Cell Line:

B16F10 cells
Concentration:

250 nM
Incubation Time:

48 hours
Result:

Induced cell apoptosis in a dose-dependent manner.

Cell Cycle Analysis^[1]

Cell Line:

B16F10 cells
Concentration:

250 nM
Incubation Time:

48 hours
Result:

Increased the amount of B16F10 cells in the G0/G1 phase.

Western Blot Analysis^[1]

Cell Line:

B16F10 cells
Concentration:

0.01, 0.05, 0.1, 0.5, and 1 μM
Incubation Time:

24 hours
Result:

Induced CDK4/6 degradation in a dose-dependent manner.

In Vivo

HEMTAC CDK4/6 degrader 1 (compound 26; 20 and 40 mg/kg; i.p.; daily, for 15 d) has antitumor efficacy in C57BL/6J mice bearing B16F10 melanoma xenografts^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

C57BL/6J mice bearing B16F10 melanoma xenografts^[1]
Dosage:

20 and 40 mg/kg
Administration:

intraperitoneal injection; daily, for 15 days
Result:

Inhibited tumor growth and resulted in fewer CDK4/6-positive cells and led to much more necrosis.

Chemical Information

CAS No. 2821803-61-4
Appearance Solid
Molecular Weight 953.49
Formula C₄₈H₅₃ClN₁₆O₄
Color Light yellow to green yellow
SMILES

ClC1=C2C(N(C=C2C#CCCN3C=C(N=N3)CNC(CN4CCN(C5=CN=C(C=C5)NC6=NC=C(C7=N6)C(C)=C(C(N7C8CCCC8)=O)C(C)=O)CC4)=O)CC9=NC=C(C(OC)=C9C)C)=NC(N)=N1
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (270 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Li Z, et, al. Targeted Protein Degradation Induced by HEMTACs Based on HSP90. J Med Chem. 2023 Jan 12;66(1):733-751. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

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100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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HEMTAC CDK4/6 degrader 1

All Hsp-targeting Chimeras Isoforms

All CDK Isoforms